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1un.

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1un.20ll
Screening Libraries
Proteins/Peptides
APIs
siRNAs
Selleck pre-defined or custom siRNA libraries in human and mouse are available in any of
our three market-leading siRNA technologies for screens with efficient, specific and
guaranteed knockdown.
Selleck compound libraries contain over 1000 unique and diverse bioactive compounds
suitable for high-throughput screening, cell based high-content screening and chemical
biology applications.
Selleck provides about 400 kinds of fine Active Pharmaceutical Ingredients (APIs) and
120 kinds of natural products for global customers.
Selleck produces over 300 grow factors, enzymes, cytokines and chemokines. We also
specialize in both peptide synthesis and peptide modifications.
Selleck provides high purity small molecule inhibitors on signaling pathways such as
Apoptosis, Akt, MAPK, angiogenesis etc.
Antibodies
Selleck offers a broad selection of monoclonal and polyclonal antibodies to human proteins
for various applications, including Western blot, immunohistochemistry, immunofluores-
cence, flow cytometry and more.
Inhibitors
Whats in it for me?
Selleck is one of the world leading suppliers of high-performance life-science
products. We have over 8,000 products which consist of inhibitors, antibodies,
RNAis, proteins and peptides those which focus on signaling pathways such
as MAPK, PI3K/Akt, and apoptosis. Furthermore, compound libraries for high-
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Selleck pays great attention to the purity, stability and activity of the products.
Not only could Selleck provides the chemical test data, such as HNMR, LC-MS
and HPLC, but also provides the reviews overall evaluations of the products
from the customers who have used our products. Western Blot, MTT, RT-PCR,
ICH photos and figures provide double guarantee for the biological activities
of our products in life-science research. If our products have any quality prob-
lems, we will unconditionally refund or replace the products .
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Selleck has been leading the way in biology, medical and pharmaceutical science
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Selleck has established long-term and stable relationships with more than 10,000
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Our goal is to provide scientists worldwide an easy access to the most innovative
life science reagents, and to help them make more significant discoveries.
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Table of Contents
EGFR
VEGFR/PDGFR
FGFR
Src-Bcl-Abl
IGF-IR
HER2
c-Kit
c-Met
FLT-3
ALK
Vascular Disrupting Agent
ETA receptor
HIF
Syk
Tie2
1 Angiogenesis/Tyrosine Kinase Pathway
3
6
11
11
13
13
14
14
15
16
16
16
16
17
17
Cell Cycle/Checkpoint Pathway
18
ROCK
PLK
CDK
Topoisomerase
Microtubule
Antimetabolites
Telomerase
DNA/RNA
Checkpoint
Dihydrofolate reductase
20
20
20
22
22
24
25
25
26
26
HDAC Signaling
HDAC
Sir2-like family deacetylase
27
27
31
Apoptosis
Bcl-2
TNF-alpha
p53
Survivin
32
34
35
35
35
PARP
PARP
36
38
Ksp
Aurora Kinase
Aurora Kinase
40
42
44
MAPK Signaling
MEK
p38 MAPK
B-Raf
JNK
45
47
48
50
50
PI3K/Akt Signaling
PI3K
mTOR
DNA-PK
GSK-3
PDK-1
ATM
Akt
51
53
56
57
57
57
58
58
Hormone
Androgen Receptor
Estrogen receptor
Aromatase
5-alpha-reductase
GPR
59
60
60
61
62
62
Proteases/HSP90/HSP70 Pathway
Proteasome
HSP-70
DPP-4
HSP-90
Aminopeptidase
HCV protease
66
68
68
69
69
70
70
Wnt/Hedgehog/Notch Pathway
Hedgehog
Wnt
VHFUHWDVH
71
72
72
72
Jak/Stat Pathway
Stat
Jak
73
74
74
Ca/cAMP/Lipid Signaling
PKC
75
76
Neuro Signaling Pathway
CGRP
COX
77
78
78
7*)6PDG6LJQDOLQJ
7*)
79
80
Integrase/CCR5 Pathway
CCR5
Integrase
63
65
65
GPCR Pathway
Vasopressin receptor
Angiotensin receptor
CB1 receptor
UHFHSWRU
Serotonin receptor
Smooth hened
mGluR2/mGlu3
81
82
83
83
83
82
82
83
Ion Channel
CFTR
Calcium channel
Proton pump
84
85
85
86
Cytochrome P450
14a-demethylase
87
88
Others
Factor Xa
S1P Receptor
sPLA2
P-glycoprotein
Reverse transcriptase
Xanthine oxidase
Serotonin reuptake
Phosphodiesterase
Acetylcholinesterase
Adrenergic receptor
Histamine
GABA
90
91
91
91
91
92
93
93
94
95
96
97
98
Peptide Inhibitors
CDK
Bcl-2
p38 MAPK
JNK
Oxytocin receptor
Glycoprotein receptor
Vasopressin receptor
LHRHR/GnRHR
PTHR
Melanocortin-1 receptor
PKC
SNAPR
NKR
BDKR/KOR
TRH receptor
CRF receptor
GRF-R
Ghrelin receptor
Tachykinin NK1 receptor
Angiotensin receptor
Secretin receptor
SSTR
GCGR
GHSR
99
100
100
100
100
100
101
101
101
102
103
103
103
103
103
104
104
104
104
105
105
105
105
105
106

Angiogenesis/Tyrosine Kinase
0rcoderesardArd|oderes|s:3|dra||rdT|ree-0|rers|ora|Turor0roWl|.
Janusz Rak, Joanne L Yu et al. J Investig Dermatol Symp Proc. 2000(5):2433.
Tumor growth is dependent on the perpetual recruitment of host blood
vessels to the tumor site. This recruitment process (mainly via angiogenesis) is
thought to be triggered by the very same set of genetic alterations as those
responsible for other aspects of malignant transformation. Potent oncogenes
are able to deregulate expression of both angiogenesis stimulators and inhibitors in
cancer cells. For example, mutant ras expression is associated with increased
production of VEGF and downregulation of TSP-1. Upregulation of VEGF and
angiogenesis can also be induced by constitutive activation of other oncogenic
proteins (e.g., EGFR, Raf, MEK, PI3K) acting at various levels on the Ras
signaling pathway. The mode and the magnitude of such pro-angiogenic
influences can be significantly modified by cell type (fibroblastic or epithelial
origin), epigenetic factors (hypoxia, changes in cell density), and/or presence of
additional genetic lesions.
Activated oncogenes (e.g. ras, src, HER-2) induce co-expression of angiogenic prop-
erties concomitantly with several highly selectable traits (increased mitogen-
esis, resistance to apoptosis). On the other hand oncogene-induced reduction
in growth requirements may also endow tumor cells with a diminished dependence
on proximity to blood vessels. Angiogenesis can be simultaneously suppressed
by effective use of the specific oncogene antagonists and signal transduction
inhibitors.
l
2
S1010 BIBF1120(Vargatef)
Inhibition of Lck enhances glucocorticoid sensitivity and apoptosis in lymphoid cell
lines and in chronic lymphocytic leukemia
MW Harr, PF Caimi, KS et al. Cell Death & Differentiation. 2010(17):1381-1391.
S1012 BMS-536924
PTK6 Regulates IGF-1-Induced Anchorage-Independent Survival
Irie HY, Shrestha Y et al. PLoS ONE. 2010;5(7): e11729.
S1014 Bosutinib(SKI-606)
Inhibition of ser/thr phosphatases induces capacitation-associated signaling in the
presence of Src kinase inhibitors
Krapf D, Arcelay E et al. J. Biol. Chem. 2010(285): 7977-7985.
S1019 CI-1033(Canertinib)
The fibroblast-derived paracrine factor neuregulin-1 has a novel role in regulating the
constitutive color and melanocyte function in human skin
Wonseon Choi, Rainer Wolber et al. J Cell Sci. 2010(123): 3102-3111.
S1021 Dasatinib
Anti-leukemic activity of Dasatinib in both p53wild-type and p53 mutated B malignant cells
Raffaella Bosco, Marco Rabusin et al. Invest New Drugs 2010.
S1021 Dasatinib/ S1026 Imatinib Mesylate
Molecular Characterization of c-Abl/c-Src Kinase Inhibitors Targeted against Murine
Tumour Progenitor Cells that Express Stem Cell Markers
Raffaella Bosco, Marco Rabusin et al. Invest New Drugs 2010.
S1023 Erlotinib Hydrochloride
Dual specificity phosphatase 6(DUSP6) is an ETS-regulated negative feedback mediator
of oncogenic ERK-signaling in lung cancer cells
Zhenfeng Zhang, Susumu Kobayashi et al. Carcinogenesis 2010;31(4): 577-586
Mechanisms of myogenic tone of coronary arteriole: Role of down stream signaling of
the EGFR tyrosine kinase
Ali H. Amin, Zakaria Y et al. Microvascular Research 2011;81(1):135-142
Papers
Using Selleck Products
EGFR (Epidermal growth factor receptor)
EGFR Ard|oderes|s/Tvros|reK|rase
3
S1392 Pelitinib
5mg
25mg
50mg
N
CN
O
N
H
O
N
HN
Cl
F
Synonyms:

EKB-569, WAY-EKB 569
Size Price
5mg
10mg
50mg
5mg
10mg
25mg
25mg
50mg
100mg
N
N
H
N
N
N
NH
S1486 AEE788
AEE788 is a novel dual inhibitor of EGFR/ErbB2 and VEGFR tyrosine kinases (IC50s: EGFR=2 nM, ErbB2=6
nM, KDR=77 nM, and Flt-1=59 nM). AEE788 demonstrated antiproliferative activity against EGFR and
ErbB2-overexpressing cell lines and inhibited the proliferation of human umbilical vein endothelial cells. Oral
administration of AEE788 to mice resulted in high and persistent compound levels in tumor tissue.
Size Price
Synonyms:

NVP-AEE 788
Produced Independently by our customer Dr.Zhang,
Tianjin Medical University
S1011 BIBW2992
Feed
Western blot analysis of extracts from EGF,
BIBW2992 treated T47D breast denocarcinoma
cell line using antibodies as indicated.
S1011 BIBW2992
F
Cl NH
N
N
H
N
O
O
N
O
BIBW2992 shows potent activity against EGFR and HER2. BIBW2992 was effective in inhibiting survival of
H1666 or NCI-H1975 EGFR, with IC50s below 100 nM . Assessed in a standard xenograft model of the
epidermoid carcinoma cell line A431.Daily oral treatment with BIBW2992 at 20 mg/kg for 25 days resulted in
dramatic tumor regression with a cumulative treated/control tumor volume ratio (T/C ratio) of 2%.
Synonyms:

Tovok
Size Price
H1666 or NCI-H1975 EGFR, with IC50s below
N
epidermoid carcinoma cell line A431.Daily oral tre
dramatic tumor regression with a cumulative treat
P-EGFR
0
n
M
1
n
M
0
.
1
n
M
0
.
0
1
n
M
0
n
M
-
+ + + +
EGF(100ng/ml)
BIBW2992
EGFR

S1028 Lapatinib Ditosylate
Lapatinib have IC50 values against purified EGFR and HER2 of 10.2 and 9.8 nM, respectively. And IC50
>10000nM against c-Raf-1, MEK, ERK, CDK1, CDK2, p38 and VEGFR-2.The IC50s for inhibition of cell
JURZWKE\KWUHDWPHQWZLWK*:DUH0IRU$0IRU+10IRU%70IRU
N87. Lapatinib undergoes first-pass metabolism catalyzed by CYP3A4/5 and does not appear to be a
substrate for P-glycoprotein.
Synonyms:

Tykerb, Tyverb, GW-572016
Size Price
N
N
HN Cl
O
F
O
NH
S
O O
S
OH
O
O
S
OH
O
O
1 10 100 1000 10000
0
50
100
lapatinib
lapatinib+7839
Lapatinib conc (nM)
%

c
o
n
t
r
o
l

c
e
l
l

g
r
o
w
t
h
EGF (100ng/ml) + -
beta-Actin
Total Akt
p-Akt (Ser.473)
p-Erk1/2 (Thr.202/Tyr.204)
p-ErbB2 (Tyr.1221/1222)
p-Tyrosine
Total Erk1/2
+ +
+
Lapatinib 0M 0M5M
0.5M0.05MGrowing
-

SKBR3 cells were starved for 4h in
serum-free medium and treated as
indicated; or left growing in complete
medium (last lane).
Sheddase inhibition
improves the ability of
lapatinib to inhibit BT-474
cell growth.
Provided from our customer Carl Uli Bialucha,Cold Spring Harbor
Laboratory ,NY,USA
S1028 Lapatinib
Feed
25mg
50mg
100mg
S1025 Gefitinib
The monolayer growth of these EGF-driven untransformed cells such as MCF10A is inhibited by ZD1839 with
an IC50 of 20 nM, similar to its IC50 in vitro for EGFR and consistent with effective inhibition of EGFR in vivo.
Cell line characteristics and sensitivity to Gefitinib at 1uM are 59% inhibition for MDA-MB-231, 74% inhibition
for A431, 81% inhibition for SKBr3,60% inhibition for SKOV3, 33% inhibition for BT474,52% inhibition for
MCF-7, 28% inhibition for T47D, respectively.
Synonyms:

ZD-1839, Iressa
Size Price
N
N
HN Cl
F
O
O N
O
Data from Oncogene (2010), 114 using our product.
Data provided by our customer
Vicky TinThe University of
Hong Kong.
Effects of shRNA-mediated RECK depletion on EGFR signaling in MEFs.
(a) Immunoblotting (IB) of the indicated proteins in wild-type MEFs
transduced with the indicated shRNAs and cultured for 48 h in the presence
of 0.1% dimethyl sulfoxide(DMSO; vehicle) or 1 mM gefitinib
(S1025, Selleck Chemicals,Houston, TX, USA).
(b) Immunoprecipitation from whole lysates of cells from panel a with
an anti-phosphorylated tyrosine (pTyr) antibody. Precipitates from 500 mg
protein in whole cell lysates (upper) or 20 mg protein in whole cell lysates
(lower) were analyzed by IB with anti-EGFR antibody.
MTT assay result. 0-500nM
Gefitinib (Selleck S1025)
treated with H1299, H358,
H25 and HCC827 cell lines
by 72h, Proliferation rate
was tested.
S1025 Gefitinib
Feed
Pelitinib is a 3-cyanoquinoline pan-ErbB tyrosine kinase inhibitor with potential antineoplastic activity. Pelitinib
irreversibly binds covalently to EGFR, ErbB-1, -2 and -4, thereby inhibiting receptor phosphorylation and signal
transduction and resulting in apoptosis and suppression of proliferation in tumor cells that overexpress these
receptors. Pelitinib inhibits EGF-induced phosphorylation of EGF-R and the growth of tumors that overexpress
EGF-R in animal models.
Toll Free:(877)796-6397 www.selleckchem.com info@selleckchem.com
Phone:+1-832-582-8158
---USA and Canada only---
\l"
S2192 AZD8931
AZD8931 is a novel potent reversible small molecule epidermal growth factor receptor, ErbB2 (HER2) and
ErbB3 inhibitor with an IC50 of 4, 3, 4 nM, respectively. It has a unique pharmacologic profile providing
equipotent inhibition of EGFR, ErbB2, and ErbB3 signaling and showing greater antitumor activity than agents
with a narrower spectrum of erbB receptor inhibition in specific preclinical models.
Size Price
S1194 CUDC-101
CUDC-101 has novel structure incorporating HDAC (IC50 4.4 nM) inhibitory functionality into the
pharmacophore of the EGFR C50 2.4 nM) and HER2 (IC50 15.7 nM) inhibitors. CUDC-101 exhibits efficient
antiproliferative activity with greater potency than vorinostat (SAHA), erlotinib, lapatinib. CUDC-101 inhibition
in various cancer xenograft models including NSCLC, liver, breast, head and neck, colon, and pancreatic
cancers.
Size Price
N
N
HN
O
O
H
N
O
HO
Data from our customer Dr Meng Xiangbing,
The University of Iowa.
Effect of CUDC101 on the viability was
detected by WST-1 method after 3 days
treatment in endometrial cancer cell
line Hec50 and Ishikawa and ovarian
cancer cell line SKOV3, Caov3 and PA1.

S1023 Erlotinib HCl
Erlotinib Hydrochloride inhibit activity against isolated tyrosine kinase(IC50, 2 nmol/L), to reduce HER1/EGFR
autophosphorylation in intact human tumor cells in vitro (IC50, 20 nmol/L), and to inhibit the EGF-dependent
proliferation of cells. It acts by inducing the expression of the cell-cycle inhibitor p27, and suppressing the
expression of the cell-cycle promoter cyclin D1, thereby blocking cell-cycle progression at the G1 phase.
Synonyms:

Tarceva, CP-358774, OSI-774, NSC 718781
Size Price
HN
N
N O
O
O
O
HCl
PC9 cell
Time(hr)
P-ERK
T-ERK
DUISP6
GAPDH
0
E D Er
3h 6h
E D Er
9h
E D Er
Time(hr) 0
D T U
3h 6h
D T U
9h
D T U
HCC827 cell
P-EGFRV
Y-1068
T-EGFR
P-ERK
T-ERK
ETS1
DUSP6
GAPDH
Breast cancer cells were starved for 16 hrs,
100ng/ml EGF for 15 min with the indicated
concentrations
Produced Independently by our customer
Dr.Zhang, Tianjin Medical University
Downregulation of DUSP6 is directly dependent on inhibition of P-ERK/ETS1
signaling and only indirectly on inhibition of EGFR activity as demonstrated
by DUSP6 expression in PC9 cells correlating closely with p-ERK activity.
Data form Carcinogenesis Advance Access Published online on Jan. 2010
using our inhibitor
DUSP6 is regulated by EGFR/ERK inhibition in NSCLC cell lines.
Protein expression levels were assayed by immunoblot for
phosphor-EGFR at indicated tyrosine sites, total-EGFR,
phosphor-ERK, total-ERK, ETS1, DUSP6 and GAPDH demonstrating
suppression of DUSP6 following inhibition of activated ERK (P-ERK)
and ETS1 levels in the presence of appropriate drug for each of the
following cell lines: HCC827 cells treated with erlotinib
S1143 AG-490
HO
HO
N
N
H
O
AG490 is a member of the tyrphostin family of tyrosine kinase inhibitors. The most-studied targets of AG490
are the Janus kinases (JAKs: JAK-2, JAK3/STAT, JAK3/AP-1, and JAK3/MAPK), a family of tyrosine kinases
that phosphorylate and thus activate the STAT transcription factors. AG490 inhibits the proliferation of several
cell types including leukemia cells and fibroblasts. AG490 is also selective inhibitor of EGFR tyrosine kinase
,&YDOXHVDUHDQG0IRU(*)5DQG(UE%UHVSHFWLYHO\
Synonyms: Tyrphostin AG490 Size Price
N
N
O
O
N
F
HN
N
H
O
Cl
S1194 CUDC-101
Feed
S1023 Erlotinib Hydrochloride
Feed
Synonyms:
ZM 252868, AG 1517, Tyrphostin AG 1517 S1079 PD153035 HCl
PD153035 effectively blocks the enhancement of mitogenesis, induction of early gene expression, and
oncogenic transformation that occur in response to EGFR stimulation. With human fibroblasts and epidermoid
carcinoma cells, PD153035 at nanomolar concentrations rapidly inhibits EGFR autophosphorylation. With
breast and ovarian cancer cells, PD153035 not only blocks cell growth via inhibition of EGFR, but also
upregulates the expression of the tumor suppressor retinoic acid receptor-beta 2.
N
N
HN
O
O
Br
HCl
Data from our customer Dr.Saraswati Sukumar,
Johns Hopkins University School of Medicine.
Inhibition of orthopoxvirus replication and spreading correlates with blocking of
(*)5VLJQDOLQJE\3'9DQGHWDQLEDQG*HWLQL:HVWHUQEORWRIFHOO
lysates obtained from VACVplaque reduction tests for analysis of EGFR-ERK1/2
signaling and VACV proteins. As an indicative band for VACV a 30KD a protein
was depicted from detection of total VACV proteins by apolyclonal antibody in
cell lysates of infected Hep2 cells.
PD153035 Vandetanib Gefitinib
Synonyms:

ZM 252868, AG 1517, Tyrphostin AG 1517, SU 5271, PD 153035
S2150 Neratinib
Neratinib is an orally available, irreversible tyrosine kinase inhibitor with IC50 of 59 nM and 92 nM for HER2
and EGFR, respectively. Neratinib binds to the HER-2 receptor irreversibly, thereby reducing
autophosphorylation in cells, apparently by targeting a cysteine residue in the ATP-binding pocket of the
receptor. Neratinib also inhibits the EGFR kinase and the proliferation of EGFR-dependent cells.
N O
HN
O
N HN Cl
O
N
N
Synonyms:

HKI-272
Size Price
Size Price
S1079 PD153035 Hydrochloride
Feed
Ard|oderes|s/Tvros|reK|rase
Solutions to Signal Transduction Research
4
EGFR
Acetyl-H3
H3
Breast Cancer Cell line MDA-MB-231
CUDC101(M) 0 0.01 0. 1 1.0 10.0 20.0
5mg
10mg
25mg
50mg
100mg
500mg
25mg
100mg
200mg
10mg
50mg
200mg
5mg
25mg
100mg
10mg
50mg
200mg
EGFR Ard|oderes|s/Tvros|reK|rase
5
N
N
N
H
N
N
Cl
O N
H
O
S1170 WZ3146
WZ3146 is 30- to 100-fold more potent against EGFR T790M, and up to 100-fold less potent against wildtype
EGFR, than quinazoline-based EGFR inhibitors (HKI-272 and CL-387,785) in vitro. WZ3146 has a 300-fold
lower half-maximum inhibitory concentration (IC50<10nM) against the PC9GR (delE746_A750/T790M,
gefitinib-resistant) cells compared with clinical-stage inhibitors such as HKI-272.
Size Price
S2406 Chrysophanic acid
Chrysophanic acid is an EGFR/mTOR pathway inhibitor. Chrysophanic acid preferentially blocked proliferation
in SNU-C5 cells but not in other cell lines with low levels of EGFR expression. Chrysophanic acid inhibited
EGF-induced phosphorylation of EGFR and suppressed activation of downstream signaling molecules, such
as AKT, ERKmTOR/p70S6K. Chrysophanic acid (80 and 120 M) significantly blocked cell proliferation when
combined with the mTOR inhibitor, rapamycin.
Size Price
Synonyms:

NSC 37132, NSC 646567
OH
O
O OH
\l"
N
N O
O
N
HN
F Br
S1046 Vandetanib
Vandetanib is a potent inhibitor of KDR tyrosine kinase activity (IC50= 40nM) and a submicromolar inhibitor of
EGFR tyrosine kinase (IC50= 500nM). The activity of Vandetanib versus KDR tyrosine kinase translates into
potent inhibition of VEGF-stimulated endothelial cell proliferation in vitro (IC50 =60 nM). Vandetanib blocks the
enzymatic activity of RET-derived oncoproteins at a one-half maximal inhibitory concentration of 100 nM.
Data from our customer Dr.Saraswati Sukumar,Johns Hopkins University School of Medicine.
Inhibition of orthopoxvirus replication and spreading correlates with blocking of
EGFR signaling by PD15303, Vandetanib and *HWLQL
Western blot of cell lysates obtained from VACV plaque reduction tests for analysis of
EGFR-ERK1/2 signaling and VACV proteins. As an indicative band for VACV
a 30KDa protein was depicted from detection of total VACV proteins by a polyclonal
antibody in cell lysates of infected Hep2 cells.
Synonyms:

Zactima, ZD6474
Size Price
S1056 BMS-599626
BMS-599626 inhibited HER1 and HER2 with IC50 of 20 and 30 nmol/L, respectively, and was highly selective
when tested against a broad panel of diverse protein kinases.BMS-599626 abrogated HER1and HER2
signaling and inhibited the proliferation of tumor cell lines that are dependent on these receptors, with IC50 in
WKHUDQJHRIWR0
Size Price
Synonyms:

AC480
N
H
O
O
H
N
O
N
N
N
HN
N
N
F
HCl
S1046 Vandetanib
Feed
breast cancer cells were starved for 16 hrs,
100ng/ml EGF for 15 min with
the indicated concentrations.
S1056 BMS-599626
Feed
Produced Independently by our customer Dr.Zhang,
Tianjin Medical University
50mg
200mg
500mg
5mg
25mg
100mg
10mg
50mg
200mg
N
N
N
H
O
N
N
Cl
O N
H
O
S1173 WZ4002
WZ4002 is 30- to 100-fold more potent against EGFR T790M, and up to 100-fold less potent against wildtype
EGFR, than quinazoline-based EGFR inhibitors (HKI-272 and CL-387,785) in vitro. WZ4002 treatment
resulted in significant tumour regressions compared with vehicle alone in both T790M-containing murine
models.
Size Price
10mg
50mg
100mg
N
N
N
H
N
N
Cl
s N
H
O
S1179 WZ8040
WZ8040 is 30- to 100-fold more potent against EGFR T790M, and up to 100-fold less potent against wildtype
EGFR, than quinazoline-based EGFR inhibitors (HKI-272 and CL-387,785) in vitro. WZ8040 has a 300-fold
lower half-maximum inhibitory concentration (IC50<10nM) against the PC9GR (delE746_A750/T790M,
gefitinib-resistant) cells compared with clinical-stage inhibitors such as HKI-272.
Size Price
10mg
50mg
200mg
10mg
25mg
100mg
Toll Free:(877)796-6397 www.selleckchem.com info@selleckchem.com
Phone:+1-832-582-8158
---USA and Canada only---
VEGFR / PDGFR
S2205 OSI-420
OSI 420 is an active metabolite of erlotinib which is an orally active EGFR tyrosin kinase inhibitor with IC50 of
2 and 20 nM for the inhibition of human EGFR and EGFR autophosphorylation in tumor cells. OSI-420
exposure (AUC) in plasma was 30%of erlotinib, and OSI-420 clearance was more than 5-fold higher than
erlotinib.
Synonyms:

Desmethyl Erlotinib,CP-473420
Size Price
S2216 Mubritinib
Roscovitine is a potent EGFR and p34cdc2 inhibitor with IC50 of 6 nM and 0.2 M, respectively. Roscovitine
displays > 4000-fold selectivity over EGFR, FGFR, PDGFR, JAK1 and Src. Roscovitine exhibits potent
antiproliferative effects in ErbB2-overexpressing cancer cell lines and significantly inhibits bladder, breast and
prostate cancer xenograft growth in vivo.
Size Price
Synonyms:

TAK 165,TAK165
F
F
F
O
N
O
N N
N
NH
N
N O
O
O
HO
HCl
\l"
\l"
S1207 AV-951
AV-951, a novel oral quinoline urea derivative, is an orally bioavailable inhibitor of VEGFRs 1, 2 and 3 with
potential antiangiogenic and antineoplastic activities. AV-951 blocks the proliferation and migration of
endothelial cells in vitro, and suppresses angiogenesis and growth of human tumor xenografts in vivo. The
compound is for the treatment of renal cell carcinoma and non-small cell lung carcinoma, and other
gastrointestinal cancer patients.
Synonyms:

Tivozanib
Synonyms:
ZM 252868, AG 1517, Tyrphostin AG 1517 S1490 AP24534
AP24534 (Ponatinib), a potent, orally available multitargeted kinase inhibitor, which is active against
pan-BCR-ABL native (IC50: 0.37nM) and mutated form (IC50: 0.3-2.0nM), VEGFR2 (IC50: 1.5nM), FGFR1
,& Q0 3'*)5 ,& Q0 DQG /<1 ,&Q0 $3 LQKLELWHG DOO WHVWHG %&5$%/
mutants with low nM IC50s in cellular assays, suppressed BCR-ABL driven tumor growth in mice, and
completely abrogated resistance in cell-based mutagenesis screens.
Synonyms:

Ponatinib
N
N
N
O
H
N
CF3
N
N
O
Cl
NH
O
NH
O
N
N
O
O
Size Price
Size Price

S1003 ABT-869
ABT-869 is a KDR inhibitor (IC50=4nM) but has much less activity (IC50s>1mM) against unrelated RTKs,
soluble tyrosine kinases, or serine/threonine kinases. The inhibition of ABT-869 inhibits RTK phosphorylation
(IC50=2, 4, and 7 nM for PDGFR-B, KDR, and CSF-1R, respectively) and VEGF-stimulated proliferation (IC50
= 0.2 nM for human endothelial cells) in cellular assays.
Synonyms:

Linifanib, AL-39324, RG3635
Size Price
N
HN
H
N
O
H
N
F
NH
2
Synonyms:
HKI-272 S1064 Masitinib
Masitinib is Phenylaminothiazole-type tyrosine kinase inhibitor that targets KIT. In Ba/F3 cells expressing
human wildtype KIT, masitinib dose-dependently inhibited SCF-induced cell proliferation with an IC50 of 150
nM.
Synonyms:

AB1010, Masivet
Size Price
ABT-869
Bcl-xl
Bcl2
DFWLQ
0
u
M
1
0
n
M
1
0
0
n
M
0
u
M
1
u
M
2
.5
u
M
0
u
M
+
R
1
0
n
M
+
R
1
u
M
+
R
2
.5
u
M
+
R
R:Radiation 16 Gy
Data produced independently by our customer Dr.Zhang,Tianjin Medical University
Western blot analysis of extracts Bcl-xl, Bcl-2; 0-2500 nM ABT-869
was added; Cell cutured with 16Gy radiation or not.
S1003 ABT-869
Feed
N
H
N
H
N
S
N
O
N
N
Ard|oderes|s/Tvros|reK|rase
Solutions to Signal Transduction Research
6
EGFR / VEGFR / PDGFR
10mg
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10mg
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100mg
25mg
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S1084 Brivanib
Brivanib is hydrolyzed to the active moiety BMS-540215 in vivo. BMS-540215 is an ATP-competitive inhibitor
of human VEGFR -2, with an IC50 of 25 nmol/L and Ki of 26 nmol/L. In addition, it inhibits VEGFR-1 (IC50 =
380 nmol/L) and VEGFR-3 (IC50 = 10 nmol/L). BMS-540215 also showed good selectivity for FGFR-1 (IC50
= 148 nmol/L), FGFR-2 (IC50 =125 nmol/L), and FGFR-3 (IC50 = 68 nmol/L).
Synonyms:

BMS-540215
Size Price
H
N
F
O
N
N
N
O OH
10mg
50mg
100mg
10mg
25mg
50mg

VEGFR/PDGFR Ard|oderes|s/Tvros|reK|rase
/
E7080 is the most potent dual inhibitor of VEGF-R3 tyrosine kinase (IC50=5.2 nM) as well as VEGF-R2
tyrosine kinase (IC50=4.0 nM) among those small-molecule inhibitors of VEGF-R kinases, such as sunitinib,
sorafenib, and CEP-7055. IE7080 suppresses lymph node and lung metastases of human mammary breast
tumor MDA-MB-231 via inhibition of angiogenesis and lymphangiogenesis in vitro. It has been used in phase
I clinical trial against hepatocellular carcinoma and non-small cell lung carcinoma.
Imatinib Mesylate is a reversible tyrosine kinase inhibitor effective in treatment of CML, gastrointestinal stromal
tumors, eosinophilic disorders, and systemic mast cell disease. The drug binds preferentially to ATPbinding
VLWHVRIWKHF.LWSURWRRQFRJHQHSURGXFW3'*)5DQGF$%/7KH,&YDOXHVIRU'&VDQG3+$ZHUH
0DQG0UHVSHFWLYHO\$W0WKHDPRXQWRIDFWLYDWHG1.N%ZDVUHGXFHGWRDQGGHFUHDVHG
WRDW0
Synonyms:

Gleevec, Glivec, CGP-57148B, STI-571
N
O
NH2 O
O
Cl
N
H
O
HN
H
N
N
N
N
H
N
O
N
N
HO S
O
O
Data from our customer Dr Thomas Krwel, Fraunhofer-Institute
for Toxicology and Experimental Medicine
S1164 E7080
S1026 Imatinib Mesylate Size Price
Size Price
Cell Viability assay results. A2C12, BetaD5, GammaA3,
GammaD12, A549, CaCo2, HepG2 cell lines were treated
with imatinib for 96h and 24h.
S1026 Imatinib Mesylate
Feed

S1017 Cediranib
AZD2171 is a highly potent inhibitor of recombinant KDR tyrosine kinase activity in vitro (IC50 < 1 nmol/L).
Additional activity is observed against the kinase associated with Flt-1 (IC50= 5 nmol/L) and the VEGF-C and
VEGF-D receptor Flt-4 (IC50 <3nmol/L). The inhibitory activity of AZD2171 was also examined against each
recombinant PDGFR-related kinase in vitro because of their structural similarity to the VEGF family of
receptors.
Synonyms:

AZD2171, Recentin
Size Price
N
N
O
H
N
F O
O N
Synonyms:
HKI-272
Synonyms:
ZM 252868, AG 1517, Tyrphostin AG 1517 S1171 CYC116
CYC116 is an orally bioavailable,small molecule Aurora kinase/VEGFR2 inhibitor with antineoplastic activity.
CYC116 inhibits Aurora kinases A and B and VEGFR2, resulting in disruption of the cell cycle, rapid cell death,
and the inhibition of angiogenesis. CYC116 has a unique target profile involving both cell cycle and
angiogenesis inhibition mechanisms. In preclinical studies, it has antitumor activity in both solid tumors and
hematological cancers.
S2202 NVP-BHG712
NVP-BHG712 is a small molecule specific EphB4, VEGFR2, c-raf, c-src and c-Abl kinase inhibitor with ED50
RI Q0 DQG 0 UHVSHFWLYHO\ 193%+* LQKLELWV PXOWLSOH (SK UHFHSWRU NLQDVHV
NVP-BHG712 inhibits VEGF driven angiogenesis. In cell based assays ED50 for inhibition of EphB4
autophosphorylation was found to be 25 nM and thereby be roughly 200 fold more potent on EphB4 than on
VEGFR2. NVP-BHG712 inhibited dose dependently VEGF stimulated tissue formation and vascularization in
this model.
Synonyms:

CP673451
Produced independently by our customer Dr.Zhang,Tianjin Medical University.
Histone H3
p-Histone H3
Aurora A
p-Aurora
A/B/C
0

M
1
0

M
0
.0
0
1

M
0
.0
1

M
0
.1

M
1

M
CYC116
N
O
O
N
N
N
NH2
N
N
H
N
N
O
S
N
NH
2
Size Price
Size Price
Western blot analysis of Histone-H3, p-Histone-H3, Aurora A,
S$XURUD$%&0&<&ZDVDGGHG
S1171 CYC116
Feed
Data from British Journal of Cancer (2010) using our product.
S1018 CHIR-258
CHIR-258 potently inhibits FGFR3 with an IC50 of 5 nM in vitro kinase assays and selectively inhibited the
growth of B9 cells and human myeloma cell lines expressing wild-type (WT) or activated mutant FGFR3.
Synonyms:

TKI-258, Dovitinib
Size Price
HN
O
NH
2
N
H
N
N N
F
S1018 CHIR-258
Feed
The effect of PD173074 on FGFR3 phosphorylation and proliferation of
FGFR3-expressing bladder tumour cell lines. RT112 cells were exposed to PD173074 (PD)
(500 nM) for 024 h, TKI-258 (TK) (500 nM) or SU5402 (SU) (5 mM) for 1 h. Cells were
lysed, FGFR3 was immunoprecipitated (immunoprecipitated, IP) and blots (immunoblot, IB)
were probed for phospho-tyrosine and reprobed for FGFR3 or (C) probed for phospho-ERK
and reprobed for total ERK.t
pERK
Total ERK
Con TK PD SU
2h 6h
IP:FGFR3
IB:Phos-tyr
IB:FGFR3
PD173074 0h 24h TK SU
10mg
25mg
50mg
10mg
50mg
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10mg
50mg
200mg
10mg
50mg
200mg
10mg
50mg
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10mg
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500mg
Toll Free:(877)796-6397 www.selleckchem.com info@selleckchem.com
Phone:+1-832-582-8158
---USA and Canada only---

S2161 RAF265
5DILVKLJKO\VHOHFWLYH5DIDQG9(*)5NLQDVHLQKLELWRUZLWK,&RIRIWR05DILVDNH\FRPSRQHQW
of the Ras/Raf/MEK/ERK signal-transduction pathway, which controls cell proliferation, differentiation, and
apoptosis in mammalian cells. Raf265 also has anti-angiogenic activity through inhibition of VEGFR.
Synonyms: CHIR-265
Size Price
S1032 Motesanib Diphosphate
AMG-706 (Motesanib) selectively targets and inhibits VEGFR1/2/3 (IC50: 2 nM /3 nM /6 nM), PDGFR (84nM),
c-kit (8nM), and Ret (59nM) receptors, thereby inhibiting angiogenesis and cellular proliferation. This
compound also performed antitumor activity in breast cancer xenografts and was currently being studied in
clinical trials for the treatment of thyroid cancer and other advanced solid tumors.
Synonyms: AMG-706 Size Price
N
NH
N
O
H
N
H
N
2H3PO4
Synonyms:
HKI-272 S1244 MP-470
MP470 is a multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Met, c-Kit, PDGFR-
DOSKD )OW ZLWK DQ ,& RI PHGLDQ 0 03 ZDV VKRZQ WR LQKLELW GV'1$ EUHDN UHSDLU DQG LQFUHDVH
apoptosis. The cytotoxicity of MP470 was evaluated on prostate cancer cell lines (LNCaP, PC-3 and DU-145).
7KHGUXJZDVHIIHFWLYHRQ/1&D3DQG3&FHOOVZLWKDQ,&RI0DQG0UHVSHFWLYHO\
O
N
N
N
N
S
NH
O
O
Synonyms:
ZM 252868, AG 1517, Tyrphostin AG 1517 S1220 OSI-930
OSI-930 is a multi-targeted tyrosine kinase inhibitor that is designed to act as a potent co-inhibitor of the
receptor tyrosine kinases c-Kit (IC50: 9.5 nM) and VEGFR-2 (IC50: 10.1 nM). OSI-930 targets both cancer cell
proliferation and angiogenesis in selected tumors. In preclinical studies, OSI-930 shows broad efficacy in
tumor models representative of small cell lung cancer, glioblastoma, colorectal, renal, head and neck,
non-small cell lung cancer and gastric cancers.
N
NH
S H
N
O
O
F
F
F
S1035 Pazopanib HCl
Pazopanib showed good potency against all the human VEGFR receptors with an IC50 of 10, 30, and 47 nM
for VEGFR-1, -2, and -3, respectively. Significant activity was also seen against the closely related tyrosine
receptor kinases PDGFR beta, c-Kit, FGF-R1, and c-fms with IC50 of 84, 74, 140,and 146 nM, respectively.
7KHF\WRFKURPH3SURILOHZDVDOVRLPSURYHGZLWKLQKLELWLRQ!0DJDLQVWWKHLVR]\PHVWHVWHGZLWKWKH
H[FHSWLRQRI&0
Synonyms: GW786034, VOTRIENT
S
O H
2
N
O
H
N
N
N N
N
N
HCl
Size Price
S1178 BAY 73-4506
BAY 73-4506 is an orally bioavailable multikinase inhibitor targeting both the tumor and its vasculature. BAY
73-4506 binds to and inhibits VEGFR-2 and -3, and tumor cell signaling kinases (RET, c-Kit, PDGFR, and
b-Raf), which may result in the inhibition of tumor angiogenesis and tumor cell proliferation. This drug shows
potent, oral activity in a wide variety of preclinical xenograft models.
Synonyms: Regorafenib Size Price
Size Price
Size Price
N
N
O
N
HN
F
F
F
N
H
N F
F
F
O
HN
N O
HN
F
HN
O
Cl
F
F
F
Ki8751 is a VEGFR-2 inhibitor. It inhibited VEGFR-2 phosphorylation at an IC50 value of 0.90 nM, and also
LQKLELWHGWKH3'*)5IDPLO\PHPEHUVVXFKDV3'*)5DQGF.LWDWQ0DQGQ0UHVSHFWLYHO\,WGLGQRW
have any inhibitory activity against other kinases such as EGFR, HGFR, InsulinR and others even at 10000
nM. Ki8751 suppressed the growth of the VEGF-stimulated human umbilical vein endothelial cell (HUVEC) on
a nanomolar level.
N O
O
O
F
H
N
H
N
O
F
F
KRN 633 is a cell-permeable, reversible, ATP-competitive VEGFR kinase inhibitor with IC50 of 170 nM, 160
Q0 DQG Q0 IRU 9(*)5 9(*)5 9(*)5 UHVSHFWLYHO\ ,W LQKLELWV 3'*)5 DQG F.LW DW KLJKHU
concentrations only (IC50 = 0.97 M and 4.33 M, respectively). Although not cytotoxic to cancer cells,
KRN633 exhibits excellent in vivo antitumor activity due to its inhibitory effects on vessel formation and
vascular permeability. N
N
O
O
O
Cl
H
N
O
H
N
S1363 Ki8751
S1557 KRN 633
S1361 MGCD-265
MGCD265 is a tyrosine kinase inhibitor that targets the c-Met, VEGFR-1, VEGFR-2, VEGFR-3, RON and TIE2
receptor tyrosine kinases, which appear to play key roles in tumour development and blood vessel formation
(angiogenesis) and tumour survival. MGCD265 is currently in phase I single-agent clinical trials for solid
tumour cancers and in phase II trials for solid tumours and NSCLC.
Size Price
Size Price
Size Price
H
N
O
H
N
S
F
O
N
S
N
N
Ard|oderes|s/Tvros|reK|rase
Solutions to Signal Transduction Research
8
VEGFR/PDGFR
5mg
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VEGFR/PDGFR
Ard|oderes|s/Tvros|reK|rase
9

S1264 PD173074
PD173074 is a potent, cell-permeable and ATP-competitive inhibitor of FGFR1 (IC50 = 21.5 nM). PD173074
inhibits PDGFR and c-Src only at much higher concentration (IC50 = 17,600 nM, 19,800 nM, respectively) and
exhibits little effect against EGFR, InsR, MEK, and cPKC even at concentrations as high as 50,000 nM.
N
N N NH
NH O
O
O
N
H
N
S2201 BMS 794833
BMS-794833, a potent ATP competitive Met/VEGFR-2 kinase inhibitor, demonstrates enhanced activity
versus both Met-dependent and Met-insensitive tumor lines. BMS-794833 also inhibits Ron, Axl and Flt-3 with
IC50 values <3 nM. The compound was selective versus a panel of >200 additional RTKs, non-RTKs and
serine/threonine kinases based on biochemical or Ambit binding assays. In cell culture, BMS-794833 inhibited
the proliferation of human tumor cell lines containing constitutively activated Met receptor.
Size Price Synonyms: BMS794833
S1040 Sorafenib Tosylate
Sorafenib Tosylate is a novel, small molecular inhibitor of several tyrosine protein kinases (VEGFR and
PDGFR) and Raf/MEK/ERK cascade inhibitor with an IC50 of 6, 22, 38 nM for Raf-1, wt b-raf and V599E
mutant b-raf. It does not significantly inhibit MEK-1 or ERK-1 activity (IC50 >10 M). It interacts synergistically
with bortezomib to induce apoptosis in a broad spectrum of neoplastic cell lines and show an important role for
the Akt and JNK pathways in mediating synergism.
Synonyms: Nexavar, Bay 43-9006 Size Price
Cl
CF3
N
H
N
H
O
O
N
N
H
O
S
HO
O
O
S1138 Brivanib alaninate
Brivanib is hydrolyzed to the active moiety BMS-540215 in vivo. BMS-540215 shows potent and selective
inhibition of VEGFR and FGFR tyrosine kinases. BMS-540215 is an ATP-competitive inhibitor of human
VEGFR-2, with an IC50 of 25 nM and Ki of 26 nmol/L. In addition, it inhibits VEGFR-1 (IC50 =380nM) and
VEGFR-3 (IC50 = 10 nM). BMS-582664 was prepared in an effort to improve the aqueous solubility and oral
bioavailability of the parent compound BMS-540215.
Synonyms: BMS-582664 Size Price

S1042 Sunitinib Malate
Evaluating the ability of SU11248 to inhibit ligand-dependent receptor phosphorylation in cells, the effect of
SU11248 on ligand-dependent proliferation of cells was examined. SU11248 inhibited VEGF- and
FGF-induced proliferation of HUVECs with IC50 values of 0.04 and 0.7 M, respectively. SU11248 also
inhibited PDGF-induced proliferation of NIH-3T3 cells overexpressing PDGFRa or PDGFRb with IC50 values
of 0.03 and 0.07 M, respectively.
Synonyms: Sutent, SU-11248 Size Price
Size Price
F
N
H
O
N
H
NH
O
N
HO
O
OH
O
OH
Data published in February 25,2010;Dol 10.1182/blood-2009-10-250118,provided by
our customers Varsha Kumar, Theodor Kocher Institute,University of Bern,Switzerland

Experimental layout for VEGF signaling blocking and LCMV infection in WT mice.
Mice received two injections on day 0 and 3 p.i. of Abs as described in Material
and Methods, or daily gavage of the VEGFR/PDGFR-inhibitor sunitinib.
N
H2N
Cl
O
F
H
N
O
NH
O
F
\l"
S1042 Sunitinib Malate
Feed
F
H
N
O
N
N
N
O
(R) (R)
O
(S) (S)
O
NH2

S2475 Imatinib
Imatinib is a number of tyrosine kinase enzymes specific inhibitor. It act by specifically inhibiting a certain
enzyme that is characteristic of a particular cancer cell, rather than non-specifically inhibiting and killing all
rapidly dividing cells, and served as a model for other targeted therapy modalities through tyrosine kinase
inhibition. As this is now a constitutively active tyrosine kinase, it is used to decrease bcr-abl activity. It is being
used as an experimental agent to suppress PDGF.
Synonyms: STI571, Gleevec, Glivec Size Price
S1119 XL184
XL-184 is an orally bioavailable, small molecule RTK inhibitor. Specifically, XL184 appears to have a strong
affinity for the Met and VEGFR2, which may result in inhibition of tumor growth and angiogenesis, and tumor
regression. This agent has also been shown to inhibit mast/stem cell growth factor (c-Kit), Flt3 and Tie-2.
F
H
N
O
HN
O
O
N
NH
N
O
N
H
O
S1111 Foretinib
GSK1363089 (XL880) is an orally bioavailable,small molecule Met/VEGFR2 inhibitor with potential
antineoplastic activity. This compound binds to and selectively inhibits HGF receptor c-Met (IC50 of 0.4 nM)
and VEGFR2, which may result in the inhibition of tumor angiogenesis, tumor cell proliferation and metastasis.
Synonyms: XL880, GSK1363089, GSK089, EXEL-2880
F
H
N
O
H
N
O
F
O
N
O
O N
O
Size Price
Size Price
N
H
N
N
N
N
H
N
O
N
\l"
5mg
10mg
50mg
10mg
50mg
200mg
10mg
50mg
200mg
10mg
50mg
200mg
10mg
50mg
200mg
10mg
25mg
50mg
10mg
50mg
200mg
10mg
50mg
Toll Free:(877)796-6397 www.selleckchem.com info@selleckchem.com
Phone:+1-832-582-8158
---USA and Canada only---
Synonyms:
HKI-272 S1470 TSU-68
TSU-68, a molecular-targeting drug, has the effect on blocking the tyrosine kinase phosphorylation of the
receptors not only for VEGF but also for PDGF and bFGF, and inhibiting angiogenesis. Studies using in vivo
experimental models of cancers such as colon cancer have reported that TSU-68 has the effect on inhibiting
tumor proliferation and metastasis through the inhibition of tumor angiogenesis. In vitro TSU-68 does not
influence the proliferation of ovarian cancer cells.
Synonyms: SU6668
N
H
O
N
H
OH
O
Size Price
Synonyms:
ZM 252868, AG 1517, Tyrphostin AG 1517 S1101 Vatalanib
)RUGLIIHUHQWUHFHSWRUNLQDVHV37.ELRFKHPLFDO,&DUH0WR.'50WR)OWX0WR
Flk,0.66 uM to Flt-4,0.73 uM to c-Kit. Selective inhibition of VEGFRs by PTK787/ZK 222584 leads to inhibition
of primary tumor growth and development of metastases in murine renal cell carcinoma. PTK787/ZK 222584
caused no obvious side effects in the RENCA model. PTK787/ZK222584, causes significant anti-arthritic
effects in models of rheumatoid arthritis.
Synonyms: Vatalanib succinate, PTK/ZK, CGP-79787D Size Price
N
N O
O
N
HN
F Br
.
2HCl
S1010 BIBF1120
The targeted kinases of BIBF1120 include all three VEGFR subtypes (IC50 = 1334 nmol/L), PDGFRa and
PDGFRh (IC50 = 59 and 65 nmol/L), and FGFR types 1, 2, and 3 (IC50 = 69, 37, and 108 nmol/L,
respectively). BIBF 1120 inhibits MAPK and Akt signaling pathways in three cell types contributing to
angiogenesis, endothelial cells, pericytes, and smooth muscle cells, resulting in inhibition of cell proliferation
(EC50=1080 nmol/L) and apoptosis.
Synonyms: Vargatef Size Price
N
H
NH
N
O
N
N
O
O
O
S1010 BIBF1120
Feed
PBLs from CLL5 were treated with vehicles (0.1% ethanol and 0.005%
DMSO), 10 nM dexamethasone, 50 nM BIBF 1120, or both for 24 h. Cells
were also treated with 0.1% ethanol or 10 nM dexamethasone in the
presence of either nonphosphorylated (control) EGQYEEIP or hosphorylated
EGQY*EEIP H
2
O soluble peptides (200 nM) for 24 h. Cell death was
measured in triplicate by trypan blue dye exclusion.
Data published in Cell Death and Differentiation, 2010, 1-11 using our product.
Synonyms:
ZM 252868, AG 1517, Tyrphostin AG 1517 S1005 Axitinib
In transfected or endogenous RTK-expressing cells, axitinib potently blocked growth factor-stimulated
phosphorylation of VEGFR-2 and VEGFR-3 with average IC50 values of 0.2 and 0.1 to 0.3 nmol/L,
respectively. Cellular activity against VEGFR-1 was 1.2 nmol/L, equivalent to an absolute IC50 of -0.1 nmol/L,
based on protein binding of axitinib. The potency against Flk-1 in Flk-1-transfected NIH-3T3 cells was 0.18
nmol/L, similar to that of its human homologue.
Synonyms: AG-013736 Size Price
S1486 AEE788 Page 3
Synonyms:
ZM 252868, AG 1517, Tyrphostin AG 1517 S1046 Vandetanib Page 5
Synonyms: NVP-AEE 788
Synonyms: Zactima, ZD6474
O
HN
S
N
H
N
N
VEGFR-2
Phospho-VEGFR-2
Axitinib (nmol/L) 0 0 0.1 1 10
VEGF (50 ng/ml) - + + + +
HUVECs were starved O/N in EBM-2 basal medium with 1% FBS and
antibiotic. Cells were pre-treated with Axitinib at 0.1, 1 and 10 nM
concentrations. VEGF stimulation was 50ng/ml for 10 minutes before
cells were collected and protein isolated for immunoprecipitation with
VEGFR2 followed by immunoblotting with VEGFR-2 and phospho-VEGFR-2.
Data from our customer Dr Cheri Pasch, UW.
S1005 Axitinib
Feed
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l0
VEGFR/PDGFR
10mg
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100mg
200mg
300mg
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100mg
200mg
5mg
10mg
50mg

ll
FGFR (Fibroblast growth factor receptor)
Src-Bcr-Abl
FGFR / Src-Bcr-Abl
Ard|oderes|s/Tvros|reK|rase
ll
Synonyms:
HKI-272 S1107 PHA-739358
CHIR-258(Dovitinib) is a highly potent, novel multitargeted growth factor receptor kinase inhibitor with IC50 of
1, 2, 10, 8, 27, 36 nM for FLT3, c-KIT, VEGFR1/2/3, PDGFR and CSF-1R, respectively. It potently inhibits
FGFR3 with an C50 of 5 nM in in vitro kinase assays and selectively inhibited the growth of B9 cells and human
myeloma cell lines expressing wild-type or activated mutant FGFR3. Antiproliferative activity of CHIR-258
against MV4;11 was ~24-fold greater compared with RS4;11.
Synonyms: Danusertib Size Price
O
N
O
H
N
N
HN
O
N
N
1
0
1 0
.1
0
.0
1
0
.0
0
1
C
o
n
tr
o
l
P-Aurora A/B/C
Aurora B
Aurora A
Histone H3
P-Histone H3
0
S1107 PHA-739358
Feed
Produced independently by our customer Dr.Zhang,Tianjin Medical University.
Western blot analysis of Histone-H3, p-Histone-H3, Aurora A, Aurora B,
S$XURUD$%&03+$ZDVDGGHG
Synonyms:
HKI-272 S1018 CHIR-258 Synonyms: TKI-258, Dovitinib, CHIR258, TKI258 Page 7
Synonyms:
ZM 252868, AG 1517, Tyrphostin AG 1517 S1490 AP24534 Page 6 Synonyms: Ponatinib
Synonyms:
ZM 252868, AG 1517, Tyrphostin AG 1517 S1010 BIBF1120 Page 10 Synonyms: Vargatef
Synonyms:
ZM 252868, AG 1517, Tyrphostin AG 1517 S1264 PD173074 Page 9
S1134 AT9283
$7DPXOWLWDUJHWHGNLQDVHLQKLELWRUZLWKSRWHQWDFWLYLW\DJDLQVW$XURUD$DQG%NLQDVHV,&Q0,Q
addition to Aurora A and Aurora B, AT9283 was also found to inhibit a number of other kinases including JAK2,
)OW DQG $EO 7, ,& Q0 7KLV FRPSRXQG GHPRQVWUDWHG LQ YLYR HIFDF\ LQ PRXVH [HQRJUDIW
models and is currently under evaluation in phase I clinical trial.
Size Price
H
N
O
HN
NH
N
N
H
N
O
N

P-STAT5
STAT5
4
4
0
0
4
9
0
1
6
0
5
0
2
0
2

S1369 Bafetinib
Bafetinib (INNO-406) is an orally available, dual Abl/Lyn kinase inhibitor that is up to 55-times more potent than
imatinib in Bcr-Abl cell lines. Numerous Bcr-Abl mutant proteins (not T315I) are sensitive to INNO-406 in vitro.
INNO-406 demonstrates specific Src kinase activity against Lyn kinase.
Synonyms:

INNO-406, NS-187
Size Price
N
N
N
N
H
N
HN
O
F F
F
N
N
Data provided by our customers Dr.Claude Haan and Catherine
Rolvering,Universite du Luxembourg
HEL cells were treated for 3 hours with the indicated concentrations
of AT 9283. AT 9283 inhibits Jak2-V617F mediated signal transduction
at submicromolar concentrations in intact cells. At concentrations of
490 nM the Jak2-V617F inhibition is almost complete and has reached
almost omplete and has reached almost background levels (for
background STAT5 phosphorylation see 4400 nM)
S1134 AT9283
Feed
S1006 AZD0530
AZD0530 is highly selective for Src and Abl kinases against a large range of tyrosine and serine-threonine
kinases (VEGFR2, FGFR, c-Kit, Aur-3 etc. >5 M). AZD0530 exerts its activity through ATP competitive and
reversible inhibition of the target enzyme. Submicromolar growth inhibition of five of the human cancer cell
lines tested with AZD0530(tumor types: colon, prostate, lung, and leukemia) was observed with IC50 values
of 0.20.7 M.
Synonyms:

Saracatinib
Size Price
N
N
O
O
N
N
O
HN
Cl
O
O
Data provided by our customer Shuxin Han, Kent State University
S1006 AZD0530
Feed
IP assay of tyrosine phosphorylation of VDR in the plasma membrane. Primary human
KHSDWRF\WHVZHUHWUHDWHGZLWK9HK2+9'Q0/&$DFHWDWH0
DQGRUWKHF6UFLQKLELWRU$='$='0IRUK$UDEELWDQWL9'5DQWLERG\
ZDVXVHGWRLPPXQRSUHFLSLWDWH9'5IURPFHOOPHPEUDQHH[WUDFWVJ$PRXVH
anti-phospho-tyrosine was used to detect phosphotyrosines in VDR. A mouse anti-VDR
was used to detect immunoprecipitated VDR. Ten % cell extract was set aside as input.
5mg
10mg
50mg
10mg
50mg
100mg
5mg
25mg
200mg
1mg
5mg
10mg
Toll Free:(877)796-6397 www.selleckchem.com info@selleckchem.com
Phone:+1-832-582-8158
---USA and Canada only---
S5002 FTY720
FTY720 is a potent sphingosine-1-phosphate (S1P) receptors agonist with IC50 of 0.137, 10.98 nM for (S)-
and (R)- FTY720-phosphate, respectively and reverses the effects of BCR-ABL kinase. It does not directly
target the bcr-Abl kinase, but instead activates phosphatase 2A (PP2A) which is a tumor suppressor that is
inactivated by Bcr-Abl. FTY720 also mediated antitumor effects in hepatocellular carcinoma (HCC) cells by
activating PKC .
Synonyms:

Fingolimod, Gilenia
Size Price
HO
NH
2
HO
.HCl
S1033 Nilotinib
Nilotinib inhibited the proliferation of Ba/F3 cells expressing p210- and p190-bcr-Abl, or K562 and Ku-812F
cells with IC50 values <12 nM. Nilotinib was quantitatively via capture ELISA for its effect on cellular bcr-Abl
autophosphorylation activity and on Bcr-Abl-dependent cell proliferation IC50 =2060 nM. Compared with the
antiproliferative activity of imatinib , AMN107 was 43times more potent in KBM5 (IC50 of 11.3 versus 480.5
nM) and 60 times more potent in KBM7(IC50 of 4.3versus 259.0 nM) cells.
Synonyms:

Tasigna, AMN-107
Size Price
H
N
N
N N
O
N
H
CF
3
N
N
Synonyms:
HKI-272 S1014 Bosutinib
SKI-606 inhibited migration of breast cancer cell lines with IC50 values of 0.1 to 0.3 umol/L; After a 48 h
treatment with 1 umol/L SKI-606, all the invasioncompetent cell lines were unable to cross the porous
membrane; cell proliferation and survival were unaffected by SKI-606 at concentrations sufficient to block cell
migration and invasion.
Synonyms:

SKI-606
Size Price
A and B. Sperm were incubated in apacitating medium supplemented
with SFK inhibitors and different concentrations of okadaic acid (OA)
(panel A) or calyculin-A (panel B), before immunodetection of p-PKA
substrates (clone 100G7E). C and D, PVDF membranes used in A and
B were stripped as described and used for western blot immunodetection
with anti-PY antibodies (clone 4G10).
Data published in J Biol Chem. 2010 Jan 12, provided by our customer Prof. Pablo E.
Visconti, Department of Veterinary and Animal Science, University of Massachusetts
N CN
O
O N
N
HN
Cl
Cl
O
S1014 Bosutinib
Feed
Synonyms:
ZM 252868, AG 1517, Tyrphostin AG 1517 S1021 Dasatinib
An ATP-competitive, dual Src/Abl inhibitor.Dasatinib is a potent inhibitor of imatinib-resistant Kit activation loop
mutants and induces apoptosis in mast cell and leukemic cell lines expressing these mutations. Dasatinib
sensitively inhibits all members of the Src family, including c-Src, Lck, Fyn, and Yes (IC50 < 1.1nmol/L). At
higher concentrations (3 to 28 nmol/L), dasatinib also inhibits the Src kinases Abl, c-Kit, PDGFR, and EphA2.
Synonyms:

BMS-354825, Sprycel, BMS354825
Size Price
N
N N
N
OH
NH
N
S
NH
O
Cl
Data from Investigational New Drugs
October 2010 using our product.
Cytotoxicity by Dasatinib treatment in leukemic cells.
/HXNHPLFFHOOOLQHVZHUHH[SRVHGWR'DVDWLQLE0
Upon treatment, cell viability (a) was calculated as percentage
with respect to the control vehicle cultures (set to 100% for
each cell line) and induction of apoptosis (b) was calculated
as percentage of Annexin V+/PI+ cells after 48 h of treatment.
S1021 Dasatinib
Feed

Synonyms:
ZM 252868, AG 1517, Tyrphostin AG 1517 S1264 PD173074 Page 9
Synonyms:
ZM 252868, AG 1517, Tyrphostin AG 1517 S1107 PHA-739358 Page 11
S2202 NVP-BHG712 Page 7
Synonyms:

Danusertib

S1490 AP24534 Page 6
Synonyms:

Ponatinib
EHEB JVM-2 JVM-3 MEC-1 MEC-2 BJAB
Untreated
Dasatinib
30
25
20
15
10
5
0
A
p
o
p
t
o
s
i
s
(
%
)
b
EHE JVM-2 JVM-3 MEC-1 MEC-2 BJAB
120
100
80
60
40
20
0
Dasatinib(24h)
Dasatinib(48h)
C
e
l
l
v
i
a
b
i
l
i
t
y
(
%

o
f

u
n
t
r
e
a
t
e
d
c
u
l
t
u
r
e
s
)
Untreated
a
Ard|oderes|s/Tvros|reK|rase
Solutions to Signal Transduction Research
l2
Src-Bcr-Abl
10mg
50mg
200mg
25mg
50mg
100mg
100mg
200mg
500mg
200mg
1g
2g
50mg
S2391 Quercetine
4XHUFHWLQLVD3,.DQG3.&LQKLELWRUZLWK,&RI0DQGJPO,WVWURQJO\DEURJDWHG3,.DQG6UF
kinases, mildly inhibited Akt1/2, and slightly affected PKC, p38 and Erk1/2. Quercetin is a naturally-occurring
polar auxin transport inhibitor with IC50 of 0.8, 16.7, 6.1, 11.36 M for the inhibition of LDH% release, the
inhibition of TNF-induced PMN-EC adhesion, TNF-induced inhibition of DNA synthesis and proliferation.
Synonyms:

Sophoretin, Meletin, Quercetine
Size Price
\l"
10mg
5mg
O HO
OH O
OH
OH
OH

HER-2 (Human Epidermal growth factor Receptor 2)
IGF-IR / HER-2
Ard|oderes|s/Tvros|reK|rase
l3
IGF-IR (Insulin-like growth factor 1 receptor)
Synonyms:
HKI-272 S1088 NVP-ADW742
NVP-ADW742 is an ATP-competitive inhibitor that inhibits IGF-IR autophosphorylation with a cellular IC50 of
WR PRO/ ZKLFK LV IROG ORZHU WKDQ WKDW RI WKH LQVXOLQ UHFHSWRU 193$': DOVR HQKDQFHV WKH
sensitivity of SCLC to etoposide and carboplatin, which are commonly used in the treatment of SCLC.
Synonyms:

ADW742
Size Price
N
N
N
NH2
O
N

S1093 GSK1904529A
GSK1904529A, which potently inhibits IGF-IR (IC50= 27 nmol/L) and IR (IC50= 25nmol/L) activities in vitro
and in vivo, is a promising candidate for therapeutic use in solid and hematologic cancers. The tumor histologic
types showing the greatest sensitivity to this compound were Ewings sarcoma and multiple myeloma, where
IC50s in three of five Ewings sarcoma cell lines were <100 nmol/L and IC50s in five of eight multiple myeloma
cell lines were <200 nmol/L.
Size Price
F F
HN O
O
N
N
N
N
HN
O
N
N
N
S
O
O
Inhibition of IGF-1 induced IGF-1R phosphorylation
by GSK1904529A. A549 cells were serum-starved O/N
DQGSUHLQFXEDWHGIRUKZLWK0*6.$
followed by stimulation with 50ng/ml IGF-1.
+ IGF-1: positive control; -S: negative control.
Data provided by our customers Ursula Broder,
ETH Zrich - Institute of Biochemistry, Switzerland
Data provided by our customers Ursula Broder,
Xuejun Jiang, Memorial Sloan-kettering Cancer Center
Immortalized wild-type mouse embryonic fibroblasts
were serumstarved for 4 hours,then stimulate with
100ng/ml IGF-1 for 5 min.Inhibitor was added for the
last 1 hour of serum starvation.
S1093 GSK1904529A
Feed
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200mg
S1486 AEE788 Page 3
S1011 BIBW2992 Page 3
Synonyms:

NVP-AEE 788
Synonyms:

Tovok
S1028 Lapatinib Ditosylate Page 3
Synonyms:

Tykerb, Tyverb, GW-572016
S1167 CP-724,714
CP-724,714 is an orally available, small molecule, potent HER-2 tyrosine kinase inhibitor under development
for the treatment of advanced HER2-overexpressing cancers. It inhibits HER2-chimera phosphorylation with
an IC50 of 15 ng/ml (32 nM), and is >500-fold selective for HER2 relative to other kinases (e.g. EGFR,
PDGFR, IGF-1R, VEGFR-2, abl, src). Additionally, CP-724,714 showed a favorable nonclinical toxicity profile
with no apparent effects on cardiac tissue.
Size Price
N
N
HN
N
H
O
O
O
N
S1019 CI-1033
CI-1033 is an orally bioavailable irreversible Pan-ErbB tyrosine kinase inhibitor, targeting EGFR with IC50 of
0.8, 19 and 7 nM for EGFR, HER-2 and ErbB-4, respectively. It effectively inhibits the growth of esophageal
squamous cell carcinoma which co-expresses both EGFR and HER2 with the inhibition of phosphorylation of
both MAPK and Akt. This inhibition is highly selective for erbB1 (epidermal growth factor receptor), ErbB2,
ErbB3, and ErbB4 without inhibiting tyrosine kinase activity of receptors such as PDGFR, FGFR, and IR, even
at high concentrations.
Synonyms:

Canertinib, PD-183805, PD183805
Size Price
N
N
HN
F
Cl
HN
O N
O
O
Produced Independently by our customer Dr.Zhang, Tianjin Medical University
Western blot analysis of extracts from EGF, CI-1033
(Selleckchem S1019) treated T47D breast adenocarcinoma
cell line using antibodies as indicated.
S1019 CI-1033
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10mg
Toll Free:(877)796-6397 www.selleckchem.com info@selleckchem.com
Phone:+1-832-582-8158
---USA and Canada only---
c-Kit (CD117, also called KIT or C-kit receptor)
Synonyms:
ZM 252868, AG 1517, Tyrphostin AG 1517 S1018 CHIR-258 Page 7
Synonyms:
ZM 252868, AG 1517, Tyrphostin AG 1517 S1363 Ki8751 Page 8
Synonyms:

TKI-258, Dovitinib, TKI258
Synonyms:
ZM 252868, AG 1517, Tyrphostin AG 1517 S1064 Masitinib Page 6
Synonyms:

AB1010, Masivet
Synonyms:
ZM 252868, AG 1517, Tyrphostin AG 1517 S1244 MP-470 Page 8
Synonyms:
ZM 252868, AG 1517, Tyrphostin AG 1517 S1220 OSI-930 Page 8
Synonyms:
ZM 252868, AG 1517, Tyrphostin AG 1517 S1178 BAY 73-4506 Page 8
Synonyms:

Regorafenib
c-Met (mesenchymal-epithelial transition factor)
Synonyms:
HKI-272 S1094 PF-04217903
PF-04217903 is an orally bioavailabe, small-molecule MET tyrosine kinase inhibitor with potential
antineoplastic activity. PF-04217903 demonstrates exquisite kinase selectivity. On the basis of the percent
inhibition or IC50 values generated from each of these screens, PF-04217903 was estimated to be>1000-fold
selective for c-Met compared with each of the other kinases included in these collective screening assays.
Size Price
N
N
N
N
N
N
N
N
HO
S1316 AMG-208
AMG 208 is a small molecule inhibitor of c-Met, which inhibits both ligand-dependent and ligand-independent
c-Met activation. It is being investigated as a cancer treatment.
Size Price
N O
O
N
N
N
N
S1114 JNJ-38877605
JNJ-38877605 is an orally bioavailable, highly specific c-Met inhibitor (selective over other 229 kinases
tested). This agent inhibits c-Met and Phospho-Met with IC50 at 4 nmol/L and 50 nmol/L, respectively. In
addition, JNJ-38877605 induces regression of U87-MG xenografts in vivo.
Size Price
N
F
F
N
N
N
N
N
N
Synonyms:
ZM 252868, AG 1517, Tyrphostin AG 1517 S1068 PF-2341066
PF-2341066 is Inhibitor of the catalytic activity of c-Met kinase and the NPM-ALK fusion protein. PF-2341066
inhibited NPM-ALK phosphorylation in Karpas299 or SU-DHL-1 ALCL cells (mean IC50 value=24 nM).
PF-2341066 potently inhibited cell proliferation, which was associated with G1-Sphase cell cycle arrest and
induction of apoptosis in ALK-positive ALCL cells (IC50 values=30 nM) but not ALK-negative lymphoma cells.
Synonyms:

Crizotinib
Size Price
N
NH2
O
(R) (R)
Cl Cl
F
N
N
HN
S1068 PF-2341066
Feed
Produced Independently by our customer Dr.Zhang, Tianjin Medical University
Western blot analysis of p-cMet, c-Met, p-MAPK, MAPK, p-Akt, Akt.
PF-2341066 treated T47D breast adenocarcinoma
cell line using antibodies as indicated.
S1068 PF-04217903
Feed
Produced Independently by our customer Dr.Zhang, Tianjin Medical University
Western blot analysis of p-cMet, c-Met, p-MAPK, MAPK, p-Akt, Akt.
PF-04217903 treated T47D breast adenocarcinoma
cell line using antibodies as indicated.
Ard|oderes|s/Tvros|reK|rase
Solutions to Signal Transduction Research
l4
c-KiI / c-IeI
10mg
50mg
200mg
5mg
10mg
50mg
10mg
50mg
200mg
5mg
10mg
50mg
cMET
MAPK
p-MAPK
AKT
p-AKT
p-cMET
0 0.1 1.0 10.0 100.0 0
HGF (ng/ml)
PF2341066(nM)
10 10 10 10 10 0
cMET
MAPK
p-MAPK
AKT
p-AKT
p-cMET
0 0.1 1.0 10.0 20.0 0
HGF (ng/ml)
Pf04217903 (M)
10 10 10 10 10 0
FLT-3 (fms-like tyrosine kinase receptor-3)
c-IeI / FLT-3
Ard|oderes|s/Tvros|reK|rase
l5
S1361 MGCD-265 Page 8
Synonyms:
ZM 252868, AG 1517, Tyrphostin AG 1517 S1111 Foretinib Page 9
Synonyms:

XL880,

GSK1363089, GSK089, EXEL-2880
S1005 Axitinib
Page 10 Synonyms:

AG-013736
S1112 SGX-523
SGX-523, an orally bioavailable small molecule, specifically binds to c-Met protein, or hepatocyte growth factor
receptor (HGFR), preventing binding of hepatocyte growth factor (HGF) and disrupting the c-Met signaling
pathway. This agent has shown exceptional selectivity for the cMET receptor tyrosine kinase over more than
200 protein kinases. SGX-523 may induce cell death in tumor cells expressing c-Met in vitro and in vivo.
Size Price
N
S
N
N
N
N
N
N
S1070 PHA-665752
PHA-665752 was identified as a small molecule, ATP-competitive, active site inhibitor of the catalytic activity
of c-Met kinase (Ki of 4 nM, IC50 of 9 nM). PHA-665752 also exhibited >50-fold selectivity for c-Met compared
with a panel of diverse tyrosine and serine-threonine kinases. In cellular studies, PHA-665752 potently
inhibited HGF-stimulated and constitutive c-Met phosphorylation, as well as HGF and c-Met-driven
phenotypes such as cell growth of a variety of tumor cells.
Size Price
Cl
Cl
S
O O
H
N
O
H
N
N
O
N

S1080 SU11274
68LVDKLJKO\VSHFLILFLQKLELWRURIF0HWZLWKLQYLWUR,&IRUWKHF0HWHQ]\PHDWPRO/7KH
inhibitor did not affect other tyrosine kinase oncoproteins, including BCR-ABL, TEL-JAK2, TEL-PDGF_R, or
TEL-ABL. Inhibition of the Met kinase activity by SU11274 led to time- and dose-dependent reduced cell
growth. SU11274 belongs to a class of small molecule RTK inhibitors that exert their activity by competing for
the Mg-ATP complex binding pocket, which results in inhibition of kinase activity and subsequent downstream
signaling.
Synonyms:

PKI-SU11274
Size Price
Cl
N
S
O O
H
N
O
HN
N
O
N
S1080 SU11274
Feed
Produced Independently by our customer Dr.Zhang, Tianjin Medical University
Western blot analysis of p-cMet, c-Met, p-MAPK, MAPK, p-Akt, Akt.
SU11274 treated T47D breast adenocarcinoma
cell line using antibodies as indicated.
cMET
MAPK
p-MAPK
AKT
P-AKT
0 0.1 1.0 10.0 20.0 0
p-cMET
HGF (ng/ml)
SU11274(M)
10 10 10 10 10 0
10mg
50mg
200mg
5mg
10mg
25mg
5mg
25mg
200mg
S1526 AC220
AC220 is a uniquely potent and selective FLT3 inhibitor with IC50 of 0.56 0.3 nM and >10 mM for MC4-11
and A375, respectively. It exhibits low nanomolar potency in biochemical and cellular assays and exceptional
kinase selectivity, and in animal models is efficacious at doses as low as 1 mg/kg given orally once daily. The
data reveal that the combination of excellent potency, selectivity, and pharmacokinetic properties is unique to
AC220, which therefore is the first drug candidate with a profile that matches the characteristics desirable for
a clinical FLT3 inhibitor.
S2158 KW 2449
KW-2449, a multi-kinase inhibitor of FLT3 (IC50 at 6.6pM), Abl(IC50 at 14pM), Abl-T315I and Aurora kinase.
KW-2449 potently and selectively inhibits the growth of leukemia cells harboring constitutively activated FLT3
kinase both in vitro and in vivo. On the other hand, KW-2449 had little effect on PDGFR, EGFR, and various
serine/threonine kinases even at a concentration of 1 uM. Among various serine/threonine kinases examined,
KW-2449 inhibited Aurora A kinase with IC50 of 48 pM and Aurora B kinase with the equivalent potency.
Size Price
Size Price
N
H
N
H
O
O
N
N
N
S
O
N
O
N
HN
O
N
N
H
Synonyms:
HKI-272 S1043 Tandutinib
In cell-based assays tandutinib inhibited FLT3, PDGFR, and KIT with IC50 values of 95-122 ng/mL, but had
no significant effect against a broad range of other kinases. In Ba/F3 cells expressing various FLT3-ITD
mutants, tandutinib inhibited IL-3-independent growth and FLT3-ITD auto-phosphorylation with IC50 values of
6-17 ng/ml. Tandutinib has a very limited spectrum of activity outside the type III receptor kinase family.
Synonyms:

MLN518, CT53518
Size Price
N N
O
N
N
H
N
O
O
O N
25mg
100mg
200mg
10mg
50mg
200mg
10mg
25mg
50mg
Toll Free:(877)796-6397 www.selleckchem.com info@selleckchem.com
Phone:+1-832-582-8158
---USA and Canada only---
VDA (Vascular Disrupting Agent)

S1537 DMXAA(ASA404)
DMXAA is a tumor-vascular disrupting agent with an IC50 of 9.46 1.7 nM. It attacks the blood supply of a
cancerous tumor to cause tumor regression. It has a striking antivascular and in some cases curative effect in
experimental tumors. The latter involving the release of further vasoactive agents, such as serotonin, tumour
necrosis factor, other cytokines, and nitric oxide from host cells.
Synonyms:

AS-1404, 5,6-MeXAA, NSC-640488, Vadimezan
Size Price
S1176 NPI-2358
NPI-2358 is a novel vascular disrupting agent acting on tubulin dimerization that destabilizes tumor vascular
endothelial cells and has cytotoxic activity (IC50 values of 10-15nM). NPI-2358 selectively induces tumor
vascular collapse and tumor regression in murine tumor models and potentiates other oncology agents.
Preclinical data suggest NPI-2358 may have advantages in terms of safety profile and activity.
Synonyms:

Plinabulin
Size Price
O
O
OH
O
HN
NH
O
O
NH
N
ETA-receptor (Endothelin receptor type A)

S1456 Zibotentan
Zibotentan is an orally administered, potent and specific ETA-receptor antagonist (IC50 = 21 nM). In vitro,
Zibotentan has been shown to compete with 125I-ET-1 for binding to the cloned human ETA-receptor with an
IC50 value of 21 nM. No binding to the ETB receptor was observed with concentrations of zibotentan in excess
RI 0 7KLV DJHQW LV FDSDEOH RI LQKLELWLQJ RU UHGXFLQJ WKH PXOWLWXGH RI HIIHFWV WKDW DUH HYRNHG E\ (7
activation of the ETA receptor and which promote tumor survival, growth and progression.
Synonyms:

ZD4054
Size Price
O
N
N
N
S
H
N O
O
N
N
O
HIF (Hypoxia-inducible factor)

S1233 2-Methoxyestradiol
2-Methoxyestradiol targets on both the tumor cell and endothelial cell compartments by inducing apoptosis in
rapidly proliferating cells and inhibiting blood vessel formation at several stages in the angiogenic cascade.
Moreover, the ability of 2-Methoxyestradiol(2ME2) to inhibit metastatic spread in several models adds to its
therapeutic value for cancer treatment at various stages of the disease.
Synonyms:

2-ME2
Size Price
O
HO
H
H
OH
H
ALK (anaplastic lymphoma kinase)
S1108 NVP-TAE684
NVP-TAE684 is a highly potent and selective small molecule ALK inhibitor, which blocked the growth of
ALCL-derived and ALK-dependent cell lines with IC50 values between 2 and 10 nM. NVP-TAE684 treatment
resulted in a rapid and sustained inhibition of phosphorylation of NPM-ALK and its downstream effectors and
subsequent induction of apoptosis and cell cycle arrest.
Synonyms:

TAE684
S1476 SB 525334
6%LVDVHOHFWLYHLQKLELWRURIWUDQVIRUPLQJJURZWKIDFWRUUHFHSWRU,$/.7*)5,,&Q0
7KLVDJHQWLQKLELWV7*)LQGXFHG$/.VHULQHWKUHRQLQHNLQDVHDFWLYLW\WKHUHE\SUHYHQWLQJSKRVSKRU\ODWLRQ
of the Smad transcription factors and subsequent gene activation.
Size Price
Size Price
N
N
NH
N
N
O
N
N
N
NH
N
N
Cl
HN
S
O
O
Synonyms:
ZM 252868, AG 1517, Tyrphostin AG 1517 S1003 ABT-869
Synonyms:
ZM 252868, AG 1517, Tyrphostin AG 1517 S1490 AP24534
Synonyms:
ZM 252868, AG 1517, Tyrphostin AG 1517 S1018 CHIR-258
Synonyms:
ZM 252868, AG 1517, Tyrphostin AG 1517 S1119 XL184
Synonyms:

Linifanib, AL-39324, RG3635
Synonyms:

Ponatinib
Synonyms:

TKI-258, Dovitinib, TKI258
Synonyms:
ZM 252868, AG 1517, Tyrphostin AG 1517 S1134 AT9283
Page 6
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Ard|oderes|s/Tvros|reK|rase
Solutions to Signal Transduction Research
l6
FLT-3 / ALK / VDA / ETA-recepIor / HIF
5mg
10mg
200mg
5mg
50mg
100mg
5mg
25mg
100mg
10mg
50mg
200mg
10mg
50mg
200mg
50mg
100mg
300mg

Tie2 kinase
Syk (Spleen tyrosine kinase)

S2206 R788
R788 is a selective Syk inhibitor with an IC50 of 41 nM. R788 exhibits inhibitory activity against SYK but also
LQKLELWVDEURDGVSHFWUXPRIRWKHUNLQDVHWDUJHWV,QDGGLWLRQWREORFNLQJ)F5PHGLDWHGHYHQWV5DOVR
blocked BCR-mediated Ag presentation, thus broadly interrupting the humoral contributions to T cell-driven
autoimmunity.
Synonyms:

FosD, Tamatinib Fosdium
Size Price
S1533 R406(free base)
R406 is an orally available spleen tyrosine kinase inhibitor with a Ki of 30 nM. R406 blocked Syk-dependent
FcR-mediated activation of monocytes/macrophages and neutrophils and BCR-mediated activation of B
lymphocytes. R406 was selective as assessed using a large panel of Syk-independent cell-based assays
representing both specific and general signaling pathways.
Size Price
O
O
O
N
H
N
N
F
N
H
N N
H
O
O
O
O
O
H
N
N
N
F
H
N N
O
N O
O
P
-
O O
-
O
Na
+
Na
+
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S2194 R406
R406 is an orally available spleen tyrosine kinase inhibitor with an IC50 of 41 nM. R406 blocked
Syk-dependent FcR-mediated activation of monocytes/macrophages and neutrophils and BCR-mediated
activation of B lymphocytes. R406 treatment ameliorated joint inflammation in a number of rodent models of
rheumatoid arthritis and also blocked JNK-mediated gene expression in human synoviocytes.
Size Price
O
O
O
N
H
N
N
F
N
H
N N
H
O
O
S
OH
O
O
\l"
S1119 XL184 Page 9
Syk / Tie2 kinase Ard|oderes|s/Tvros|reK|rase
l/
10mg
50mg
200mg
10mg
50mg
200mg
1mg
5mg
50mg
Toll Free:(877)796-6397 www.selleckchem.com info@selleckchem.com
Phone:+1-832-582-8158
---USA and Canada only---
l8
Cell Cycle/Checkpoint Pathway
The term cell-cycle checkpoint refers to mechanisms by which the cell
actively halts progression through the cell cycle until it can ensure that an
earlier process, such as DNA replication or mitosis, is complete. The cell
cycle and cell cycle-associated proteins play essential roles in cell fate,
including cell replication, cell death, and cell function.
At present, the most well-characterized cell-cycle proteins are the
serine/threonine kinases Cdk1 and Cdk2 and proteins acting as inhibitors of
these kinases, p21 and p27. Rho in this definition functions as a molecular
switch in cellular processes such as cell morphogenesis, adhesion, migration
and cell cycle progression including cytokinesis. DNA polymerases are
rarely the actual, final target for chemotherapeutics, the biological activity of
some nucleoside-based drugs absolutely depends upon DNA polymerases
to incorporate them into DNA. The purine- and pyrimidinebased nucleoside
antimetabolites are frontline therapies for a large number of different tumors.
DNA topoisomerases are critical for DNA replication because of their ability
to unwind DNA and relieve superhelical stress in the DNA enzyme potently
kills replicating cells.
Aro|elorrove|ce||-cvc|eprole|rs|rpodocvleo|o|odv.
Peter M. Price. Kidney International. 2010(77), 660 661
lrlroducl|orloCarcerC|erol|erapeul|cs.
Donna S. Shewach. Chem. Rev. 2009;109 (7):28592861

l9
S1109 BI 2536
Targeting Mitotic Exit Leads to Tumor Regression In Vivo: Modulation by Cdk1, Mastl and the
PP2A/B55a,d Phosphatase.
Eusebio Manchado et al. Cancer Cell, 2010(18):641654
Small Molecule Kinase Inhibitor Screen Identifies Polo-Like Kinase 1 as a Target for Neuro-
blastoma Tumor-Initiating Cells.
Natalie Grinshtein et al. Cancer Res, 2011(71):1385-1395
S1532 AZD7762
Histone Deacetylase Inhibitors Downregulate Checkpoint Kinase 1 Expression to Induce Cell
Death in Non-Small Cell Lung Cancer Cells.
William Brazelle et al. PLoS ONE, 2010; 5(12): e14335.
Papers
Using Selleck Products
ROCK
PLK (Polo-like kinase)

S1573 Fasudil HCl
)DVXGLO+&OLVF\FOLFQXFOHRWLGHGHSHQGHQWSURWHLQNLQDVHLQKLELWRUDQG52&.LQKLELWRUZLWKDQ,&RI
M. It is also a Ca
2+
antagonist and vasodilator. It also inhibits proliferation of vascular smooth muscle cells.
Synonyms:

HA-1077, AT-877
Size Price
S1474 GSK429286A
GSK429286A is a cell-permeable, selective inhibitor of Rho-associated kinase (ROCK). ROCK inhibitors have
been found to prevent apoptosis, as well as to enhance the survival and cloning efficiency of dissociated
human embryonic stem (ES) cells without affecting their self-renewal properties or pluripotency. Because of
GSK429286A's specificity, this reagent may be useful in assessing the cellular roles of individual ROCK
isoforms.
Size Price

S1049 Y-27632
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rabbit tissues respectively. The IC50 value of Y-27632 was 1 0.2 mol/L for the inhibition of shape change
by U46619.
Size Price
N
S
N
O
O
NH
HCl
H
N O
H
N
O
F F
F
F
N
H
N
N
N
H
O
H
NH
2

S1109 BI 2536
BI 2536 is a small molecule compound with potential anti-neoplastic activities. BI 2536 binds to and inhibits
PLK1 (with IC50of 0.83 nM), resulting in mitotic arrest, disruption of cytokinesis, and apoptosis in susceptible
tumor cell populations. This compound showed a more than 1000-fold selectivity relative to a panel of 63 other
protein kinases, but it also affected the activities of PLK2 at an IC50 of 3.5 nM and, to a slightly lesser extent,
the activity of PLK3 (IC50 9.0 nM).
Size Price
S2193 GSK461364
GSK 461364 is a potent small molecule PLK1 inhibitor with a Ki of 2.2 nM. GSK461364 is an ATP-competitive
inhibitor of PLK1 and forms a rapidly reversible complex with PLK1. It has a 400-fold greater potency for PLK1
than for PLK2 and PLK3. It is > 100-fold selective with respect to PLk2, PLK3, and 48 other kinases tested.
Size Price
O
N
N
H
N
H
O N
N
N O
N
\l"
N
N
N
N
S
O
NH2
O
F
F
F
CDK (Cyclin-dependent kinase)
S1485 HMN-214
HMN-214 is a potent PLK1 inhibitor (an average cell IC50 of 118 nM). HMN-176 interferes with PLK1, but does
not appear to directly inhibit PLK1. Instead, it alters its spatial distribution, resulting in cell cycle arrest at the
G2M phase, with destruction of the spindle polar bodies followed by DNA fragmentation. Drug-resistant cell
lines showed low crossresistance to HMN-176. In human tumor xenografts, there was a broad spectrum of
antitumor activity.
Size Price
Synonyms:

IVX-214
S1362 ON-01910
ON-01910 is a non-ATP-competitive small molecule Plk1 inhibitor with an IC50 of 9 nM. It induces mitotic
arrest of tumor cells characterized by spindle abnormalities leading to their apoptosis. In vivo, this compound
did not exhibit hematotoxicity, liver damage, or neurotoxicity, and was a potent inhibitor of tumor growth in a
variety of xenograft models. ON01910 showed strong synergy with several chemotherapeutic agents, often
inducing complete regression of tumors.
Size Price
Synonyms:

Estybon
N N
S
O
O
O
O
O
O
O O
S
O O
O
NH
ONa
O

S1524 AT7519
AT7519 is a novel small molecule multi-cyclin-dependent kinase inhibitor. It selectively binds to and inhibits
CDKs, which may result in cell cycle arrest, induction of apoptosis, and inhibition of tumor cell proliferation.
CDKs are serine/theronine kinases involved in regulation of the cell cycle and may be overexpressed in some
types of cancer cells.
Synonyms:
AT 7519 Size Price Size Price
Cl Cl
NH O
HN N
O
N
H
NH
Ce||Cvc|e/C|ec|po|rl
Solutions to Signal Transduction Research
20
ROCK / PLK / CDK
10mg
50mg
100mg
2mg
50mg
10mg
50mg
200mg
5mg
10mg
50mg
10mg
50mg
200mg
10mg
50mg
200mg
10mg
50mg
200mg
5mg
10mg
25mg
S1153 Roscovitine
Roscovitine is a potent and selective inhibitor of CDKS. Roscovitine inhibits p34 cdc2/cyclin B (IC50 = 0.65
M), p33 CDK2/cyclin A (IC50 = 0.70 M), p33 CDK2/cyclin E (IC50 = 0.70 M), and p33 cdk2/p35(IC50 =
0.20 M) by competing for the ATP binding domain of these kinases. Roscovitine exhibits very low sensitivity
towards related kinases, such as Erk1 and Erk2 (IC50 = 34 M and 14 M, respectively). Roscovitine displays
increased anti-mitotic activity at the G1/S and G2/M phases of the cell cycle.
Synonyms:

CYC202, Seliciclib
Size Price
N
N
N
N
N
H
HO
HN
S1572 BS-181 HCl
BS-181 is a selective cyclin-dependent kinase inhibitor with an IC50 of 21 nM for the inhibition of
CDK-activating kinase. Testing of other CDKs as well as another 69 kinases showed that BS-181 only
LQKLELWHG&'.DWFRQFHQWUDWLRQVORZHUWKDQ0ZLWK&'.EHLQJLQKLELWHGIROGOHVVSRWHQWO\,&
nM) than CDK7. In MCF-7 cells, BS-181 inhibited the phosphorylation of CDK7 substrates, promoted cell cycle
arrest and apoptosis to inhibit the growth of cancer cell lines.
Size Price
N
N
N
N
H
H2N
HN
HCl

S2386 Indirubin
,QGLUXELQLVDSRWHQWF\FOLQGHSHQGHQWNLQDVHVDQG*6.LQKLELWRUZLWK,&RIDERXWQ0DQG0,W
LQKLELWV&'.DQG*6.PHGLDWHGWDXSKRVSKRU\ODWLRQ$OVRLQKLELWV$03./&.DQG6*.,QGXFHVFHOO
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inflammatory agents and carcinogens.
Size Price
H
N
O
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O
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S1230 Flavopiridol
Flavopiridol inhibited rhabdoid cell growth (IC50-200nmol/L) , induced G1 and G2 arrest, and apoptosis in vitro
in a concentration-dependent manner. These effects were correlated with the down-modulation of cyclin D1,
up-regulation of p21, and induction of caspase 3/7 activities. Flavopiridol (at 7.5 mg/kg) significantly inhibited
the growth of xenografted rhabdoid tumors, and its effect was correlated with the induction of p21 and
down-modulation of cyclin D1.
Synonyms:

HMR-1275, Alvocidib, L868275
Size Price
S1249 JNJ-7706621
JNJ-7706621 blocked proliferation of cancer cells regardless of their p53, retinoblastoma or P-glycoprotein
status and induced cell death by activating apoptosis; delayed progression through G1 and arrested the cell
cycle at the G2/M phase; decreased CDK1 kinase activity, altered CDK1 phosphorylation status and blocked
signaling to downstream substrates of CDKs; reduced histone H3 phosphorylation; inhibited Aurora kinase. In
YLWURFHOOSUROLIHUDWLRQDVVD\V,&PRO/+H/D,&+&7,&3&,&
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S1116 PD0332991
PD0332991 is an orally available pyridopyrimidine-derived CDK inhibitor with potential antineoplastic activity.
7KLVFRPSRXQGLVDKLJKO\VSHFLILFLQKLELWRURI&'.,&PRO/DQG&'.,&PRO/
having no activity against a panel of 36 additional protein kinases. Therapeutic doses of PD0332991 cause
elimination of phospho-Rb and the proliferative marker Ki-67 in tumor tissue and downregulation of genes
under the transcriptional control of E2F.
Size Price

S1487 PHA-793887
PHA-793887 is a novel pan-cdk inhibitor, including CDK1, CDKT2, CDK4, CDK5, CDK7, and CDK9 with IC50
in the 5 to 140 nM range. It is inactive against other 34 kinases representative of all kinase families, in
particular c-Abl, c-Kit, lck, and TRKA with IC5010 mM. It shows anti-proliferative activity against several
solid tumor cell lines, with IC501 mM. In these cells, it is able to inhibit Rb phosphorylation and expression
of S-phase cyclins, such as cyclin A.
Size Price
O
O OH
HO
N
H
HO
Cl
HN
N
N
N
H
N
N
N O
O
H
N
N
N
N
O
HN
O
Data provided by our customer Pierre Roger,
IRIBHM,ULB,BRUSSELS(Belgium).
S
H
2
N
O
O
NH
N
N
N
H
2
N
F
F
O
S1249 JNJ-7706621
Feed
Produced Independently by our customer Dr.Zhang, Tianjin Medical University
Western blot analysis of p-Histone H3, Histone H3, p-Aurora A/B/C,
$XURUD$0-1-ZDVDGGHG
S1116 PD-0332991
Feed
Serum-deprived T98G glioma cells are restimulated with
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CDK4/6 inhibitor.
CDK Ce||Cvc|e/C|ec|po|rl
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p-Histone H3
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p-Aurora
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0

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M JNJ-7706621
10mg
25mg
50mg
5mg
25mg
100mg
10mg
25mg
50mg
1mg
5mg
10mg
5mg
10mg
25mg
5mg
10mg
50mg
10mg
25mg
50mg
Toll Free:(877)796-6397 www.selleckchem.com info@selleckchem.com
Phone:+1-832-582-8158
---USA and Canada only---
Topoisomerase
S1145 SNS-032
SNS-032 is a small-molecule CDK inhibitor for the treatment of B-cell malignancies and advanced solid
tumors. SNS-032 is a specific and potent inhibitor of CDK2, 7 and 9 which induces cell cycle arrest and
apoptosis in tumor cell lines. It was shown to inhibit in vitro angiogenesis and prostaglandin E2 (PGE2)
production, both strongly associated with tumorigenesis. Phase I clinical trials support the safety and
tolerability of SNS-032 as evaluated in dose-escalation studies.
Size Price
Synonyms:

BMS-387032
N
O
S
N
S
H
N
O
NH

S1208 Adriamycin
Adriamycin is an anthracycline antibiotic and is used in cancer chemotherapy. It inhibits the progression of the
enzyme topoisomerase II, which relaxes supercoils in DNA for transcription. Doxorubicin stabilizes the
topoisomerase II complex after it has broken the DNA chain for replication, preventing the DNA double helix
from being resealed and thereby stopping the process of replication. It has an inhibitory effect on MCF-7 and
0'$0%ZLWK,&RIDQG0UHVSHFWLYHO\
Synonyms:

Doxorubicin, Rubex
Size Price

S1288 Camptothecine
Camptothecin (CPT) is a cytotoxic quinoline alkaloid which inhibits the DNA enzyme topoisomerase I (topo I).
It was isolated from the bark and stem of Camptotheca acuminata, a tree native in China. Two CPT analogues
have been approved and are used in cancer chemotherapytoday, topotecan and irinotecan.
Size Price
S2217 Irinotecan HCl Trihydrate
,ULQRWHFDQK\GURFKORULGHWULK\GUDWHLVDWRSRLVRPHUDVH,LQKLELWRUZLWK,&RIDQG0IRU/R9RFHOOV
and HT-29 cells, respectively. As a Topo I inhibitor, Irinotecan inhibits the religation step of the enzymes
normal action, inducing single stranded DNA breaks. Irinotecan is activated by esterases to produce the
activated metabolite and has been reported to be associated with cleavage of PARP in colon carcinoma cells.
Synonyms:

CPT 11, Camptosar, Campto, Irinotecan
Size Price
O O
O
OH
OH
O
O
H
OH
NH2
OH
O
OH
.HCl
O N
O
O
HO N
N N
O
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N
N
O
O
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H2O
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Microtubule

S2209 Vinflunine Tartrate
Vinflunine Tartrate is a new microtubule inhibitor with IC50 of 18.8 nM. Vinflunine suppressed the rate of
WUHDGPLOOLQJ,& 02WKHUHIIHFWVVXFKDVLQGXFWLRQRIFHOOF\FOHDUUHVWDW*0GLVUXSWLRQRIWKH
microtubular network of interphase cells and formation of paracrystals, generally required 3- to 17-fold higher
concentrations of vinflunine than the other vinca alkaloids.
Size Price
N
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O
O
O
O
O
N
H
N
F
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S1225 Etoposide
Etoposide caused an increase in the mean fluorescence intensity of FasR in both subclones, and an induction
of FasL in the ES subclone. However, no change in the numbers of apoptotic cells induced by etoposide was
observed when FasR was blocked by an antagonist anti-Fas antibody, nor was an agonist anti-Fas antibody
alone cytotoxic to the subclones or enhanced the cytotoxic effect of etoposide.
Synonyms:

Eposin, Vepesid, VP-16, Toposar
Size Price
O
O
O
O
H
O
OH
O
H
O O
H
OH
OH
O
O
H
H

S1198 Irinotecan
Irinotecan is an inhibitor of topoisomerase I and is activated by hydrolysis to SN-38. The inhibition of
topoisomerase I by the active metabolite SN-38 eventually leads to inhibition of both DNA replication and
transcription. Its main use is in colon cancer, particularly in combination with other chemotherapy agents. The
F\WRWR[LFLW\RILULQRWHFDQDQG61LQWKHWZRFHOOOLQHVZDVDVIROORZHGLULQRWHFDQ,&YDOXHVZHUH0
IRU/R9RFHOOVDQG0IRU+7FHOOV61,&YDOXHVZHUHQ0IRU/R9RFHOOVDQGQ0IRU
HT-29 cells.
Synonyms:

Camptosar
Size Price

S2485 Mitoxantrone
Mitoxantrone is a type II topoisomerase inhibitor with IC50 of 2.0 M, 0.42 mM for HepG2 and MCF-7/wt cells,
respectively. It disrupts DNA synthesis and DNA repair in both healthy cells and cancer cells. It is used in the
treatment of certain types of cancer, mostly metastatic breast cancer, acute myeloid leukemia, and
non-Hodgkins lymphoma. It was also shown to improve the survival of children suffering from first relapse of
acute lymphoblastic leukaemia.
Size Price
N N
O
O N
N
O
O
O
HO
S1231 Topotecan HCl
Topotecan hydrochloride is a chemotherapy agent that is a topoisomerase I inhibitor. It is the water-soluble
derivative of camptothecin. It is used to treat ovarian cancer and lung cancer, as well as other cancer types.
Synonyms:

Hycamtin, NSC 609699
Size Price
N
N
OH
N
O
O
O
HO
HCl
OH
OH
O
O
HN
HN
H
N
OH
N
H
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Ce||Cvc|e/C|ec|po|rl
Solutions to Signal Transduction Research
22
CDK / Topoisomerase / IicroIubule
25mg
100mg
200mg
5mg
10mg
50mg
500mg
1g
5g
100mg
200mg
1g
25mg
100mg
500mg
100mg
200mg
1g
100mg
200mg
250mg
50mg
100mg
200mg
10mg
50mg
200mg


S2195 CYT997
CYT997, a synthetic small molecule optimized for antiproliferative activity in a panel of cell-based assays, in
which the compound shows an IC50 of between 1 and 100 nmol/L across a panel of cancer cell lines. The
FRPSRXQG LQKLELWV WKH SRO\PHUL]DWLRQ RI WXEXOLQ ZLWK DQ ,& RI PRO/ &<7 FDXVHV D VLJQLILFDQW
increase of cells in the G2/M phase of the cell cycle. Caspase-3 activation is also observed in cells treated with
CYT997 along with the generation of PARP.
Size Price

S1165 ABT-751
ABT-751 is a bioavailable antimitotic sulfonamide agent that binds to the colchicine-binding site on
beta-tubulin and inhibits the polymerization of microtubules, thereby preventing tumor cell replication.
ABT-751 is not a substrate for the MDR transporter and is active against cell lines resistant to vincristine,
doxorubicin, and cisplatin. This agent also disrupts tumor neovascularization, reducing tumor blood flow and
so inducing a cytotoxic effect.
Size Price

S2284 Colchicine
Colchicine inhibits microtubule polymerization by binding to tubulin. Since one of the defining characteristics
of cancer cells is a significantly increased rate of mitosis, this means that cancer cells are significantly more
vulnerable to colchicine poisoning than are normal cells. However, the therapeutic value of colchicine against
cancer is limited by its toxicity against normal cells.
Size Price
S1148 Docetaxel
Docetaxel is a semi-synthetic, second-generation taxane, with anti-neoplastic application for the treatment of
breast, ovarian, and non-small cell lung cancer. Docetaxel binds to and stabilizes tubulin, thereby inhibiting
microtubule disassembly which results in cell- cycle arrest at the G2/M phase and cell death. The overall cells
mean IC50 for docetaxel treatment was 4.67 nM,This agent also inhibits pro-angiogenic factors such as VEGF
and displays immunomodulatory and pro-inflammatory properties by inducing various mediators of the
inflammatory response.
Synonyms:

Taxotere
Size Price
O
S
O
O
H
N
N HN
OH
O
O
N
H
O
O
O
O
H
O
O
O
OH
O HO
O
Ac OH O
O
OH
N
H
O
O
S1297 Epothilone A
Epothilone A is a new kind of microtubule function inhibitor with an IC50 of 4.4 nM for tubulin polymerization
and cytotoxicity. It competitively inhibits [3H]-paclitaxel binding to microtubules. It prevents cancer cells from
dividing by interfering with tubulin. It exhibits kinetics similar to paclitaxel by inducing tubulin polymerization in
vitro and producing enhanced microtubule stability and bundling in cultured cells. Epothilone A exhibits a
greater cytotoxicity against P-glycoprotein-expressing multidrug resistant (MDR) cells (IC50 = 20 nM).
Synonyms:

Ellence, Pharmorubicin, Epirubicin Ebewe
Size Price
O O
N
S
O
OH
O
OH
N N
N
H
O
NH
O
N
H
N
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S1364 Epothilone B
Epothilone B is a new kind of cancer drugs and microtubule function inhibitor with an IC50 of 3.5 nM.
Epothilone B suppressed microtubule dynamics in a concentration-dependent manner coincident with mitotic
block. At the IC50, 80% of the cells had nearly complete stabilization of microtubule dynamics, and no
anaphase or telophase figures were observed.
Synonyms:

EPO906, EpoB, Patupilone
Size Price
O O
N
S
O
OH
O
OH

S1150 Paclitaxel
Paclitaxel is a microtubule polymer stabilizer with an IC50 of 0.1 pM for human endothelial cells. It selectively
inhibits the proliferation of human endothelial cells at ultra low concentrations (0.1-100 pM), while it inhibits
non-endothelial type human cells with IC50 1-10 nM. The selectivity of paclitaxel inhibition of cell proliferation
is also species specific. Paclitaxel blocks cells in G2/M, and this may result in a schedule-dependent effect on
paclitaxel cytotoxicity.
Synonyms:

Onxol, Taxol, Nov-Onxol
Size Price

S1241 Vincristine Sulfate
Vincristine Sulfate is a kind of microtubule function inhibitor with IC50 of 10.41.1, 28.13.4, 22.42.1 M for
HL-60, Bel7402, HO-8910, respectively. Vincristine binds irreversibly to microtubules and spindle proteins in
S phase of the cell cycle and interferes with the formation of the mitotic spindle, thereby arresting tumor cells
in metaphase. This agent also depolymerizes microtubules and may also interfere with amino acid, cyclic
AMP, and glutathione metabolism.
Synonyms:

leurocristine, Oncovin, Vincasar PFS, Vincrex
Size Price

S1240 Vinflunine
Vinflunine is a novel fluorinated Vinca alkaloid currently and tubulin assembly inhibitor with an IC50 of 18.8 nM
for mitotic accumulation. t is interesting that the IC50 and IC70 concentrations suppressed microtubule
dynamics, slowed down mitotic progression from metaphase to anaphase, and induced a postmitotic G1
arrest. This G1 arrest was associated with an increase in p53 and p21 expression and with their nuclear
translocation.
Synonyms:

Javlor
Size Price
O
N
H
HO
O
O
O
O
O
OH
O
O
O
O
O
OH
H
O
N
N
O
H
O O
OH
O
O
H
O
O
HN
N OH
H
S
O
O
OH
HO
N
N
H
HOH
O
O
O
O
O
N
H
N
F
F
O
O
IicroIubule Ce||Cvc|e/C|ec|po|rl
23
10mg
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1mg
5mg
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1g
10mg
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1mg
5mg
Toll Free:(877)796-6397 www.selleckchem.com info@selleckchem.com
Phone:+1-832-582-8158
---USA and Canada only---
Antimetabolites
S1156 Capecitabine
As a prodrug, capecitabine is selectively activated by tumor cells to its cytotoxic moiety, 5-fluorouracil (5-FU);
subsequently, 5-FU is metabolized to two active metabolites, FdUMP and FUTP by both tumor cells and
normal cells. Capecitabine is a chemotherapy drug that is given as a treatment for many types of cancer,
including bowel cancer, breast cancer, stomach cancer and oesophageal cancer.
Synonyms:

Xeloda
Size Price

S1199 Cladribine
Cladribine is a drug used to treat hairy cell leukemia and multiple sclerosis. As a purine analog, it is a synthetic
anti-cancer agent that also suppresses the immune system. Chemically, it mimics the nucleoside adenosine
and thus inhibits the enzyme adenosine deaminase, which interferes with the cells ability to process DNA. It
is easily destroyed by normal cells except for blood cells, with the result that it produces relatively few side
effects and results in little non-target cell loss.
Synonyms:

Leustatin, 2-chlorodeoxyadenosine
Size Price

S1218 Clofarabine
Clofarabine is a second generation purine nucleoside analog. It is phosphorylated intracellularly, which inhibits
the enzymatic activities of ribonucleotide reductase (IC50 = 65 nM) and DNA polymerase, resulting in inhibition
of DNA repair and synthesis of DNA and RNA. Clofarabine also disrupts mitochondrial function and membrane
integrity, resulting in the release of pre-apoptotic factors, including cytochrome C and apoptotic-inducing
factor, which activate apoptosis.
Synonyms:

Clolar, Evoltra
Size Price

S1200 Decitabine
Decitabine is a cytidine antimetabolite analogue with potential antineoplastic activity. Decitabine incorporates
into DNA and inhibits DNA methyltransferase, resulting in hypomethylation of DNA and intra-S-phase arrest of
DNA replication. The use of decitabine could result in activation of several tumor suppressor genes and
induction of differentiation of undifferentiated cells.
Synonyms:

Dacogen, 5-aza-2'-deoxycytidine
Size Price
S1299 Floxuridine
Floxuridine is an oncology drug that belongs to the class known as antimetabolites. The drug is most often
used in the treatment of colorectal cancer. Floxuridine, an analog of 5-fluorouracil, is a fluorinated pyrimidine.
Synonyms:

Fluorodeoxyuridine
Size Price
N N
O
F
O
OH
HO
N
H
O
O
N N
N
N
H
2
N
Cl
O
OH
OH
N
N
N
N
NH2
Cl
O
F
HO
OH
O
HO
HO
N
N
N
O
NH
2
O
N
HO
HO
NH
O
F
O

S1229 Fludarabine Phosphate
Inside the cells rephosphorylation occurs which leads to fuoroadenine arabinoside triphosphate (F-ara-ATP),
the major cytotoxic metabolite of F-ara-A. This metabolite inhibits several key processes necessary for the
DNA replication. Fludarabine can also induce pro-inflammatory stimulation of monocytic cells, as evaluated by
increased expression of ICAM-1 and IL-8 release. Fludarabine did not affect the growth of ovarian cancer cell
lines, whereas it induced a marked and dose-dependent inhibition of proliferation in melanoma cell lines.
Synonyms:

Fludara
Size Price
S1491 Fludarabine
Fludarabine inhibits several key processes necessary for the DNA replication, ribonucleotide reductase, DNA
primase, DNA polymerase, 3-5 exonuclease activity of DNA polymerase d and e and DNA ligase I.
Fludarabine can also induce pro-inflammatory stimulation of monocytic cells, as evaluated by increased
expression of ICAM-1 and IL-8 release. Fludarabine did not affect the growth of ovarian cancer cell lines,
whereas it induced a marked and dose-dependent inhibition of proliferation in melanoma cell lines.
Synonyms:

Fludara
Size Price

S1149 Gemcitabine HCl
Gemcitabine is converted intracellularly to the active metabolites difluorodeoxycytidine di- and triphosphate
(dFdCDP, dFdCTP). dFdCDP inhibits ribonucleotide reductase, thereby decreasing the deoxynucleotide pool
available for DNA synthesis; dFdCTP is incorporated into DNA, resulting in DNA strand termination and
apoptosis. Gemcitabine inhibits proliferation BxPC-3 pancreatic cancer cell line with IC50 of 0.06 M.
Synonyms:

Gemzar
Size Price

S1135 Pemetrexed disodium
Pemetrexed disodium (Alimta, Rolazar, Tifolar, MTA) is a thymidylate synthase, dihydrofolate reductase and
glycinamide ribonucleotide formyltransferase inhibitor with an IC50 of 25, 34, 220 nM for CCRF-CEM,
GC3/cl1, HCT-8, respectively.
Synonyms:

Alimta, LY-231514
Size Price

S1192 Raltitrexed
Raltitrexed is an antimetabolite drug used in cancer chemotherapy. It is an inhibitor of thymidylate synthase.
Raltitrexed is chemically similar to folic acid. It works by inhibiting Dihydrofolate reductase, an enzyme used in
the synthesis of tetrahydrofolate, thereby preventing the synthesis of thymidylate. Raltitrexed inhibits L1210
cell growth in culture IC50 = 9 nM, which is one of the strongest antimetabolites in use.
Synonyms:

Tomudex
Size Price
N N
N
N
H
2
N
F
O
HO
OPO
3
H
2
OH
O
N
N
N
N
NH
2
F
OH
HO
HO
N
N
O
O
HO
HO
F
F
NH
2
HCl
N
H
O
ONa
O ONa
O
HN
N
HN
O
H2N
O
OH
O
HO
NH
O S
N
NH
N
O
Ce||Cvc|e/C|ec|po|rl
Solutions to Signal Transduction Research
24
AnIimeIaboliIes
100mg
200mg
1g
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100mg
10mg
25mg
50mg
25mg
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Telomerase
DNA/RNA

S1521 Carmustine
Carmustine(BiCNU) is a cell-cycle phase nonspecific alkylating antineoplastic agent with ED50 ranging from
5.0 M to 11.9 M. It is used in the treatment of several types of brain cancer (including glioma, glioblastoma
multiforme, medulloblastoma and astrocytoma), multiple myeloma and lymphoma (Hodgkins and
non-Hodgkin). Three lines with O6-AGT activity below 25 fmol/mg protein had carmustine ED50 values
ranging from 5.0 M to 11.9 M.
Synonyms:

Gliadel, BCNU, NSC-409962, Becenun
Size Price

S1648 Cytarabine
&\WDUDELQH LV DQ DQWLPHWDEROLF DJHQW ZLWK WKH FKHPLFDO QDPH RI DUDELQRIXUDQRV\OF\WRVLQH ,W LV D
chemotherapy agent used mainly in the treatment of hematological malignancies. Because the arabinose
sugar sterically hinders the rotation of the molecule within DNA, DNA replication ceases, specifically during the
S phase of the cell cycle. This agent also inhibits DNA polymerase, resulting in a decrease in DNA replication
and repair.
Synonyms:

Ara-C, Cytosine Arabinoside, Cytosar-U
Size Price

S1666 Flucytosine
Flucytosine is a fluorinated pyrimidine analogue and a synthetic antimycotic drug. It is intrafungally converted
into the cytostatic fluorouracil that undergoes further steps of activation and finally interacts as
5-fluorouridinetriphosphate with RNA biosynthesis and disturbs the building of certain essential proteins. The
other mechanism is the conversion into 5-flourodeoxyuridinemonophosphate which inhibits fungal DNA
synthesis.
Synonyms:

Ancobon, 5-fluorocytosine, Ancotil
Size Price
S1889 Mitoxantrone 2HCl
Mitoxantrone Hydrochloride is a synthetic antineoplastic anthracenedione. It is a DNA-reactive agent that
intercalates into DNA through hydrogen bonding, causes crosslinks and strand breaks. It also interferes with
RNA and is a potent inhibitor of topoisomerase II, an enzyme responsible for uncoiling and repairing damaged
DNA. It has a cytocidal effect on both proliferating and nonproliferating cultured human cells, suggesting lack
of cell cycle phase specificity.
Synonyms:

NSC-310739, Novantrone
Size Price
N
Cl
N
H
Cl
N
O
O
N
O H
2
N
O
HO
OH
OH
HN
N O
F
NH
2
OH
OH
O
O
HN
H
N
OH
HN
N
H
OH
HCl
HCl

S1384 Mizoribine
Mizoribine is an imidazole nucleoside and an immunosuppressive agent. The immunosuppressive effect of is
due to the inhibition of DNA synthesis in the S phase of the cell cycle. Because of its relative lack of toxicity,
during the past decade MZB has been frequently used instead of azathioprine as a component of
immunosuppressive drug regimens. MZB is being used to treat renal transplantation patients, IgA
nephropathy, lupus erythematosus, and nephrotic syndrome.
Synonyms:

Bredinin
Size Price
S1915 Sulfamethoxazole
Sulfamethoxazole is a sulfonamide bacteriostatic antibiotic. It is most often used as a part of synergistic
combination with trimethoprim in a 5:1 ratio in co-trimoxazole. Sulfonamides are structural analogs and
competitive antagonists of para-aminobenzoic acid (PABA). They inhibit normal bacterial utilization of PABA
for the synthesis of folic acid, an important metabolite in DNA synthesis.
Synonyms:

Gantanol, Gantanol DS
Size Price
O
N
HO
HO
OH
N
OH
NH
2
O
H
2
N
S
N
H
O
N
O O
TelomeIase / DNA/RNA Ce||Cvc|e/C|ec|po|rl
25
S1186 BIBR1532
BIBR1532 is a selective telomerase inhibitor. This reagent inhibits the in vitro processivity of telomerase in a
dose-dependent manner, with IC50 of 93 nM. The selectivity of BIBR1532 was assessed in a panel of DNA
and RNA polymerases, showing that none of these enzymes was inhibited in concentrations up to 100 uM.
BIBR1532 has a direct cytotoxic effect on leukemia cells but not in normal hematopoietic stem cells.
Size Price
(E) N
H
O
COOH
10mg
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1g
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100mg
10mg
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Toll Free:(877)796-6397 www.selleckchem.com info@selleckchem.com
Phone:+1-832-582-8158
---USA and Canada only---
CHK (Checkpoint kinase,CSK-homologous kinase)
Dihydrofolate reductase

S1584 NSC 131463
NSC 131463 is a dihydrofolate reductase potent inhibitor with an IC50 of 1 nM. It is a minor metabolite of
methotrexate. It inhibited L1210 cell proliferation in culture (IC50 = 0.3 M), and prolonged the survival of
L1210 leukemic mice (98% increase in lifespan at 120 mg/kg, qdx9). The increased dose of mAPA-HCysA
required to inhibit tumor growth in vitro and in vivo relative to methotrexate may reflect the inability of this
compound to form non-effluxing polyglutamates.
Synonyms:

NSC 133723, Deoxyaminopteroic acid, DAMPA
Size Price
N
N N
N
H
2
N
NH
2
N
O
OH
Ce||Cvc|e/C|ec|po|rl
Solutions to Signal Transduction Research
26
CHK / DihydroIolaIe reducIase

S1532 AZD7762
AZD7762 is a novel checkpoint kinase inhibitor with an IC50 of 5 and <10 nM for Chk1 and Chk2, respectively.
It significantly prolonged the median time required for tumor volume doubling in response to gemcitabine and
radiation. G2 checkpoint abrogation and homologous recombination repair inhibition both contribute to
sensitization by Chk1 inhibition. The clinical use of AZD7762 in combination with gemcitabine and radiation for
patients with locally advanced pancreatic cancer.
Size Price
F
S
NH
NH
2
O
HN
O
N
H
5mg
25mg
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10mg
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200mg
2/
HDAC
l|sloredeacelv|ase|l0AC)|r||o|loracl|val|orolp21
wAF1
|rvo|vesc|ardes|r
proroler-assoc|aledprole|rs,|rc|ud|rdl0AC1.
C.-Y. Gui, L. Ngo. PNAS, 2004,101(5):1241-1246
HDACs and histone acetyltransferases are the enzymes that determine, in
part, the pattern of histone acetylation. The pattern of acetylation of histones
as well as the pattern of methylation and phosphorylation of histones may
represent a code that is recognized by non-histone complexes involved in
the regulation of gene expression.
There are three classes of HDAC enzymes. Class I deacetylases include
HDACs 1, 2, 3, and 8, are related to yeast RPD3 deacetylase, and have
molecular masses of 2255 kDa. Class II deacetylases include HDACs 4, 5,
6, 7, 9, and 10, are related to yeast Hda1 deacetylase, and have molecular
masses of 120130 kDa. HDAC 11 contains conserved residues in the catalytic
core region shared by both class I and II enzymes. The third class of HDACs
are the nicotine adenine dinucleotide-dependent Sir 2 family of deacetylases,
which differ from class I and II HDACs in that they are not inhibited by TSA,
SAHA, or related compounds.
A number of chemically diverse agents have been discovered, including the
hydroxamic acids SAHA and TSA, which inhibit HDAC activity. Inhibiting
HDAC activity with SAHA and related agents alters gene expression, but,
contrary to what might be anticipated by the wide distribution of HDACs in
chromatin, there is not a global alteration in gene transcription. Furthermore,
alteration of the chromatin structure in the transcribed region of a gene has
been shown to be associated with induced expression of that gene by transcription
factor complexes containing RNA polymerase II.
28
S1030 LBH-589(Panobinostat)
Induction of TAp63 by histone deacetylase inhibitors.
Berna S. Sayana et al. Biochem Bioph Res Co, 2010(22):1748-1751
S1053 MS-275(Entinostat)
DNMT1 Stability Is Regulated by Proteins Coordinating Deubiquitination
and Acetylation-Driven Ubiquitination.
Zhanwen Du, Jing Song et al. Sci Signal, 2010;146(3):ra80
Histone Deacetylase Inhibitors Downregulate Checkpoint Kinase 1 Expression
to Induce Cell Death in Non-Small Cell Lung Cancer Cells
William Brazelle, Jenny M. Kreahling et al. PLoS One, 2010; 12(5):e14335.
S1047 Vorinostat(SAHA)
A Novel Xenograft Model of Cutaneous T-cell Lymphoma.
Krejsgaard T, Kopp K et al. Exp Dermatol, 2010; 19(12):1096-1102.
Itch/AIP4-independent proteasomal degradation of cFLIP induced by the histone
deacetylase inhibitor SAHA sensitizes breast tumour cells to TRAIL.
Rosario Yerbes et al. Invest New Drugs, 2010 Nov 25. [Epub ahead of print]
Papers
Using Selleck Products
HDAC (Histone deacetylases)
Belinostat is a novel hydroxamate-type inhibitor of HDAC activity. Belinostat inhibits HDAC
activity in HeLa cell extracts with an IC50 of 27 nM. PXD101 is cytotoxic in vitro in a number of
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induces apoptosis.
Synonyms:

PXD101, PX105684
Size Price S1085 Belinostat
S
N
H
N
H
O
OH
O O
Acetyl-H3
H3
0

M
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S1085 Belinostat
Produced Independently by our customer Dr.Zhang, Tianjin Medical University
:HVWHUQEORWDQDO\VLVRI+$FHW\O+0
Belinostat treated MDA-MB-231 breast denocarcinoma
cell line.
50mg
200mg
10mg
S1095 LAQ824
LAQ824 is a histone deacetylase inhibitor, inhibited in vitro enzymatic activities (IC50= 0.032uM) and
WUDQVFULSWLRQDOO\ DFWLYDWHG WKH S SURPRWHU LQ UHSRUWHU JHQH DVVD\V ,& 0 /$4 VHOHFWLYHO\
inhibited growth of cancer cell lines at submicromolar levels after 48-72 h of exposure, the calculated IC50s
ZHUH DQG 0 LQ + DQG +&7 FHOOV UHVSHFWLYHO\ ,Q DGGLWLRQ /$4 H[KLELWHG DQWLWXPRU
effects in a xenograft animal model.
Synonyms:

NVP-LAQ824, Dacinostat
Size Price
50mg
100mg
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100mg
5mg
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5mg
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10mg

S1030 LBH-589
A novel broad-spectrum HDAC inhibitor belongs to the hydroxamate class, in Philadelphia chromosomenegative
(Ph-) ALL. HDACs are regulating gene transcription, protein function, and stability. The IC50 value for
inhibition of proliferation in MOLT-4 cells is approximately 5 nM and for Reh cells is approximately 20
nM.Similar results were observed at 24 and 72 hours.
Synonyms:

Panobinostat, NVP-LBH589
Size Price

S1484 MC1568
MC1568 is a potent selective class II (IIa) histone deacetylas (HDAC II) inhibitor (IC50 of a maize deacetylase
HD2 at 22.0 M). MC1568 had no or a weak effect on the class I HDACs. MC1568 shows no inhibitory activity
against HDAC1 but was able to inhibit HDAC4.
Size Price

S1122 MGCD0103
MGCD0103, an orally available small molecule, binds to and inhibits Class 1 isoforms of HDAC, specifically
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tumor cells and so tumor cell death. In intact cells, MGCD0103 inhibited only a fraction of the total HDAC
activity and showed long-lasting inhibitory activity even upon drug removal. MGCD0103 induced
hyperacetylation of histones, selectively induced apoptosis, and caused cell cycle blockade in various human
cancer cell lines in a dose-dependent manner.
Synonyms:

Mocetinostat
Size Price
Acetyl-H3
H3
2
0

M
1
0

M
1

M
0
.
1

M
0
.
0
1

M
0

M
N
OH
H
N
HO
O
HN
N
H
HN
O
H
N
OH
F
O
N
H
N
O
OH
Data Provided by our customer Marianne Skeie Rdland,
University of Oslo/Oslo University Hospital
17AAG 50 nM 100 nM
Ac-tubulin
Tubulin
hours Ctr 8 8 16 24 8 16 24
LBH-589
O
H
N
N
H
N
N
N NH
2
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S1095 LAQ824
Produced Independently by our customer Dr.Zhang, Tianjin Medical University
:HVWHUQEORWDQDO\VLVRI+$FHW\O+0
LAQ824 treated MDA-MB-231 breast denocarcinoma
cell line.
Feed
S1095 LAQ824
Western blot analysis of Ac-tubulin and Tubulin.
Cell line was treated with 50 or 100 nM LBH-589
for 8, 16, 24 hours.
Feed
S1122 MGCD0103
Produced Independently by our customer Dr.Zhang, Tianjin Medical University
:HVWHUQEORWDQDO\VLVRI+$FHW\O+0
MGCD0103 treated MDA-MB-231 breast denocarcinoma
cell line.
Acetyl-H3
H3
2
0

M
1
0

M
1

M
0
.1

M
0
.0
1

M
0

M
H
3

HDAC l0AC
29
Toll Free:(877)796-6397 www.selleckchem.com info@selleckchem.com
Phone:+1-832-582-8158
---USA and Canada only---
2
0

M
1
0

M
1

M
0
.
1

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0
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0
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Droxinostat is a selective inhibitor of HDAC3, HDAC6, and 6and8. Droxinostat shows comparable inhibition of
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development and progression. This agent could sensitize malignant cells to death receptor ligands (Fas and
TRAIL).
Size Price

S2170 ITF2357
S1422 Droxinstat
ITF2357 is a HDAC inhibitor of the hydroxamate family, which inhibits both class I and class II HDAC. ITF2357
induces apoptosis of MM and AML cells and this apoptosis takes place following induction of p21 and
down-modulation of Bcl-2 and Mcl-1 proteins. When tested on normal cells, ITF2357 inhibits the production of
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IL-6 and VEGF by mesenchymal stromal cells.
Synonyms:

Givinostat, Gavinostat
Size Price

S1096 JNJ-26481585
JNJ-26481585 is an orally bioavailable, hydroxamic acid-based inhibitor of HDAC with potential antineoplastic
activity. HDAC inhibitor JNJ-26481585 inhibits HDAC leading to an accumulation of highly acetylated histones,
which may result in an induction of chromatin remodeling; inhibition of the transcription of tumor suppressor
genes; inhibition of tumor cell division; and the induction of tumor cell apoptosis.
Size Price
Cl
O
N
H
O
OH
N
+
O
H
N
O
H
N
OH
O
H
Cl
-
H
2
O
N
N
H
N
N
N
O
H
N
OH
Acetyl-H3
H3

0
C
o
n
t
r
o
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JNJ-26481585(M) 0 0.01 0. 1 1.0 10.0 20.0
Acetyl-H
3
H
3
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S1422 Droxinstat
Produced Independently by our customer Dr.Zhang, Tianjin Medical University
Western blot analysis of H3, Acetyl-H3. 0.01-10 0
Droxinstat treated MDA-MB-231 breast denocarcinoma
cell line.
Feed
S1096 JNJ-26481585
Produced Independently by our customer Dr.Zhang, Tianjin Medical University
Western blot analysis of H3, Acetyl-H3. 0-20 0
JNJ-26481585 treated MDA-MB-231 breast denocarcinoma cell line.
10mg
25mg
5mg
25mg
50mg
10mg
50mg
200mg
10mg
10mg
25mg
5mg
50mg
200mg
10mg
50mg
200mg
10mg

S2190 Pyroxamide
Pyroxamide is a potent HDAC inhibitor with an IC50 of 100 nM for HDAC-1. Despite the potent
growth-inhibitory effects of pyroxamide in this CWR22 prostate cancer xenografts model, serum
prostate-specific antigen levels in control versus pyroxamide-treated mice were not significantly different. It
causes the accumulation of acetylated core histones in MEL cells cultured with the agent.
Synonyms:

NSC 696085, NSC-696085
Size Price
S1053 MS-275
MS-275 is synthetic benzamide derivative with potential antineoplastic activity. This agent preferentially
inhibits HDAC1 (IC50=300 nM) over HDAC3 (IC50=8 M) and has no inhibitory activity towards HDAC8
(IC50>100 M). This agent appears to exert dose-dependent effects in human leukemia cells at low drug
concentrations in human prostate cancer cell lines.
Synonyms:

Entinostat, SNDX-275, MS-27-275
Size Price
NH
O
NH
2
H
N O
O
N

S1090 PCI-24781
PCI-24781 is a novel broad spectrum hydroxamic acid-based inhibitor of HDAC that shows antitumor activity
in vitro and in vivo and is under evaluation in phase I clinical trials. PCI-24781 inhibited pure recombinant
HDAC1 with a Ki of 0.007 Mmol/L, and also inhibited the other HDAC isozymes HDAC2, HDAC3/SMRT,
HDAC6, HDAC8, and HDAC10 in the nanomolar range.
Synonyms:

CRA-02478
Size Price
O
N
O
HN
O
O
NH
OH
Acetyl-H3
H3
2
0

M
1
0

M
1

M
0
.
1

M
0
.
0
1

M
0

M
N
H
N
N
H
OH
O
O
Feed
S1053 MS-275
Produced Independently by our customer Dr.Zhang, Tianjin Medical University
:HVWHUQEORWDQDO\VLVRI+$FHW\O+0
MS-275 treated MDA-MB-231 breast denocarcinoma
cell line.
l0AC
Solutions to Signal Transduction Research
30
HDAC

50mg
200mg
10mg
50mg
200mg
10mg
10mg
50mg
1mg
500mg
1g
100mg
Sir2-like Family Deacetylase
Data from Experimental
Dermatology 2010 using our
product.
S1168 Sodium valproate
Sodium valproate is a HDAC inhibitor with an IC50 of 0.4 mM and exhibits anticancer, anti-inflammatory and
neuroprotective effects. Sodium valproate can inhibit cell apoptosis. It displays anticonvulsive activity via an
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voltage-gated Na
+
channels and modulates firing of neurons. It enables induction of pluripotent stem cells from
somatic cells by Oct4 and Sox2.
Synonyms:

valproate Sodium, Depakene, Valproate, Valrelease
Size Price

S1045 Trichostatin A
Trichostain A is an antifungal antibiotic with cytostatic and differentiating properties in mammalian cell culture.
TSA inhibited proliferation of eight breast carcinoma cell lines with mean SD IC50 of 124.4 120.4 nm.
HDAC inhibitory activity of TSA was similar in all cell lines with mean SD IC50 of 2.4 0.5 nm, and TSA
treatment resulted in pronouncing histone H4 hyperacetylation.
Synonyms:

TSA
Size Price

S1047 Vorinostat
9RULQRVWDWHIILFLHQWO\VXSSUHVVHG0(66$FHOOJURZWKDWDORZGRVDJH0DOUHDG\DIWHUKRXUVWUHDWPHQW
Decrease of cell survival was even more pronounced after prolonged treatment and reached 9% and 2% after
DQG KRXUV RI WUHDWPHQW UHVSHFWLYHO\ &RORQ\ IRUPLQJ FDSDELOLW\ RI 0(66$ FHOOV WUHDWHG ZLWK 0
vorinostat for 24 and 48 hours was significantly diminished and blocked after 72 hours.
Synonyms:

Zolinza, MK-0683, SAHA
Size Price
ONa
O
N
N
H
O O
OH
H
N
O
N
H
O
OH

control SAHA 31nm
SAHA promotes C2C12
differentiationIn the images, the
red is the myotube indicating
differentiation,
the blue is the nuclei.
9RULQRVWDWLQKLELWVWKHWXPRUJURZWK12'6&,'%PPLFHZHUHLQMHFWHG
s.c. with 1 106 MyLa2059 cells into both flanks.When the mice had developed
established palpable tumors treatment was initiated (day 1). The mice received
HLWKHUYHKLFOHEODFNOLQHRUPJNJYRULQRVWDWJUH\OLQHLSILYHGD\VDZHHN
In total, there were four mice in the group receiving vehicle and three mice in
thegroup receiving vorinostat. The length and width of the tumors were measured
continuously until the experiment was terminated on day 20 post treatment initiation.
Feed
S1045 Trichostatin A
Produced Independently by our customer Dr.Zhang, Tianjin Medical University
:HVWHUQEORWDQDO\VLVRI+$FHW\O+0
Trichostatin A treated MDA-MB-231 breast denocarcinoma cell line.
Feed
S1047 Vorinostat
500mg
1g
100mg

S1541 EX 527
EX 527 is a potent and selective SIRT1 class III HDAC enzyme inhibitor with an IC50 of 38 nM. It is Selective
inhibitor of SIRT1 that does not class I/II inhibit HDAC or other sirtuin deacetylase family members (SIRT1,
SIRT2, SIRT3, HDAC and NADase respectively). It was thought to block the release of deacetylated peptide
and O-acetyl-ADP-ribose from the enzyme following the deacetylation process. Blocking of SIRT1 by EX 527
also demonstrated that deacetylation of the important tumor suppressor protein p53 is mediated by SIRT1 as
well.
Synonyms:

SEN0014196
Size Price
H
N
Cl
O
H
2
N


S1515 SB939
SB939 is a novel potent and orally active HDAC inhibitor with an IC50 of 52 nM for HDAC1 and a GI50 of 0.56
M for Colo205. Its IC50 for HCT-116 colon cancer cell line and HL-60 acute myeloid leukemia cell line is 0.48
0DQGQ0UHVSHFWLYHO\,QYLWUR6%LQKLELWVFODVV,,,DQG,9+'$&VZLWKQRHIIHFWVRQRWKHU]LQF
binding enzymes, and shows significant antiproliferative activity against a wide variety of tumor cell lines.
Size Price
N
N
N
H
O
HO
N
Acetyl-H3
H3

0
C
o
n
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S1194 CUDC-101 Page 4
Feed
S1515 SB939
Produced Independently by our customer Dr.Zhang, Tianjin Medical University
:HVWHUQEORWDQDO\VLVRI+$FHW\O+0
SB939 treated MDA-MB-231 breast denocarcinoma
cell line.
Acetyl-H3
H3
2
0

M
1
0

M
1

M
0
.
1

M
0
.
0
1

M
0

M
HDAC / Sir2-like Family DeaceIylase
l0AC
3l
Toll Free:(877)796-6397 www.selleckchem.com info@selleckchem.com
Phone:+1-832-582-8158
---USA and Canada only---
32
Apoptosis
Redu|al|orolCe||0eal|:T|eCa|c|ur-Apoplos|sL|r|.
Sten Orrenius et al.Nat Rev Mol Cell Bio, 2003(4):552-565
T|e8CL-2prole|rlar||v:oppos|rdacl|v|l|esl|alred|alece||deal|.
Richard J. Youle et al. Nat Rev Mol Cell Bio, 2008(9):47-59
Fala|||a|sorsolp53W|l|8axard8a|.
Jean-Luc Perfettini et al. Nat Cell Bio, 2004;6(5):386-388.
3urv|v|rVodu|alesV|croluou|e0vrar|csardNuc|eal|orl|roud|oull|eCe||
Cvc|e.
Jack Rosa et al. MBoC, 2006(17):1483-1493.
Apoptosis is a genetically controlled and evolutionarily conserved form of
cell death that is of importance for normal embryonic development and for
the maintenance of tissue homeostasis in the adult organism. Apoptotic cell
death is triggered by extrinsic, receptor-mediated, or intrinsic, mitochondria-
mediated, signalling pathways that induce death-associated proteolytic
and/or nucleolytic activities.
All pathways to apoptosis converge on the activation of caspases, which are
cysteinyl aspartate proteases that coordinate the efficient dismantling and
engulfment of doomed cells. Two pathways of cell death can be distinguished
by whether they require BCL-2 family proteins and by which caspases are
crucial for their execution.
Survivin is a member of the inhibitor of apoptosis gene family. Although
survivin-like IAP molecules in model organisms seem to participate cytoki-
nesis, reduction or loss of survivin in mammalian cells has been associated
with panoply of cell division defects that include supernumerary centrosomes,
aberrant spindle assembly, mislocalization of mitotic kinases, loss of mitotic
checkpoint(s), and cytokinesis failure with appearance of multinucleated
cells.
p53 can induce apoptosis through its well defined role as a regulator of
transcription, but also by a less well defined transcription independent
mechanism. p53 mediates mitochondrial permeabilization through direct
physical interactions with the pro-apoptotic Bcl-2 family members, Bax and
Bak.
33
S1001 ABT-263(Navitoclax)
Diminished sensitivity of Chronic Lymphocytic Leukemia cells to ABT-737 and ABT-263 due to
albumin binding in blood.
Meike Vogler et al. Clin Cancer Res, 2010(16):4217
S1002 ABT-737
Prolyl hydroxylase 3 (PHD3) is essential for hypoxic regulation of neutrophilic inflammation in
humans and mice.
Sarah R. Walmsley et al. J Clin Invest, 2011; 121(3):1053-1063
The BH3-mimetic ABT-737 targets the apoptotic machinery in cholangiocarcinoma cell lines
resulting in synergistic interactions with zoledronic acid.
Antonello A. Romani et al. Cancer Chemother Pharmacol, 2011;67(3):557-567
ABT-737 Overcomes Resistance to Immunotoxin-Mediated Apoptosis and Enhances the Delivery
of Pseudomonas ExotoxinBased Proteins to the Cell Cytosol.
Roberta Traini et al. Mol Cancer Ther, 2010; 9(7):2007-2015
*O\FRJHQV\QWKDVHNLQDVHLQKLELWRUVVXSSUHVVOHXNHPLDFHOOJURZWK
Emma Y. Song et al. Exp Hematol, 2010; 38(10):908-921.e1
S 8SUHJXODWHG 0RGXODWRU RI$SRSWRVLV 380$$FWLYDWLRQ &RQWULEXWHV WR 3DQFUHDWLF &HOO
Apoptosis Induced by Proinflammatory Cytokines and Endoplasmic Reticulum Stress.
Esteban N. Gurzov et al. J Bio Chem, 2010; 285(26):19910-19920
Histone deacetylase inhibitors synergistically potentiate death receptor 4-mediated apoptotic cell
death of human T-cell acute lymphoblastic leukemia cells.
Eun-Sil Sung et al. Apoptosis, 2010; 15(10):1256-1269
Papers
Using Selleck Products
Bcl-2 (B-cell lymphoma 2)

S1002 ABT-737
ABT-737 is a pan-Bcl-2 inhibitor that has a wide range of single-agent activity against ALL cell lines and
xenografts. Increased expression of the Bcl-2 family of proteins in cancers has been associated with
chemotherapy resistance. The ABT-737 single-agent LC90 values ranged from 100 nM for COG-LL-319 and
RS4;11 cells to low micromolar concentrations for the other ALL cell lines.
Size Price

S1057 Obatoclax Mesylate
Specific apoptosis was induced at 250 nM obatoclax (16.04 %) and increased in a dose-dependent manner
up to the highest dose tested (10 M, 73.48 %). The average IC50 for the seven AML patient samples tested
was 3.59 M. Obatoclax has been reported to similarly antagonize all antiapoptotic Bcl-2 family proteins
(average IC50=3 M), including Mcl-1 (IC50=2.9 M) and Bfl-1 (IC50=5 M).
Synonyms:

GX15-070
Size Price

S1001 ABT-263
The oral bioavailability of ABT-263 in preclinical animal models is 20% to 50%, depending on formulation.A
wide range of SCLC cellular activity was observed with ABT-263 having aEC50 of 110 nmol/L against the most
VHQVLWLYHOLQH+ZKHUHDVLWVDFWLYLW\LQWKHOHDVWVHQVLWLYHOLQH+UHVXOWHGLQDQ(&DWPRO/,Q
DOOFHOOOLQHVZKHUHWKH(&ZDVPRO/
Synonyms:

Navitoclax
Size Price
Cl
N
N
N
H
O
S
O O
N
H
SPh
N
O S
F3C O
O
O
H
N
N
N
S
O O
NO2
H
N
S
N
Cl
N
H
N
O
HN
CH
3
SO
3
H
(EC50 64.9 nM)
80
100
ABT-263
20
40
60
%

P
S
+
c
e
l
l
s
0
0 1 3 10 30 100 300 1000
(nM)
Produced Independently by our customer
Dr.Zhang,Tianjin Medical University.
Data Provided by our customer Prof. Angelo F, Borghetti
of Universita degli Studi di Parma
0'%0$FHOOVZHUHH[SRVHGWR0
cisplatin in the absence or in the presence
of 100nM Obatoclax Mesylate. The cell were
stained with Hoechst 33342 , MitoTracker
Red and yo-pro-1.
Cells were exposed to ABT-737 at a concentration
ranging from 1 to 50 lM. Following 72 h of incubation,
growth inhibition was analyzed by crystal violet assay.
Doseeffect plot of ABT-737 treatment is presented.
Lower panel detection of PARP-1, cleaved caspase-9
and caspase-3, BCL-2 and MCL-1 in TFK-1 and EGI-1
cells after 72 h of ABT-737 treatment (1, 3, 10, 25,50
lM). Cell lysates were analyzed on Western blotting.
Produced Independently by our customer
Dr.Zhang, Tianjin Medical University.
0'%0$FHOOVZHUHH[SRVHGWR0
cisplatin in the absence or in the presence
of 100nM ABT737. The cell were stained
with Hoechst 33342 , MitoTracker Red
and yo-pro-1.
Data provided by our customer Dr Christine Hawkins,
c/o Biochemistry Department OfficeLa Trobe University
CLL cells freshly isolated from peripheral blood of CLL patients
were incubated in RPMI + 10% FCS with different concentrations
of ABT-737 or ABT-263 for 4 h before apoptosis was assessed by
externalization of phosphatidylserine (PS) and staining with
AnnexinV-FITC (n=21, *=P<0.05).
Data from AACR. July 2 2010 using our product.
S1001 ABT-263
Feed
S1002 ABT-737
Feed
S1057 Obatoclax Mesylate
Feed
MEF cells were treated for 24 hrs with the Bcl-2
antagonists Obatoclax mesylate at the indicated
doses. Acute survival was monitored by propidium
iodide uptake assays (red lines). Long term survival
(red lines) was measured by replacing the
drug-containing media with normal media and
incubating the cells until visible colonies formed.
Clonogenic survival is expressed relative to the
numbers of colonies formed following 24 hr incubation
in normal media (lacking drugs).
S1121 TW-37 Size Price
S
O
O
N
H
O
HO
OH
OH
TW-37 binds to the BH3 binding groove in Bcl-2 protein competing with BH3 peptides derived from Bid, Bim,
and Bad proteins. TW-37 binds to Bcl-2 with a K(i) value of 290 nM and also to Bcl-xL and Mcl-1 with high
affinities. TW-37 potently inhibits cell growth in PC-3 prostate cancer cells with an IC50 value of 200 nM and
effectively induces apoptosis in a dose-dependent manner.
Data provided by our customer Dr Christine Hawkins,c/o Biochemistry Department Office
La Trobe University
MEF cells were treated for 24 hrs with the Bcl-2 antagonists TW-37 at the indicated
doses. Acute survival was monitored by propidium iodide uptake assays (red lines).
Long term survival (red lines) was measured by replacing the drug-containing media
with normal media and incubating the cells until visible colonies formed. Clonogenic
survival is expressed relative to the numbers of colonies formed following 24 hr
incubation in normal media (lacking drugs).
S1123 TW-37
Feed
Apoplos|s
Solutions to Signal Transduction Research
34
Bcl-2
10mg
25mg
5mg
10mg
50mg
5mg
20mg
200mg
10mg
10mg
25mg
5mg
p53 (protein 53)
S1172 JNJ 26854165
JNJ-26854165 is an orally bioavailable, small-molecule HDM2 antagonist with potential antineoplastic activity.
This agent inhibits the binding of the HDM2p53 complex to the proteasome, blocking the degradation of p53.
In addition to p53, degradation of other HDM2 client proteins may be inhibited. HDM2, a zinc finger protein, is
a negative regulator of the p53 pathway; often overexpressed in cancer cells, this oncoprotein has been
implicated in cancer cell proliferation and survival.
Synonyms:

Serdemetan
Size Price
NH
H
N
HN
N
71)7XPRUQHFURVLVIDFWRUDOSKD

S1567 Pomalidomide
3RPDOLGRPLGHLV71)LQKLELWRUDQGDQHZLPPXQRPRGXODWRUZLWKDQ,&RI0,WKHOSVWRUHVWULFWWXPRUV
necessary blood vessel growth. Compared to thalidomide, pomalidomide has demonstrated enhanced
immunological effects in lab testing, including an approximately 500-2,000 times greater potency at stimulating
the proliferation of T-cells. Pomalidomide appears to function through multiple pathways to inhibit myeloma
FHOOVJURZWKDQGVXUYLYDO
Synonyms:

CC-4047, Actimid
Size Price
S1029 Lenalidomide
/HQDOLGRPLGHLVDGHULYDWLYHRIWKDOLGRPLGHZLWKDQWLDQJLRJHQLFDQGDQWLQHRSODVWLFSURSHUWLHVFHOO,&
M). It was initially intended as a treatment for multiple myeloma. Lenalidomide inhibits TNF-alpha production,
stimulates T cells, reduces serum levels of the cytokines VEGF and bFGF, and inhibits angiogenesis. This
agent also promotes G1 cell cycle arrest and apoptosis of malignant cells.
Synonyms:

CC-5013, Revlimid
Size Price
N
NH
2
O
NH
O
O
N
NH
2
O
O
NH
O
O
006ZHUHWUHDWHGZLWK$70OHQDOLGRPLGH0RU
combined therapy for 72 hours. Annexin/PI staining show increased
apoptosis associated with caspase 8 and PARP cleavage after 18
and 36 hours of exposure. B) MM.1S cells were treated with AT9283
0OHQDOLGRPLGH0RUFRPELQHGWKHUDS\IRUKRXUV
Whole lysates were immunoblotted with indicated antibodies
Data from our customer DANA-FARBER CANCER INSTITUTE
using our product.
B A
S1029 Lenalidomide
Feed
Survivin
50mg
200mg
10mg

S1130 YM155
YM155, a novel small molecule survivin inhibitor, suppressed expression of survivin and induced apoptosis in
PC-3 and PPC-1 human HRPC cell lines at 10nmol/L. Pharmacokinetic analyses indicated that YM155 is
highly distributed to tumors and at concentrations f20-fold higher than those in plasma.
Size Price
N
N
O
O
N
N
O
Br
94
YIl55
9l
0.9% Nacl
92
0.9% Nacl
Total RNA from livers of these mice were isolated from tissues
using TRIZOL (Invitrogen). cDNA synthesis was performed with
the M-MLV RTase cDNA Synthesis Kit.qRT-PCR reactions were
performed using SYBR Greenon ABI 7500 Fast system. Expression
levels of Survivin gene were measured by qRT-PCR in livers injected
with 0.9% NaCl or YM155 48 hours after DEN treatment.
Data from our customer Lihua Min , Chinese Academy of Sciences
S1130 YM155
Feed
Apoplos|s
35
50mg
200mg
10mg
50mg
200mg
10mg
25mg
100mg
5mg
TNF- / p53 / Survivin
Toll Free:(877)796-6397 www.selleckchem.com info@selleckchem.com
Phone:+1-832-582-8158
---USA and Canada only---
36
PARP
Po|v|A0P-r|oose)po|vrerase|r||o|lorsaspror|s|rdcarcerl|erapeul|cs.
Jin-xue He et al. Acta Pharmacol Sin, 2010(31):11721180.
The members in the PARP superfamily related to the activity of DNA mainly
include PARP1, PARP2, Tank1, and Tank2. PARP1 accounts for at least
80% of total cellular PARP activity, and together with its nearest relative
PARP2, constitutes the DNA-damage-dependent PARPs. PARP1 poly(ADP-
ribosyl)ates various nuclear proteins including histones H1 and H2B,
XRCC1, CENP-A, CENP-B, BUB3, and itself, whereas PARP2 adds PAR to
XRCC1, CENP-A, CENP-B, BUB3, and itself. Most of those proteins are
involved in the activities of DNA and centrosomes, especially in DNA-damage
repair, specifically the base excision repair. Once one strand of DNA breaks,
PARP1/2 bind to the nicked site, which activates their own enzymatic activity,
causing the poly(ADP-ribosyl)ation of PARP1/2 and other nuclear proteins
including histones and XRCC1 at the expense of NAD+. Consequently,
'1$SRO\PHUDVHDQGWKHOLJDVH,,,;5&&FRPSOH[DUHUHFUXLWHGWRWKH
poly(ADPribosyl) ated PARP1/2 to repair the SSB.
Since 2005, the rapid development of PARP inhibitors for cancer therapy
has brought at least 7 PARP inhibitors into clinical anticancer investigations,
and 2 of them have entered phase III clinical trials for cancer therapy. The
encouraging results from those clinical studies further reveal a promising
future of targeting PARP as an anticancer strategy.
3/
S1004 ABT-888(Veliparib)
ABC transporters in the blood-brain barrier limit the brain penetration of the PARP inhibitor
ABT-888
Lin Fan et al. AACR 2010.
S1098 AG-014699(PF-01367338)
Embryonic lethal phenotype reveals a function of TDG in maintaining epigenetic stability.
Daniel Cortazar et al. Nature, 2011(470):419423
S1060 AZD2281(Olaparib)
MSH3 Mediates Sensitization of Colorectal Cancer Cells to Cisplatin, Oxaliplatin, and a
Poly(ADP-ribose) Polymerase Inhibitor.
Masanobu Takahashi et al. J Bio Chem, 2011(286):12157-12165
S1087 BSI-201
Tumor necrosis factor-like weak inducer of apoptosis and fibroblast growth factor-inducible
14 mediate cerebral ischemia-induced poly(ADP-ribose) polymerase-1 activation and neuro-
nal death.
Haile WB et al. Neuroscience, 2010; 171(4):1256-1264.
Papers
Using Selleck Products
PARP (Poly (ADP-ribose) polymerase)
S2178 AG14361
AG14361 is a potent PARP-1 inhibitor with a GI50 of 10.9 M. It caused a >3-fold sensitization of PARP-1+/+
FHOOVWRWRSRWHFDQFRPSDUHGZLWKDIROGVHQVLWL]DWLRQLQ3$53FHOOV,Q.FHOOV$*FDXVHG
a 2-fold sensitization to camptothecin-induced cytotoxicity. AG14361 did not affect the cellular activity of topo
I as determined by measurement of cleavable complexes and topo I relaxation activity, showing that
sensitization was not due to topo I activation.
Size Price
N
HN
N
O
N
S2197 A-966492
A-966492 is a highly potent and efficacious PARP inhibitor with a Ki and EC50 of 1 nM. In addition, it is orally
bioavailable across multiple species, crosses the blood-brain barrier, and appears to distribute into tumor
tissue. It also demonstrated good in vivo efficacy in a B16F10 subcutaneous murine melanoma model in
combination with temozolomide and in an MX-1 breast cancer xenograft model both as a single agent and in
combination with carboplatin.
Size Price
H
2
N O
N
H
N
F
N
H

S1004 ABT-888
ABT-888 is a potent inhibitor of both PARP-1 and PARP-2 by [3H]NAD
+
with Kis of 5.2 and 2.9 nmol/L,
respectively. The compound has good oral bioavailability and crosses the blood-brain barrier. ABT-888
strongly potentiated temozolomide in the B16F10 s.c. murine melanoma model. In the MX-1 breast xenograft
model, ABT-888 potentiated cisplatin, carboplatin, and cyclophosphamide, causing regression of established
tumors, whereas with comparable doses of cytotoxic agents alone, only modest tumor inhibition was exhibited.
Synonyms:

Veliparib
Size Price
Data from our customer Dr David
Schrmann, University of Basel
switzerland
D-XRCC1 D-PAR DAPI/DNA
* * * * control
no
1 nM
10 nM
100 nM
1 M
Data from our customer Dr Steve Reuland,UC Denver,
AMC,usa
451 Lu cells, 120 h treatment
0
20
40
60
80
100
120
0 50 100 150 200 250 300 350 400
[Temozolomide, M]
%
r
e
la
t
iv
e
v
ia
b
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c
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Vehicle
25 M
ABT-888
H
2
N O
N
H
N
N
H

S1098 AG-014699
AG-014699 is a PARP inhibitor (Ki, 1.4 nmol/L) with outstanding in vivo chemosensitization potency, which is
greater chemosensitization of temozolomide at a dose of 1 mg/kg. AG-014699 is a tricyclic indole PARP
inhibitor with potential antineoplastic activity. It blocks base excision repair mediated by PARP 1 on single
strand breaks and may be particularly efficacious in inducing apoptosis in breast cancer associated gene-1
and -2 (BRCA1/2) deficient tumor cells.
Synonyms:

AG-14447, AG-014447, AG-14699, PF-01367338
Size Price

HN
NH
F
H
N
O
P
OH
OH
O
HO
Data from our customer Dr David SchrmannUniversity of Baselswitzerland
D-XRCC1 D-PAR DAPI/DNA
* * * * control
no
1 nM
10 nM
100 nM
1 M
Caption: 451 Lu is a melanoma cell line with high PARP
expression that is resistant to temozolomide. Treatment
with 25 M ABT-888 greatly increased sensitivity to
temozolomide compared to cells without ABT-888
treatment as measured by MTS assay.
\l"
Fluorometric analysis result of
3$5VLJQDO0$%7
was added.
S1004 ABT-888
Feed
S1098 AG-014699
Feed
)OXRURPHWULFDQDO\VLVUHVXOWRI3$5VLJQDO0$*
was added.
25mg
100mg
5mg

S1060 AZD2281
PARP is anenzyme that is involved in a specific kind of DNA repair called base-excision repair, which is used
ZKHQ WKHUH LV DQ HUURU LQ D VWUDQG RI WKH '1$ ,& RI $=' 0 3$53 3$53
PF50=25.8. AZD2281(Olaparib) at 400 mg twice daily is well tolerated and highly active. The toxicity that was
seen in BRCA1/BRCA2 carriers was similar to the previously reported toxicity in noncarriers.
Synonyms:

Olaparib, KU-0059436, KU0059436
Size Price
NH
N
O
N
O
F
N O
Data from our customer Dr Meng Xiangbing, The University of Iowa.
Effect of AZD 2281 on the viability of endometrial cancer cell line Hec50
and Ishikawa and ovarian cancer cell line SKOV3,Caov3 and PA-1
was detected by WST-1 method after 3 days treatment.
S1060 AZD2281
Feed
PARP
Solutions to Signal Transduction Research
38
PARP
10mg
25mg
5mg
10mg
50mg
5mg
25mg
50mg
10mg
50mg
200mg
10mg

50mg
200mg
10mg

S1087 BSI-201
BSI-201 is a small molecule believed to achieve its anti-neoplastic effect by covalently binding and inhibiting
PARP-1. BSI-201 is active against a broad range of cancer cells in culture, including drug resistant cell lines.
BSI-201 has shown a strong safety profile and no significant toxicities attributable to drug in studies of more
than 200 patients treated to date with monotherapy, as well as in combination with chemotherapeutic
regimens.
Synonyms:

Iniparib, NSC-746045, IND-71677
Size Price
H
2
N O
I
NO
2
Data from Neuroscience 171 (2010) 12561264 using our product.
The interaction between TWEAK and Fn14 induces PARP-1 cleavage and
accumulation of Poly(ADP-ribose) polymers in vitro and in vivo.(AC)
Representative Western blot analysis and quantification of the mean intensity
of the band of total PARP-1(E) and caspase 3 activation (F) in Wt neurons
incubated with TWEAK either alone or in combination with the PARP-1
inhibitor BSI-201. * P<0.05 compared to cells co-treated with BSI-201.
10mg
25mg
50mg

S1132 INO-1001
INO-1001 is an isoindolinone derivative and potent inhibitor of the nuclear enzyme PARP with
chemosensitization and radiosensitization properties. INO-1001 inhibits PARP, which may result in inhibition
of tumor cell DNA repair mechanisms and, so, tumor cell resistance to chemotherapy and radiation therapy.
INO-1001 improves the recovery of myocardial and endothelial function after hypothermic cardiac arrest and
reduces pulmonary injury associated.
Size Price

NH
2
O
NH
2
S1087 BSI-201
Feed
PARP PARP
39
Toll Free:(877)796-6397 www.selleckchem.com info@selleckchem.com
Phone:+1-832-582-8158
---USA and Canada only---
40
Aurora Kinase/ksp
lderl|l|cal|orolderesl|alcorlerlurorce||res|slarcelol|eAurora8||rase
|r||o|lor,AZ01152.
J Guo et al. Pharmacogenomics J, 2009(9): 90102.
Ap|asellr|a|ol|sp|res|o,a||res|rsp|rd|eprole|r|r||o|lor,W|l|docelaxe||r
pal|erlsW|l|advarcedso||dlurours.
S P Blagden, L R Molife et al. Br J Canc, 2008(98):894899.
The Aurora kinase family is a collection of serine/threonine kinases that
functions as key regulators of cell division. Three Aurora kinases (known as
Aurora A, Aurora B and Aurora C) are expressed in mammalian cells, each
carrying out a distinct biological function. Aurora A localizes to spindle poles
and has a crucial role in bipolar spindle formation. Aurora B, a chromosome
passenger protein, localizes to centromeres in early mitosis and then the
spindle midzone in anaphase, and is required for mitotic histone H3 phosphory-
lation, chromosome biorientation, the spindle assembly checkpoint and
cytokinesis. Aurora C is also a chromosomal passenger protein and, in
normal cells, its expression is restricted to the testis where it functions
primarily in male gametogenesis. As the Aurora kinases serve essential
functions in mitosis, considerable attention has been given to targeting this
family of kinases for cancer therapy. Several small-molecule inhibitors have
been developed including Hesperadin, ZM447439, VX-680/MK0457,
AZD1152 and MLN8054.
Kinesin spindle protein (KSP) provides the propulsive forces required to
separate centrosomes during prophase, enabling them to migrate to opposite
poles and establish a functional bipolar spindle. Ksp is greatly expressed in
proliferating over non-proliferating cells and in tumour tissue relative to
normal tissue. In in vitro experiments, cells treated with the prototype KSP
inhibitor, monastrol, displayed abnormal, monopolar spindles with chromosomes
attached via microtubules to a single pole, resulting in deranged cell division,
mitotic cell cycle arrest and apoptosis.
4l
S1147 AZD1152-HQPA(Barasertib)
System-Level Analysis of Neuroblastoma TumorInitiating Cells Implicates AURKB as a
Novel Drug Target for Neuroblastoma.
Olena Morozova et al. Clin Cancer Res, 2010(16):4572
S1133 MLN8237
Drug-Resistant Aurora A Mutants for Cellular Target Validation of the Small Molecule Kinase
Inhibitors MLN8054 and MLN8237.
Dominic A. Sloane et al. ACS Chem Biol, 2010; 5(6):563576
Emerging drugs for high-grade osteosarcoma.
Hattinger CM et al. Expert Opin Emerg Drugs, 2010;15(4):615-34
Uncovering new substrates for Aurora A kinase.
Teresa Sardon et al. EMBO reports, 2010(11):977-984
S1048 VX-680(Tozasertib)
Activity of the Aurora Kinase Inhibitor VX-680 against Bcr/Abl-Positive Acute Lymphoblastic
Leukemias.
Fei F et al. Mol Cancer Ther, 2010;9(5):1318-1327
Papers
Using Selleck Products
Aurora Kinases

S1103 ZM-447439
ZM447439 dose-dependently inhibited proliferation of all three cell lines (BON, QGP-1 and MIP-101) with IC50
values in the nanomolar to low micromolar range. Moreover, aurora kinase inhibition by ZM447439 potently
induced apoptosis, which was accompanied by DNA fragmentation and caspase 3 and 7 activation.
Size Price
O N
O
O
N
N
NH
HN
O

S1147 AZD1152-HQPA
AZD1152 is a dihydrogen phosphate prodrug of a pyrazoloquinazoline Aurora kinase inhibitor and is converted
rapidly to the active AZD1152-HQPA in plasma. AZD1152-HQPA is a highly potent and selective inhibitor of
Aurora B (Ki, 0.36 nM) compared with Aurora A (Ki, 1,369 nM) and has a high specificity versus a panel of 50
other kinases. Consistent with inhibition of Aurora B kinase, addition of AZD1152-HQPA to tumor cells in vitro
induces chromosome misalignment, prevents cell division, and consequently reduces cell viability and induces
apoptosis.
Synonyms:

Barasertib
Size Price

S1519 CCT129202
&&7LVD$XURUDNLQDVHLQKLELWRUZLWK,&RIDQGPRO/
for Aurora A, Aurora B, and Aurora C, respectively. It showed high selectivity for the Aurora kinases over a
panel of other kinases tested and inhibits proliferation. The results showed that the CCT129202 is an
ATP-competitive inhibitor of recombinant Aurora A kinase with a Ki of 49.8 nmol/L.
1
0
M
1
M
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.
1
M
0
.
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M
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.
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1
M
C
o
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Aurora A
P-Aurora A/B/C
Histone H3
P-Histone H3
ZM447439
Size Price
S1451 Aurora A Inhibitor
Aurora A Inhibitor LVDVHOHFWLYH$XURUD$LQKLELWRU$XURUD$,&DW0$XURUD%,&DW0
(B / A ratio=1000). Aurora A Inhibitor I belongs a class of 2,4-dianilinopyrimidine inhibitors. Its selectivity for
Aurora A is 1000 folds over Aurora B, both in enzymatic assays and in cellular phenotypic assays. Thr217 of
Aurora A is the critical residue as a gating binding to this agent, which is responsible for the enhanced
selectivity over Aurora B.
Size Price
N N
N
H
F
N
H
O
Cl
NH
N
O
N
N
N
HN
HN
N
NH
O
O N
HO
F
N
N
H
N
Cl
N
N
N
N
H
O
S
N
Data from Clinical Cancer Research. July 22, 2010 using our product.
Neuroblastoma TICs are sensitive to Aurora B kinase inhibition. A. Western 6 blot analysis confirmed the presence of AURKB
protein in NB TICs but not SKPs. B&C.7 shRNA knockdown of AURKB reduces the proliferation of NB TICs. Growth curves of 8
NB TICs infected with shRNA against AURKB or controls are shown in B, qRT PCR 9 was used to determine the effectiveness of
AURKB knockdown (76-86%) D. The 10 alamarBlue assay revealed that AURKB inhibition with AZD1152 was effective in NB 11
7,&VDW(&RI0ZKHUHDV$85.%LQKLELWLRQZDVHIIHFWLYHLQ6.3VDW0
S1147 AZD1152-HQPA
Feed
Feed
S1103 ZM-447439
Produced Independently by our customer Dr.Zhang, Tianjin Medical University
Western blot analysis of Aurora A, p-Aurora A/B/C, Histone H3 and p-Histone H3.
0=0ZDVDGGHG
S1181 ENMD-2076
ENMD-2076 is an Aurora A/angiogenic kinase inhibitor with potent activity against Aurora A and multiple
tyrosine kinases linked to cancer and inflammatory diseases. ENMD-2076 is relatively selective for the Aurora
A isoform in comparison to Aurora B. ENMD-2076 has demonstrated significant, dose-dependent preclinical
activity as a single agent, including tumor regression, in multiple xenograft models.
Size Price
N
N
HN
N
N
NH
N
Data from our customer Antonino Maria Spart,
Centre for Integrative Biology (CIBIO) University of Trento
ENMD-2076 has been tested it on two different neuroblastoma
cell lines (SK-N-BE(2) and CHP-134) being calculated the IC50
by a WST-1 (Roche) proliferation assay, as shown in the table below.
Its in vitro activity is in the micromolar range and has a comparable
effect on both lines. VX-680 was used as standard, and it proved more
potent on CHP-134 cells.

Histone H3
p-Histone H3
Aurora A
p-Aurora
A/B/C
0

M
1
0

M
0
.0
0
1

M
0
.0
1

M
0
.1

M
1

M
IC50(M)
ENMD-2076 4.48 6.64
vx-680 7.01 0.9
SK-N-BE(2) CHP-134
Feed
S1181 ENMD-2076
Produced Independently by our customer Dr.Zhang,
Tianjin Medical University
Western blot analysis of Aurora A, p-Aurora A/B/C,
+LVWRQH+DQGS+LVWRQH+0(10'
was added.
Solutions to Signal Transduction Research
42
Aurora/Ksp Aurora Kinase
50mg
200mg
10mg
10mg
50mg
5mg
50mg
200mg
10mg
25mg
50mg
10mg
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200mg
10mg

S1454 PHA-680632
PHA-680632 is the first representative of a new class of Aurora inhibitors (Aurora A/B/C IC50 at 27, 135 and
120 nM, respectively). PHA-680632 is active on a wide range of cancer cell lines and shows significant tumor
growth inhibition in different animal tumor models at well-tolerated doses. The IC50 of PHA-680632 for cell
anti-proliferation ranged from 0.11 M to 5.6 M.
Size Price

S1154 SNS-314 Mesylate
SNS-314 Mesylate is an ATP-competitive, potent and selective inhibitor of Aurora kinases A (IC50=9.0nM), B
(IC50=31nM), and C (IC50=3.4nM). Histone H3 phosphorylation was potently inhibited by SNS-314 in all 6 cell
lines. SNS-314 Mesylate represents a new class of highly potent Aurora kinase inhibitors and is being
evaluated in a phase-1 dose escalation study designed to assess safety and tolerability in patients with
advanced solid malignancies.
Size Price
N N
O
HN
NH
N
N
O
HN
N
N
S
HN S
N
NH
NH
O
Cl
S
O
O
OH
Histone H3
p-Histone H3
Aurora A
p-Aurora
A/B/C
0

M
1
0

M
0
.0
0
1

M
0
.0
1

M
0
.1

M
1

M
SNS-314
Produced Independently by our customer Dr.Zhang,
Tianjin Medical University
Western blot analysis of Aurora A, p-Aurora A/B/C,
+LVWRQH+DQGS+LVWRQH+06160HV\ODWH
was added.
S1154 SNS-314 Mesylate
Feed

S1100 MLN8054
MLN8054 is an orally bioavailable, highly selective small molecule inhibitor of the Aurora A kinase with
potential antineoplastic activity. MLN8054 inhibits recombinant Aurora A kinase activity in vitro and is selective
IRU$XURUD$,&0RYHUWKHIDPLO\PHPEHU$XURUD%,&0LQFXOWXUHGFHOOV0/1
treatment results in G2/M accumulation and spindle defects and inhibits proliferation in cultured human tumor
FHOOVOLQHV,&0
Size Price

S1133 MLN8237
MLN8237 is a second-generation, orally bioavailable, highly selective small molecule inhibitor of the Aurora A
kinase. MLN8237 binds to and inhibits After treatment in eight multiple myeloma cell lines with MLN8237
00IRUKWKHDIIHFWRI$XURUD$NLQDVHHIIHFWRQERWKYLDELOLW\DQGSUROLIHUDWLRQ0
was examined. Tumor burden was significantly reduced and overall survival was significantly increased in
animals treated with 30mg/kg MLN8237.
Size Price
S1529 Hesperadin
Hesperadin is a human Aurora B inhibitor with an IC50 of 40 nM for the prevention of the phosphorylation of
substrate. Growth of cultured bloodstream forms was also sensitive to Hesperadin with an IC50 of 50 nM. It
blocked nuclear division and cytokinesis, but not other aspects of the cell cycle. Hesperadin also causes cells
arrested by taxol or monastrol to enter anaphase within <1 h, whereas cells in nocodazole stay arrested for 3-5
h.
Size Price
N
H
O
H
N
S
O
O
NH
N
O
F
N
N
N
Cl
HN
O
OH
O
N Cl
F
F
N
N
HN
O
OH
Inhibition of Aurora A (12.5 nM) by MLN8054 or MLN8237 was assessed in
GXSOLFDWHUDGLRPHWULFDVVD\VFRQWDLQLQJ@0>3@$73DQGTXDQWLILHG
by p81 phosphocellulose assay and scintillation counting. Kinase activity is
reported as a percentage of control calculated from duplicate incubations
containing 2.5% (v/v)DMSO.
Data from ACS Chem. Biol., 2010, 5 (6) using our product.
S1133 MLN8237
Feed
Aurora Kinase Aurora/Ksp
43
50mg
200mg
10mg
50mg
200mg
10mg
10mg
50mg
5mg
50mg
200mg
10mg
50mg
200mg
10mg
Toll Free:(877)796-6397 www.selleckchem.com info@selleckchem.com
Phone:+1-832-582-8158
---USA and Canada only---

S1048 VX-680
VX-680 is the inhibitor of Aurora-A,-B,-C kinases with apparent inhibition constant values of 0.6,18,4.6 nM
respectively.VX-680 caused accumulation of cells with 4N DNA content and potently inhibited the proliferation
of a wide variety of tumor cell types with IC50 values ranging from 15 to 113 nM.VX-680 had no effect on the
viability of noncycling primary human cells at concentrations as high as 10uM.
Synonyms:

MK-0457, Tozasertib
Size Price
N
N
H
N S
N
N
N
H
N
NH
O
Data published in Mol Cancer Thel;9(5) 1318-1327 using our product.
Data published in Mol Cancer Thel;9(5) 1318-1327 using our producht.
Synonyms:
ZM 252868, AG 1517, Tyrphostin AG 1517 S1134 AT9283 Page 11
Synonyms:
ZM 252868, AG 1517, Tyrphostin AG 1517 S1171 CYC116 Page 7
Synonyms:
ZM 252868, AG 1517, Tyrphostin AG 1517 S1249 JNJ-7706621 Page 21
Synonyms:
ZM 252868, AG 1517, Tyrphostin AG 1517 S2158 KW 2449 Page 15
Synonyms:
ZM 252868, AG 1517, Tyrphostin AG 1517 S1107 PHA-739358 Page 11
Synonyms:

Danusertib
VX-680 and dasatinib synergize to induce cytotoxic activity in wild-type Bcr/Abl-positive human ALL cells. A, TXL2 and UCSF02 cells were exposed
WRPRO/9;ZLWKRUZLWKRXWQPRO/GDVDWLQLEIRUWRKRXUVDVLQGLFDWHGDIWHUZKLFKWKHSHUFHQWDJHRIYLDEOHFHOOVZDVGHWHUPLQHGE\WU\SDQ
blue exclusion. B, TXL2 cells were treated with or without VX-680 and dasatinib for 48 hours in triplicate. **, P < 0.001, VX-680 and dasatinib cotreated
TXL2 compared with VX-680treated or dasatinib alonetreated TXL2 cells. Apoptotic cells were defined by flow cytometry as Annexin V and propidium iodide
(PI) double-positive cells. C, TXL2 cells were exposed to VX-680 and/or dasatinib and cell cycle distribution was assessed by flow cytometry.
5HVSRQVHVRIKXPDQ$//FHOOVWRVKRUWWHUP9;WUHDWPHQW$%/4FHOOVZHUHWUHDWHGZLWKPRO/9;IRUGD\V$IWHUGD\VWKHGUXJZDV
removed from the medium and cells were cultured without VX-680. During this period (days 321) without drug, viability (top left), cell numbers (bottom left),
and cell cycle distribution (right) of BLQ1 cells were assessed. B, BLQ1 and BLQ1-VX-Tx cells were cytospun onto glass slides and fixed, dried, and stained
ZLWK:ULJKW*LHPVDRQGD\$OOLPDJHVDUHDWPDJQLILFDWLRQ&%/4DQG%/49;7[FHOOVZHUHWUHDWHGZLWKPRO/9;RUQPRO/YLQFULVWLQH
for 72 hours. Cell viability was measured by trypan blue exclusion. *, P < 0.05, vincristine-treated BLQ1 compared with vincristine-treated BLQ1-VX-Tx.
S1048 VX-680
Feed
Ksp (Kinesin spindle protein)

S1452 Ispinesib
Ispinesib mesilate is an agent which inhibits the mitotic kinesin KSP with a Ki of 0.6 nM and has cytotoxic
activity at less than 10 nM in a spectrum of tumor cell lines. Ispinesib mesilate is a potent inhibitor of kinesin
spindle protein. In vivo, Ispinesib mesilate enhanced the antitumor activity of trastuzumab, lapatinib,
doxorubicin, and capecitabine and exhibited activity comparable with paclitaxel and ixabepilone.
Synonyms:

SB-715992, CK0238273
Size Price

S2182 SB 743921
SB743921 is a second generation, highly potent and active KSP inhibitor with a Ki of 0.1 nM for KSP (Eg5). It
is 5-fold more potent against the ATPase activity of KSP than ispinesib. It has cytotoxic activity at less than 2
nM is a spectrum of tumor cell lines. It is negative in a mouse model of peripheral neuropathy in which
paclitaxel is positive.
Size Price
Cl N
N
O
N
H
NH2
O
O
O
N NH2 O
Cl
HCl
Solutions to Signal Transduction Research
44
100mg
300mg
25mg
50mg
200mg
10mg
50mg
200mg
10mg
Aurora/Ksp Aurora Kinase / Ksp
45
MAPK
Pharmacological inhibitors of MAPK pathways.
Jessie M. English, Melanie H. Cobb. Trends Pharmacol Sci, 2002(23):40-45.
Mitogen-Activated Protein Kinase Pathways Mediated by ERK, JNK and p38 Protein
Kinases.
Gary L. Johnson, et al. Science. 2002(298):1911-1912
Multicellular organisms have three well-characterized subfamilies of mitoge-
nactivated protein kinases (MAPKs) that control a vast array of physiological
processes. These enzymes are regulated by a characteristic phosphorelay
system in which a series of three protein kinases phosphorylate and activate
one another. The extracellular signal-regulated kinases (ERKs) function in
the control of cell division, and inhibitors of these enzymes are being
explored as anticancer agents. The c-Jun amino-terminal kinases (JNKs)
are critical regulators of transcription, and JNK inhibitors may be effective in
control of rheumatoid arthritis. The p38 MAPKs are activated by inflamma-
tory cytokines and environmental stresses and may contribute to diseases
like asthma and autoimmunity.
Several structural studies focused on p38 bound to the pyridinyl imidazoles
VK19911, SB203580, SB216995, SB218655 and SB220025, compounds
that bind in the ATP binding pocket of p38. The amino acid residue in the
position equivalent to 106 of human p38 is crucial for determining the sensi-
tivity of protein kinases to these inhibitors.
The development of MEK1 and MEK2 inhibitors has also progressed. Struc-
tural information is particularly important for this class of kinase inhibitors
because two of these inhibitors, PD98059 and U0126, do not appear to com-
pete with ATP and thus are likely to have a distinct binding site on MEK.
Enhanced MEK1 and MEK2 activity was detected in a significant number of
primary human tumor cells. Thus, MEK1 and MEK2 inhibitors are being
developed as therapeutic agents for the treatment of cancer.
S1008 AZD6244(Selumetinib)
Melanomas acquire resistance to B-RAF(V600E) inhibition by RTK or N-RAS upregulation.
Ramin Nazarian et al. Nature, 2010(468): 973977
Vertical Targeting of the Phosphatidylinositol-3 Kinase Pathway as a Strategy for Treating
Melanoma.
Saadia A. Aziz et al. Clin Cancer Res, 2010(16):6029-6039.
Activation of FOXO3a Is Sufficient to Reverse Mitogen-Activated Protein/Extracellular
Signal-Regulated Kinase Kinase Inhibitor Chemoresistance in Human Cancer.
Jer-Yen Yang et al. Cancer Res, 2010(70):4709
MEK1 mutations confer resistance to MEK and B-RAF inhibition.
Caroline M. Emery et al. PNAS, 2009;106(48):20411-20416
S1020 CI-1040 (PD184352)
BRAF gene amplification can promote acquired resistance to MEK inhibitors in cancer cells
harboring the BRAF V600E mutation.
Corcoran RB et al. Sci Signal, 2010; 3(149):ra84.
S1036 PD0325901
RDEA119/BAY 869766: a potent, selective, allosteric inhibitor of MEK1/2 for the treatment of
cancer.
Iverson C et al. Cancer Res, 2009;69(17):6839-6847.
BRAF gene amplification can promote acquired resistance to MEK inhibitors in cancer cells
harboring the BRAF V600E mutation.
Corcoran RB et al. Sci Signal, 2010;3(149):ra84.
S1177 PD98059
Inhibitors of MAPK pathway ERK1/2 or p38 prevent the IL-1{beta}-induced up-regulation of
SRP72 autoantigen in Jurkat cells.
Arana-Argez VE et al. J Biol Chem, 2010;285(43):32824-32833
S1102 U0126-EtOH
Differences in Wound Healing in Mice with Deficiency of IL-6 versus IL-6 Receptor.
Molly M. McFarland-Mancini et al. J Immunol, 2010;184(12): 7219-7228.
46
Papers
Using Selleck Products
MEK (MAPK/Erk kinase)

S1531 BIX 02189
BIX 02189 is a selective MEK5/ERK5 inhibitor with an IC50 of 59 nM. It inhibited catalytic function of purified,
MEK5 enzyme. The MEK5 inhibitors blocked phosphorylation of ERK5, without affecting phosphorylation of
ERK1/2 in sorbitol-stimulated HeLa cells. The compounds also inhibited transcriptional activation of MEF2C,
a downstream substrate of the MEK5/Erk5 signaling cascade, in a cellular trans-reporter assay system.
Size Price
10mg
25mg
200mg

S1561 BMS 777607
%06LVD6PDOO0ROHFXOH0HW.LQDVH,QKLELWRUZLWKDQ,&RI0,WVWUHDWPHQWKDGOLWWOHHIIHFW
on tumor cell growth but inhibited cell scattering activated by exogenous HGF, with almost complete inhibition
DWPRO/LQ3&DQG'8FHOOV0HFKDQLVWLFDOO\QDQRPRODUGRVHVRI%06SRWHQWO\EORFNHG
HGF-stimulated c-Met autophosphorylation and downstream activation of Akt and extracellular
signal-regulated kinase.
Size Price
N
H
N
O
O
N
H
N
N H2N
Cl
O
F
H
N
O
N
O
O
F
S1475 AS703026
AS703026 is a novel, selective, orally bioavailable MEK1/2 inhibitor, in human multiple myeloma. AS703026
inhibited growth and survival of MM cells (cell IC50 ranging from 0.005 to 2 M) and cytokine-induced
osteoclast differentiation more potently (9- to 10-fold) than AZD6244. Inhibition of proliferation induced by
AS703026 was mediated by G0-G1 cell cycle arrest and was accompanied by reduction of MAF oncogene
expression.
Synonyms:

MSC1936369B
Size Price
S2134 AZD8330
AZD8330 is an orally active, selective MEK inhibitor with potential antineoplastic activity. It specifically inhibits
MEK, resulting in inhibition of growth factor-mediated cell signaling and tumor cell proliferation. MEK is a key
component of the MAPK signaling pathway that regulates cell growth. Constitutive activation of this pathway
has been implicated in many cancers.
Synonyms:

ARRY-424704, ARRY-704
Size Price
I
F
H
N
N
H
N O OH
OH
I
F
H
N
N
O
H
N
O
OH O

S1020 CI-1040
CI-1040 is a non-competitive inhibitor of MEK1/2 with a Ki of 300nM in vitro CI-1040 inhibited MEK (as
measured by phosphorylated ERK (p-ERK) levels) with a half-maximal inhibitory concentration of 100500nM
in all cell lines tested.
Synonyms:

PD184352
Size Price
F
F
NH
Cl
I
N
H
O
O

S1530 BIX 02188
%,;LVD0(.VHOHFWLYHLQKLELWRUZLWKDQ,&RI0,WFRPSOHWHO\UHYHUVHGWKHLQKLELWRU\HIIHFWV
of flow. The physiological roles of Erk5 in neuronal cells have not been clarified. One reason was the lack of a
selective Erk5 pharmacological inhibitor until the novel selective MEK5/Erk5 inhibitors BIX02188 and
BIX02189.
Size Price
S1008 AZD6244
MAPK kinase , immediately downstream of BRAF, is a promising target for ras-raf-MEK-ERK pathway
inhibition. Four lines bearing V600E BRAF mutations were all sensitive to AZD6244, with GI50 values ranging
from 14 to 50 nM. A positive control BRAF mutant melanoma line, SKMel28, exhibited a similar GI50 of 23 nM.
Synonyms:

ARRY-142886, Selumetinib, ARRY142886
Size Price
H
N
Cl
Br F
N
N
H
N O
O
HO
N
H
H
N
O
O
N
H
N
Data from Cancer Research.June 15 using our product.
lysatesfromvariouscancer celllines:
breastcancer(MDA-MB-435),coloncancer(HCT116,SW620,andHT29),
DQGPHODQRPD:0WUHDWHGZLWK'062RU$='PRO/
for4hweresubjectedtoimmunoblottingwiththeindicatedantibodies.
S1008 AZD6244
Feed
Data from our customer Dr Dong Shou, Baylor College of Medicine.
The bar chart represents the relative numbers of third-round colonies
of primary hematopoietic cells transduced with MLL-AF9 with treatment
of compound PD184352 (CI-1040, 10uM, a MEK inhibitor) and SB216763
(10uM, GSK-3 inhibitor). The synergiceffect between compounds CI-1040
and SB-216763 has been observed.
0
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Corlro| 3821Z3|10uV) P0181352|10uV) P0181352 3821Z3
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Corlro| 3821Z3|10uV) P0181352|10uV) P0181352 3821Z3 Corlro| 3821Z3|10uV) P0181352|10uV) P0181352 3821Z3
N
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S1020 CI-1040
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IEK VAPK
4/
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10mg
10mg
50mg
5mg
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200mg
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200mg
10mg
Toll Free:(877)796-6397 www.selleckchem.com info@selleckchem.com
Phone:+1-832-582-8158
---USA and Canada only---
S1177 PD98059
PD 98059 is a highly selective inhibitor of MEK1 and MEK2 with IC50 values of 4 M and 50 M respectively.
PD98059 does not inhibit activation of other highly related dual-specificity protein kinases or the activity of over
18 other Ser/Thr protein kinases. At concentrations up to 100 M, PD98059 does not inhibit activation of MKK3
or SEK (MKK4) as determined by measuring phosphorylation at its activation site.
Size Price
O
O
NH
2
O
Data from JBC.August 19, 2010 using our product.
&7KHHIIHFWRI(5.LQKLELWRU3'0
was evaluated in SRP72 immunoprecipitated cell lysates.
WB using anti-phosphoserine antibody showed a decreased
653EDQGZKHQXVHGWKHLQKLELWRUDWFRQFHQWUDWLRQRI0
DWPLQ0DWPLQDQG0DWDQGPLQ
(lanes 3,5,8 and 9). 3 D) Results were analyzed and RUA graphicated,
ILQGLQJVLJQLILFDQWUHVXOWVDW0DWYV0DWYVDQG
0DWYVPLQ
p38 MAPK (P38 mitogen-activated protein kinases)
S1177 PD98059
Feed

S1574 BIRB 796
BIRB 796 is a small molecule p38 MAPK inhibitor with an Kd of 0.1 nM. It is more potent than SB 203580 on
SDQGS0$3.V,WLVDSRWHQWLDODJHQWIRUWKHWUHDWPHQWRILQIODPPDWRU\GLVHDVHV%,5%EORFNHG
baseline and bortezomib-triggered upregulation of p38 MAPK and Hsp27 phosphorylation, thereby enhancing
cytotoxicity and caspase activation.
Synonyms:

BIX02188
Size Price
Data from The Joumal of Immunology.May 10 2010 using our product.
S1102 U0126-EtOH
U0126 is an inhibitor of both MEK1(IC50 of 72 nM) and MEK2(IC50 of 58 nM). U0126 is a highly selective
inhibitor of both MEK1 and MEK2. U0126 was found to functionally antagonize AP-1 transcriptional activity via
noncompetitive inhibition of the dual specificity kinase MEK with IC50 of 72 nM for MEK1 and 58 nM for MEK2.
U0126 sensitized MDA-MB231 and HBC4 to anoikis, i.e., upon treatment with U0126, cells deprived of
anchorage entered apoptosis.
Size Price
NH
2
NH
2
S
CN
S
CN
NH
2
NH
2
OH
Total and p-ERKs were assessed in small wounds
generated in WTand Il6ra2/2 mice treated topically with
vehicle(DMSO) or with the MEK inhibitor U0126. Wounds
were harvested after 1 d, and western blotting was
performed on lysates.

S1036 PD0325901 Size Price
PD318088 is a non-ATP competitive allosteric MEK1/2 inhibitor. It is a small-molecule inhibitor bound within
the allosteric site. The binding modes of two kinase inhibitors are shown in relation to the binding site of ATP
in the kinase active site. The MEK1 inhibitor PD318088 binds with ATP in a region of the kinase active site that
is adjacent to the ATP-binding site.
Size Price
F
F
H
N
F
I
O
H
N
O
OH
HO
F
F Br
H
N
F
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Data provided by our customer Dr.Deborah Citrin,NIH.
Western blot analysis of p-Erk1/2, total Erk1/2, PD0325901
treated HT29 xenograft tumours.

PD0325901 is non-competitive with ATP and is exquisitely specific and highly potent against purified MEK,
exhibiting a Kiapp of 1 nM against activated MEK1 and MEK2. PD0325901 is roughly 500-fold more potent
than CI-1040 with respect to its cellular effects on phosphorylation of ERK1 and ERK2, exhibiting
subnanomolar activity.

S1568 PD318088
S1036 PD0325901
Feed
S1102 U0126-EtOH
Feed
Solutions to Signal Transduction Research
48
VAPK IEK / p38 IAPK
25mg
50mg
5mg
50mg
200mg
10mg
100mg
200mg
25mg
50mg
200mg
10mg
10mg
50mg
5mg
O
N
N
H
N
H
O
N
N
O


S1494 LY2228820
LY2228820 is a novel and potent p38MAPK inhibitor: in vitro kinase enzyme activity showed that the IC50 for
S0$3.DQGS0$3.ZHUHQ0DQGQ0UHVSHFWLYHO\ZKLOHWKDWIRUS0$3.S0$3.DQGD
panel of 172 additional kinases was more than 20 M. Phosphorylation of MAPKAPK2 and/or HSP27,
downstream targets of p38 MAPK, was significantly inhibited by LY in both MM cell lines and LT-BMSCs.
Size Price
N
H
N N
F
N
N
NH2
S
O
O
OH S
O
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OH
S1077 SB 202190
In the presence of SB202190, the ED50 values for the farnesyltransferase inhibitor FPT inhibitor II and MEK
inhibitor U0126 were significantly decreased. SB202190 increased the phosphorylation of C-Raf and
extracellular regulated kinase. SB202190 suppressed the kinase activity of p38, leading to inhibition of
activation of MAPKAPK2. SB202190 blocked p38 half maximally at 30 nM, concentrations as high as 30,000
nM did not inhibit ERK and JNK activity.
Size Price
F

N
NH
N
OH
Data from JBC.August 19, 2010 using our product.
-XUNDWFHOOVZLWK6%DWZHUHWHVWHG
and a decreased SRP72 expression was found when using
DW0ODQHVDQG
S1077 SB 202190
Feed
S1458 VX-745
VX-745 is a lead anti-inflammatory candidate, p38 MAPK inhibitor (IC50=10 nM) for the treatment of
Rheumatoid arthritis (RA). In vitro, VX-745 was selective for p38 MAPK compared to a large panel of kinases
,&09;VHOHFWLYHO\LQKLELWHGS0$3.,&Q0S0$3.,&Q0EXWQRW
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DQG71)UHVSHFWLYHO\
Size Price

S1527 Vinorelbine
Vinorelbine is the first 5NOR semi-synthetic vinca alkaloid and an anti-mitotic chemotherapy drug. In the
breast cancer cell lines MCF-7 and MDA-MB-468, increased p38 activity was demonstrated following
vinorelbine but not doxorubicin treatment, whether vinorelbine was given prior to or simultaneously with
doxorubicin. MAPK activity and p53 expression remained unchanged following vinorelbine treatment.
Synonyms:

Navelbine
Size Price

S6005 VX-702
9; GRVHGHSHQGHQWO\ LQKLELWHG WKH SURGXFWLRQ RI ,/ ,/ DQG 71) ,& DQG QJPO
respectively). Platelet function alone, or in conjunction activation was completely or partially inhibited by
SUHLQFXEDWLRQZLWK0RI9;,&WRQ09;KDGQRHIIHFWRQSODWHOHWDJJUHJDWLRQLQGXFHG
by any of the p38 MAPK agonists.
Size Price
N
N H
H O
O
O
O
HO
O
O
O
NH
N
F
F
N
O H
2
N
N
NH
2
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S
N
N
N O
Cl
Cl

S1076 SB 203580
SB 203580 is a potent inhibitor of LPS-induced cytokine synthesis in the human monocyte cell line THP-1
(IC50 = 50-100 nM). SB 203580 inhibited the RK from heat-shocked HeLa cells and osmotically stressed
3&FHOOVRUEDFWHULDOO\H[SUHVVHG&6%3ZLWKDQ,&RI06%LQGXFHGDFWLYDWLRQRIF5DILV
independent of stress-activated protein kinase 2a/p38 inhibition.
Synonyms:

RWJ 64809, PB 203580
Size Price
N
N
H
N
F
S
O
Data from JBC.August 19, 2010 using our product.
7KHHIIHFWVRISLQKLELWRU6%0RQ653SURWHLQ
expression was evaluated by WB using antibodies against human SRP72,
SRP54 and GAPDH. A decreased intensity of SRP72 bands were noted
ZKHQXVLQJWKHLQKLELWRUDW0FRQFHQWUDWLRQDWPLQODQHDQG
0DWDQGPLQODQHVDQG
S1076 SB 203580
Feed
p38 IAPK
49
50mg
100mg
25mg
50mg
200mg
10mg
50mg
100mg
25mg
50mg
200mg
10mg
50mg
100mg
25mg
50mg
200mg
10mg
VAPK
Toll Free:(877)796-6397 www.selleckchem.com info@selleckchem.com
Phone:+1-832-582-8158
---USA and Canada only---
JNK(Jun N-terminal kinase)

S1460 SP600125
SP600125 is a JNK inhibitor (IC50=40 nM for JNK-1 and JNK-2 and 90 nM for JNK-3). This agent exhibits
greater than 300-fold selectivity for JNK against related MAP kinases Erk1 and p382, and the serine
threonine kinase PKA. SP600125 is a reversible ATP-competitive inhibitor. In cells, SP600125 dose
GHSHQGHQWO\LQKLELWHGWKHSKRVSKRU\ODWLRQRIF-XQWKHH[SUHVVLRQRILQDPPDWRU\JHQHV&2;,/,)1
71)
Size Price
25mg
50mg
500mg
O
N
NH
%5DI
Synonyms:
ZM 252868, AG 1517, Tyrphostin AG 1517 S2161 RAF265 Page 8
Synonyms:

CHIR-265
Synonyms:
ZM 252868, AG 1517, Tyrphostin AG 1517 S1040 Sorafenib Tosylat Page 9
Synonyms:

Nexavar, Bay 43-9006
Synonyms:
ZM 252868, AG 1517, Tyrphostin AG 1517 S1178 BAY 73-4506 Page 8
Synonyms:

Regorafenib

S1152 PLX-4720
PLX4720 inhibits B-Raf V600E with an IC50 of 13 nM. PLX4720 preferentially inhibits the active B-Raf V600E
kinase compared with a broad spectrum of other kinases (IC50:B-Raf=160 nM, BRK=130 nM, other kinases
!Q0 DQG SRWHQW F\WRWR[LF HIIHFWV DUH DOVR H[FOXVLYH WR FHOOV EHDULQJ WKH 9( DOOHOH *, 0
ZKLOHRWKHUZLOGFHOO*,!0
Size Price
5mg
10mg
25mg
N
N
H
Cl
O
F
F
N
H
S
O
O
1mg
5mg
10mg
S1104 GDC-0879
GDC-0879 is a highly selective, novel potent, orally bioavailable B-Raf inhibitor in various in vitro and
cell-based assays with an IC50 estimate of 0.13 nM against purified B-Raf V600E enzyme and a cellular pErk
IC50 of 63 nM in the MALME-3M cell line. For this compound, subnanomolar enzyme potency translated into
very effective reduction of cellular viability of BRAF-mutant Malme3M cells (EC50 values were 0.75 mol/L for
GDC-0879).
Size Price
S1267 PLX-4032
PLX4032 is a highly selective inhibitor of b-Raf kinase activity, with an IC50 of 44 nmol/L against
V600E-mutant b-Raf. b-Raf mutant melanoma cell strains were highly sensitive to PLX4032 with IC50 in the
Q0UDQJHQ0ZKHUHDV%5$)ZLOGW\SHFHOOVZHUHUHVLVWDQWZLWK,&0RUDERYH
Synonyms:

RG7204, R7204, RO5185426
Size Price
OH
N
N
N
N
HO
N
N
H
Cl O
HN
F
S
O
O
F
B-RafV600E mutated melanoma line,A375,was treated with different
doses of GDC0879 for 1h or 24 h. Cell lystates were analyzed by
Western blotting to determine the leves of phosphorylated MEK1/2
(pMEK1/2) and phosphorylated ERK1/2 (pERK1/2)
Data provided by our customer Jong-in Park,Ph.D.,Medical College of Wisconsin
S1104 GDC-0879
Feed
Data provided by Daniel C. Cho, MD Instructor, Harvard Medical School Director,
Experimental Therapeutics Program Division of Hematology
and Oncology Beth Israel Deaconess Medical Center
a dose titration of PLX-4720 in A375 melanoma cells which possess
a V600E B-Raf mutation. Effects of increasing PLX-4720 dose on
Erk phosphorylation and on tumor cell proliferation as determined
by MTS assay are shown.
S1152 PLX-4720
Feed
10mg
50mg
200mg
Solutions to Signal Transduction Research
50
VAPK B-RaI / 1NK
5l
PI3K/Akt
AP|arraco|od|ca|Vapoll|ePl3-KFar||v0el|resaRo|elorp110a|rlrsu||r
3|dra||rd.
Zachary A. Knight et al. Cell, 2006(125):733747.
Phosphoinositide 3-kinases (PI3Ks) catalyze the synthesis of the phosphati-
dylinositol (PI) second messengers PI(3)P, PI(3,4)P2, and PI(3,4,5)P3. In
the appropriate cellular context, these three lipids control diverse physiological
processes including cell growth, survival, differentiation, and chemotaxis.
The PI3-K family comprises 15 kinases with distinct substrate specificities,
expression patterns, and modes of regulation.
The class I PI3Ks (p110a, p110b, p110d, and p110g) are activated by tyrosine
kinases or G protein-coupled receptors to generate PIP3, which engages
downstream effectors such as the Akt/PDK1 pathway, the Tec family
kinases, and the Rho family GTPases. The class II and III PI3-Ks play a key
role in intracellular trafficking through the synthesis of PI(3)P and PI(3,4)P2.
The PIKKs are protein kinases that control cell growth (mTORC1) or monitor
genomic integrity (ATM, ATR, DNA-PK, and hSmg-1).
52
S1009 BEZ235(NVP-BEZ235)
Activation of FOXO3a Is Sufficient to Reverse Mitogen-Activated Protein/Extracellular
Signal-Regulated Kinase Kinase Inhibitor Chemoresistance in Human Cancer.
Jer-Yen Yang et al. Cancer Res, 2010(70):4709
Inhibition profiles of phosphatidylinositol 3-kinase inhibitors against PI3K superfamily and
human cancer cell line panel JFCR39.
Kong D et al. Eur J Cancer. 2010;46(6):1111-1121.
Correlating Phosphatidylinositol 3-Kinase Inhibitor Efficacy with Signaling Pathway Status: In
silico and Biological Evaluations.
Shingo Dan et al. Cancer Res, 2010(70):4982
S1065 GDC-0941
Vertical inhibition of the mTORC1/mTORC2/PI3K pathway shows synergistic effects against
melanoma in vitro and in vivo.
Werzowa J et al. J Invest Dermatol, 2011;131(2):495-503.
S1022 Deforolimus(MK-8669)
Inhibition of glycogen biosynthesis via mTORC1 suppression as an adjunct therapy for
Pompe disease.
Ashe KM et al. Mol Genet Metab, 2010;100(4):309-315
S1120 Everolimus(RAD001)
Pharmacodynamic Characterizationof the Efficacy Signals Due to Selective BRAF Inhibition
with PLX4032 in Malignant Melanoma.
Tap WD et al. Neoplasia, 2010;12(8):637-649.
S1226 KU-0063794
The Mechanical StressActivated Serum-, Glucocorticoid-Regulated Kinase 1 Contributes to
Neointima Formation in Vein Grafts.
Jizhong Cheng et al. Circulation Res, 2010(107):1265-1274.
S1044 Temsirolimus
Inhibition of glycogen biosynthesis via mTORC1 suppression as an adjunct therapy for
Pompe disease.
Ashe KM et al. Mol Genet Metab, 2010;100(4):309-15.
Papers
Using Selleck Products
PI3K
Data from our customer Dr.Saraswati Sukumar,Johns Hopkins University School of Medicine.
DMSO AS-605240 GDC-0941 GSK1059615 LY294002 PI-103
AKT
P-AKT (S473)
AKT
P
P-AKT (S473) P
DMSO PIK-90 TG100-115 TGX-221 ZSTK474

S1360 GSK1059615
*6.LVDSDQ3,.UHYHUVLEOHLQKLELWRUZLWKVXEQDQRPRODU,&IRU3,.Q0DQG3,.
Q0 DQG VKRZV ORZ QDQRPRODU DFWLYLW\ WRZDUGV Q0 Q0 DQG P725 Q0 *6. LQKLELWV
PI3K pathway in cells inducing G1 arrest, although apopto-sis was observed in a subset of cell lines. Breast
tumor cells seem to be more sensitive to this compound.
Size Price

S1268 IC-87114
,&LVWKHILUVWLVRIRUPVHOHFWLYH3,.LQKLELWRU7KLVTXLQD]ROLQRQHSXULQHLQKLELWVS,&0
DWPLGQDQRPRODUFRQFHQWUDWLRQVDQGVKRZVIROGVHOHFWLYLW\RYHURWKHUFODVV,3,.VSS
DQGS7KHVHOHFWLYLW\RI,&LVUHPDUNDEOHJLYHQWKDWWKHUHVLGXHVWKDWOLQHWKH$73ELQGLQJSRFNHW
of the class I PI3Ks are highly conserved.
Size Price

S1105 LY294002
LY 294002 has been shown to be a potent inhibitor of PI3K activity, acting as a competitive inhibitor for ATP
binding site of the enzyme. LY 294002 inhibits cell proliferation of choroidal melanoma OCM-1 cells, the IC50
ZDVREVHUYHGDERXW0/<LVDOVRDQLQKLELWRURIFDVHLQNLQDVH,,$SSOLFDWLRQRI/<FDXVHV
DVXEVWDQWLDODFFHOHUDWLRQRI0(33IUHTXHQF\0DWWKHIURJQHXURPXVFXODUMXQFWLRQ
Size Price

S1038 PI-103
PI-103 is a potent, cell-permeable, ATP-competitive PI3K family members inhibitor with IC50 of 2, 8, 20, 26,
Q0 IRU '1$3. S P725& 3,.& S P725& S DQG S
respectively. PI-103 was essentially cytostatic for cell lines and induced cell cycle arrest in the G1 phase.
PI-103 had additive proapoptotic effects with etoposide in blast cells and in immature leukemic cells.
Size Price
N
N
HN
S
O
O
N
N
O
N
N
N
N
H2N
O
O
N
O
N
N
N
O
N
OH
O
Data from our customer Dr.Saraswati Sukumar,Johns Hopkins University School of Medicine.
We treated all of drugs in T47D which has a PIK3CA H1047R mutation with
the concentration shown below for 1 hour and performed western blot analysis
using antibodies to phospho-AKT (serine 473), and total AKT.
5uM AS-605240, 3uM GDC-0941, 4uM GSK1059615, 10uM LY294002,
8uM PI-103, 3uM PIK-90, 4uM TG100-115, 5uM TGX-221, 3uM ZSTK474.
We treated all of drugs in T47D which has a PIK3CA H1047R mutation with
the concentration shown below for 1 hour and performed western blot analysis
using antibodies to phospho-AKT (serine 473), and total AKT.
5uM AS-605240, 3uM GDC-0941, 4uM GSK1059615, 10uM LY294002,
8uM PI-103, 3uM PIK-90, 4uM TG100-115, 5uM TGX-221, 3uM ZSTK474.
Data from our customer Dr.Saraswati Sukumar,
Johns Hopkins University School of Medicine.
We treated all of drugs in T47D which has a PIK3CA H1047R
mutation with the concentration shown below for 1 hour and
performed western blot analysis using antibodies to phospho-AKT
(serine 473), and total AKT. 5uM AS-605240, 3uM GDC-0941,
4uM GSK1059615, 10uM LY294002, 8uM PI-103, 3uM PIK-90,
4uM TG100-115, 5uM TGX-221, 3uM ZSTK474.
P-AKT
AKT

0
+ + + + + -
GSK1059615
EGF(100ng/ml)
S1360 GSK 1059615
Feed
Produced Independently by our customer Dr.Zhang,
Tianjin Medical University
Western blot analysis of Akt and p-Akt,
0*6.ZDVDGGHG
DMSO AS-605240 GDC-0941 GSK1059615 LY294002 PI-103
AKT
P-AKT (S473)
AKT
P
P-AKT (S473) P
DMSO PIK-90 TG100-115 TGX-221 ZSTK474
S1105 LY294002
Feed
S1038 PI-103
Feed

S1410 AS-605240
$6LVD3,.LQKLELWRU,&DWQ0ZKLFKGLVSOD\VIROGVHOHFWLYLW\RYHU3,.DQG3,.DQG
IROGVHOHFWLYLW\RYHU3,.7KLVDJHQWLVWKHILUVWH[DPSOHVRIVHOHFWLYH3,.LQKLELWRUVDQGZDVXVHGWR
block neutrophil chemotaxis in vitro and in vivo. In passive mouse models for rheumatoid arthritis these
compounds minimized progression of joint destruction.
Size Price
N
N
S
HN
O
O
DMSO AS-605240 GDC-0941 GSK1059615 LY294002 PI-103
AKT
P-AKT (S473)
AKT
P
P-AKT (S473) P
DMSO PIK-90 TG100-115 TGX-221 ZSTK474
P-AKT
AKT

0
+ + + + + -
AS-605240
EGF(100ng/ml)
Data from our customer Dr.Saraswati Sukumar,
Johns Hopkins University School of Medicine.
We treated all of drugs in T47D which has a PIK3CA H1047R
mutation with the concentration shown below for 1 hour and
performed western blot analysis using antibodies to phospho-AKT
(serine 473), and total AKT. 5uM AS-605240, 3uM GDC-0941,
4uM GSK1059615, 10uM LY294002, 8uM PI-103, 3uM PIK-90,
4uM TG100-115, 5uM TGX-221, 3uM ZSTK474.
S1410 AS-605240
Feed
Produced Independently by our customer Dr.Zhang,
Tianjin Medical University
Western blot analysis of Akt and p-Akt,
0$6ZDVDGGHG
DMSO AS-605240 GDC-0941 GSK1059615 LY294002 PI-103
AKT
P-AKT (S473)
AKT
P
P-AKT (S473) P
DMSO PIK-90 TG100-115 TGX-221 ZSTK474
PI3K Pl3K/A|l
53
50mg
200mg
10mg
10mg
50mg
1mg
25mg
50mg
10mg
50mg
200mg
10mg
50mg
100mg
10mg
Toll Free:(877)796-6397 www.selleckchem.com info@selleckchem.com
Phone:+1-832-582-8158
---USA and Canada only---
S1009 BEZ235
NVP-BEZ235 inhibits PI3K and mTOR kinase activity by binding to the ATP-binding cleft of these enzymes.
The PI3K/Akt/ mTOR pathway is often constitutively activated in human tumor cells. For Class I PI3K family,
193%(=ELRFKHPLFDO,&DUHQ0DJDLQVWSQ0DJDLQVWSQ0DJDLQVWSQ0DJDLQVW
S4XDQWLILFDWLRQRI6$NWDQG73$NWOHYHOVUHYHDOHGWKDWUHGXFWLRQRFFXUUHGDWDFRPSRXQG
concentration of 8.0 and 30 nmol/L.
Synonyms:

NVP-BEZ235
Size Price
S1065 GDC-0941
*'&DJDLQVWSD,&080*,&0$,&0DQGLQYLWURPHWDEROLF
VWDELOLW\ LQ PRXVH DQG KXPDQ LV 7KH LQKLELWLRQV RI 80* 3& 0'$0% FDQFHU FHOO
SUROLIHUDWLRQDUH,&0UHVSHFWLYHO\
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S1462 AZD6482
$='LVD3,.LQKLELWRU,&0XVHGLQDQWLWKURPERWLFWKHUDS\7KLVDJHQWWDUJHWVDSURFHVV
that is critical to pathological thrombus formation without interfering with normal haemostasis, which avoids the
GUDZEDFNVRIWKHH[LVWLQJDQWLWKURPERWLFWKHUDS\7KLVDJHQWLQKLELWV3,.ZLWK,&RI
0UHVSHFWLYHO\
Size Price
O
OH
NH
N
N
O
N
O
NH
N N
N
S
N
O
N
N
S
O
O
Data published in European Journal
of Cancer (2010,46:1111-1121),
by our customer Dexin Kong,Japanese
Foundation for Cancer Research.
Relative kinase activities of
SPXWDQWVDQGWKH
inhibitory effect of PI3K
inhibitors against hotspot
PXWDQWVRIS
Data from Cancer Research.
June 15 2010 using our
product.
DMSO AS-605240 GDC-0941 GSK1059615 LY294002 PI-103
AKT
P-AKT (S473)
AKT
P
P-AKT (S473) P
DMSO PIK-90 TG100-115 TGX-221 ZSTK474
N
N
N
O
N
N
3,.DFWLYLW\DQG,&WHVWUHVXOW
Q00=67.*'&
NVP-BEZ235, LY294002 were added.
S1009 BEZ235
Feed
Data from our customer Dr.Saraswati Sukumar,Johns Hopkins University School of Medicine.
We treated all of drugs in T47D which has a PIK3CA H1047R mutation with
the concentration shown below for 1 hour and performed western blot analysis
using antibodies to phospho-AKT (serine 473), and total AKT.
5uM AS-605240, 3uM GDC-0941, 4uM GSK1059615, 10uM LY294002,
8uM PI-103, 3uM PIK-90, 4uM TG100-115, 5uM TGX-221, 3uM ZSTK474.
S1065 GDC-0941
Feed
DMSO AS-605240 GDC-0941 GSK1059615 LY294002 PI-103
AKT
P-AKT (S473)
AKT
P
P-AKT (S473) P
DMSO PIK-90 TG100-115 TGX-221 ZSTK474

S1169 TGX-221
7*; LV D SRWHQW VHOHFWLYH DQG FHOO SHUPHDEOH LQKLELWRU RI 3,. S 7KURPERJHQL[ FRPSRXQG
7*; LV D /< DQDORJXH DEOH WR LQKLELW VHOHFWLYHO\ WKH 3,. LVRIRUP LQ YLWUR 7*; LV D
ORZQDQRPRODU UDQJH LQKLELWRU VKRZV DERXW IROG KLJKHU VHOHFWLYLW\ RYHU 3,. DQG LV FHOO SHUPHDEOH
7*; LQWHUIHUHG ZLWK VKHDU VWUHVVLQGXFHG 3WG,QV3 SURGXFWLRQ DQG LQWHJULQ ,,EPHGLDWHG
adhesion in platelets.
Size Price

S1118 XL147
XL147 is a selective inhibitor of Class I PI3K isoforms. XL147 reversibly binds to class 1 PI3Ks in an
ATP-competitive manner, inhibiting the production of PIP3 and activation of the PI3K signaling pathway.
XL147 exhibits dose-dependent and sustained inhibition of PI3K signaling in multiple human tumor xenograft
models when administered as a single agent.
Synonyms:

SAR245408
Size Price
Feed
S1169 TGX-221
N
H
N
N
O N
O
N
N NH
NH
N
S N
S O O
Data from our customer Dr.Saraswati Sukumar,Johns Hopkins University School of Medicine.
We treated all of drugs in T47D which has a PIK3CA H1047R mutation with
the concentration shown below for 1 hour and performed western blot analysis
using antibodies to phospho-AKT (serine 473), and total AKT.
5uM AS-605240, 3uM GDC-0941, 4uM GSK1059615, 10uM LY294002,
8uM PI-103, 3uM PIK-90, 4uM TG100-115, 5uM TGX-221, 3uM ZSTK474.
S1118 XL147
Feed
Produced Independently by our customer Dr.Zhang,
Tianjin Medical University
Western blot analysis of Akt and p-Akt,
0;/ZDVDGGHG
Solutions to Signal Transduction Research
54
Pl3K/A|l PI3K
50mg
200mg
10mg
100mg
200mg
25mg
10mg
50mg
5mg
25mg
100mg
5mg
10mg
50mg
5mg

S1523 XL765
;/LVDPL[HGP7253,NLQKLELWRUZLWK,&RIDQGQ0IRUP725SDQG
respectively. It is an orally available small molecule that has been shown selectively inhibit the activity of PI3K
and mTOR. XL765 has also been shown to enhance the anti-tumor effects of several chemotherapeutic
agents in preclinical cancer models.
Synonyms:

SAR245409
Size Price

S1072 ZSTK474
=67.LVDQLQKLELWRURI3,.,&DWQ07KLVDJHQWLQKLELWV3,.DQG3,.ZLWK,&RIDQG
53 nM, respectively. ZSTK474 was identified from a chemical library of about 1500 triazine derivatives, and
selected for their ability to block tumor cell growth. Toxicity was reported to be moderate.
Size Price
DMSO AS-605240 GDC-0941 GSK1059615 LY294002 PI-103
AKT
P-AKT (S473)
AKT
P
P-AKT (S473) P
DMSO PIK-90 TG100-115 TGX-221 ZSTK474
N
N
NH
O
O
HN S
O
O
NH
O
O
N
N
N
N
N
N
N
O
O
F
F
Data from our customer Dr.Saraswati Sukumar,Johns Hopkins University School of Medicine.
We treated all of drugs in T47D which has a PIK3CA H1047R mutation with
the concentration shown below for 1 hour and performed western blot analysis
using antibodies to phospho-AKT (serine 473), and total AKT.
5uM AS-605240, 3uM GDC-0941, 4uM GSK1059615, 10uM LY294002,
8uM PI-103, 3uM PIK-90, 4uM TG100-115, 5uM TGX-221, 3uM ZSTK474.
S1118 XL147
Feed

S2207 PIK-293
3,. LV D 3,. LQKLELWRU3,. LQKLELW WKH SSSDQG S ZLWK ,& RI
100uM,25uM,0.24uM,and 10uM.PIK-293 is the parent compand of PIK-294.
Synonyms:

AS605240
Size Price
\l"
DMSO AS-605240 GDC-0941 GSK1059615 LY294002 PI-103
AKT
P-AKT (S473)
AKT
P
P-AKT (S473) P
DMSO PIK-90 TG100-115 TGX-221 ZSTK474
S1489 PIK-93
3,.LVD3,.,,,LQKLELWRU,&DWQ03,.LVWKHILUVWUHSRUWHG3,NLQDVHLQKLELWRUZKLFKLVDEOHWR
LQKLELW3,.,,,DWORZQDQRPRODUUDQJH,QDGGLWLRQWKLVFRPSRXQGDOVRLQKLELWVSRWHQWO\3,.LQYLWUR,&
DWQ07KLVFRPSRXQGLQKLELWVSSSZLWK,&RI0
Size Price

S1187 PIK-90
3,.LVDSRWHQWDQGFHOOSHUPHDEOH3,.LQKLELWRUZLWK,&YDOXHVQ0RIDQGIRUS
DQGLVRIRUPVORZP725DFWLYLW\%HVLGHV9DO+ELQGLQJ3,.XVHVLWVS\ULGLQHULQJWRHQWHUWKH
hydrophobic affinity pocket of the ATP binding site, where it also interacts with Lys833.
Size Price
O
O
N
N
N
NH
N O
Cl
S
O
O
S
N
NH
O
NH
HO
Data from our customer Dr.Saraswati Sukumar,Johns Hopkins University School of Medicine.
We treated all of drugs in T47D which has a PIK3CA H1047R mutation with
the concentration shown below for 1 hour and performed western blot analysis
using antibodies to phospho-AKT (serine 473), and total AKT.
5uM AS-605240, 3uM GDC-0941, 4uM GSK1059615, 10uM LY294002,
8uM PI-103, 3uM PIK-90, 4uM TG100-115, 5uM TGX-221, 3uM ZSTK474.
S1187 PIK-90
Feed
N
N
O
N
N
N
N
NH2
55
50mg
200mg
10mg
50mg
200mg
10mg
10mg
50mg
5mg
5mg
25mg
1mg
200mg
1g
50mg
PI3K Pl3K/A|l
Data from our customer Dr.Saraswati Sukumar,Johns Hopkins University School of Medicine.
S1352 TG100-115
7*LQKLELW3,.DQG,&YDOXHVRIDQGQ0UHVSHFWLYHO\ZKHUHDVERWK3,.DQG
ZHUH UHODWLYHO\ XQDIIHFWHG ,& YDOXHV! 0 $V D JDXJH RI JHQHUDO VSHFLILFLW\ 7* ZDV DOVR
DVVD\HGDJDLQVWDSURWHLQNLQDVHSDQHOQRQHRIZKLFKZDVLQKLELWHGDW,&YDOXHV0
Size Price
DMSO AS-605240 GDC-0941 GSK1059615 LY294002 PI-103
AKT
P-AKT (S473)
AKT
P
P-AKT (S473) P
DMSO PIK-90 TG100-115 TGX-221 ZSTK474
N
N
N
N
NH
2
NH
2
OH
OH
We treated all of drugs in T47D which has a PIK3CA H1047R mutation with
the concentration shown below for 1 hour and performed western blot analysis
using antibodies to phospho-AKT (serine 473), and total AKT.
5uM AS-605240, 3uM GDC-0941, 4uM GSK1059615, 10uM LY294002,
8uM PI-103, 3uM PIK-90, 4uM TG100-115, 5uM TGX-221, 3uM ZSTK474.
S1352 TG100-115
Feed
50mg
200mg
10mg
64XHUFHWLQ
Synonyms:

6RSKRUHWLQ0HOHWLQ4XHUFHWLQH
Page 12
Toll Free:(877)796-6397 www.selleckchem.com info@selleckchem.com
Phone:+1-832-582-8158
---USA and Canada only---

S1022 Deforolimus
Deforolimus is a small-molecule inhibitor of mTOR. It is an immunosuppressant for the treatment of certain
cancers. Blocking mTOR creates a starvation-like effect in cancer cells by interfering with cell growth, division,
metabolism, and angiogenesis.
Synonyms:

AP23573, MK-8669, Ridaforolimus
Size Price

S1555 AZD8055
AZD8055 is a potent, selective, and orally bioavailable ATP-competitive mTOR kinase inhibitor with an IC50
of 0.8 nM. It inhibits the phosphorylation of mTORC1 substrates p70S6K and 4E-BP1 as well as
phosphorylation of the mTORC2 substrate AKT and downstream proteins. The rapamycin-resistant T37/46
phosphorylation sites on 4E-BP1 were fully inhibited by AZD8055, resulting in significant inhibition of
cap-dependent translation.
Size Price
HO
O
N N
N
N
O
N
O
O
O
P
O
O
O OH
O
O
N
H
O
O
O
OH H
O
O
Data from our customer Neal M. Davies,Department of
Pharmaceutical Sciences, Washington State
University, Pullman, Washington
Concentration-time profile in rat serum following
administration of deforolimus formulations
(10 mg/kg) intravenously to rats (mean SEM).
S1022 Deforolimus
Feed
Produced Independently by our customer Dr.Zhang,
Tianjin Medical University
Western blot analysis of mTOR and p-mTOR,
05DSDP\FLQDQG(YHUROOPXVZHUHDGGHG
mTOR (Mammalian target of rapamycin)
Data from Circulation Research using our product.
S1226 KU-0063794
Ku-0063794 is a specific inhibitor of mTOR, which inhibits both mTORC1 and mTORC2 with an IC50 of
approximately 10 nM, but does not suppress the activity of 76 other protein kinases or seven lipid kinases,
including Class 1 PI3Ks at 1000-fold higher concentrations. Ku-0063794 also suppressed cell growth and
induced a G1-cell-cycle arrest.
Size Price
N
N N N
O
N
O
OH
O
Mechanical stretchinduced SGK-1 activation is dependent on IGF-1R and
mTORC2 signaling pathway.mTORC2-mediated stretch-induced SGK-1
phosphorylation. SMCs infected with Ad-SGK-1 were pretreated with
PPP (10 umol/L), rapamycin (100 nmol/L),or Ku-0063794 (10 umol/L) for
30 minutes and then were subjected to stretch or IGF-1 (10 ng/mL)
for 30 minutes.

S1039 Rapamycin
RAPA administration prevented the rejection of the donor graft, accelerated post-BMT hematopoietic
recovery, and did not compromise recipient survival. In vitro, rapamycin inhibited the proliferation of primary
bone marrow cells induced by IL-3, GM-CSF, KL, or a complex mixture of factors present in cell-conditioned
media.
Synonyms:

Sirolimus, Rapamune
Size Price

S1044 Temsirolimus
Temsirolimus is a recently developed mTOR inhibitor, with improved aqueous solubility and more favorable
pharmaceutical properties compared with the parent compound rapamycin. Temsirolimus has shown
promising preclinical and early clinical antitumor activity and is currently in phase III clinical development for
the treatment of different solid tumors.
Synonyms:

Torisel, CCI-779
Size Price
HO
O
O O
O
N
O
O
O
HO
OH
O
O
O
O
O
O
O OH
O
O
N
H
O
O
O
OH H
O
O
O
OH HO

S1266 WYE-354
WYE-354,a cell-permeable pyrazolopyrimidine compound,is a potent and ATP competitive inhibitor of mTOR
,& Q0 ZLWK VLJQLILFDQW VHOHFWLYLW\ RYHU 3,. LVRIRPV !IROG :KHQ LQMHFWHG LQWR WXPRUEHDULQJ
nude mice, WYE-354 inhibited mTORC1 and mTORC2 and displayed robust antitumor activity in PTEN-null
tumors.
Size Price
N
H
O
O N
N
N
O
N
N
N
O
O
S1039 Rapamycin
Feed
Produced Independently by our customer Dr.Zhang,
Tianjin Medical University
Western blot analysis of mTOR and p-mTOR,
05DSDP\FLQDQG(YHUROOPXVZHUHDGGHG
S1226 KU-0063794
Feed
Solutions to Signal Transduction Research
56
200mg
500mg
50mg
50mg
200mg
25mg
50mg
200mg
10mg
10mg
50mg
5mg
10mg
25mg
5mg
50mg
200mg
10mg
Pl3K/A|l mTOR
S1120 Everolimus
In cells, Everolimus binds to the immunophilin FK Binding Protein-12 (FKBP-12) to generate an
immunosuppressive complex that binds to and inhibits the activation of mTOR. Inhibition of mTOR activation
results in the inhibition of T lymphocyte activation and proliferation associated with antigen and cytokine (IL-2,
IL-4, and IL-15) stimulation and the inhibition of antibody production.
Synonyms:

RAD001, SDZ-RAD, Certican, Zortress, Afinitor
Size Price
OH
O
O
O
O
N
O O
O
HO
O
O
O
O
OH

Synonyms:
ZM 252868, AG 1517, Tyrphostin AG 1517 S1009 BEZ235 Page 54
Synonyms:
ZM 252868, AG 1517, Tyrphostin AG 1517 S1360 GSK1059615 Page 53
Synonyms:

NVP-BEZ235
Synonyms:
ZM 252868, AG 1517, Tyrphostin AG 1517 S1038 PI-103 Page 53
Synonyms:
ZM 252868, AG 1517, Tyrphostin AG 1517 S1523 XL765 Page 55

Synonyms:
ZM 252868, AG 1517, Tyrphostin AG 1517 S2406 Chrysophanic acid Page 5 Synonyms: Chrysophanol, NSC 37132, NSC 646567
\l"
S1120 Everolimus
Feed
Produced Independently by our customer Dr.Zhang,
Tianjin Medical University
Western blot analysis of mTOR and p-mTOR,
05DSDP\FLQDQG(YHUROOPXVZHUHDGGHG
PDK-1 (3-phosphoinositide-dependent protein kinase)
GSK-3 (Glycogen synthase kinase)
DNA-PK (DNA-activated protein kinase)

S1205 PIK-75 HCl
3,.+\GURFKORULGHLVDSUHIHUHQWLDOSIRUPVRI3,.LQKLELWRUZLWK,&RIQ0IRU
SSSSUHVSHFWLYHO\%HVLGHVLQKLELWLRQRI3,.3,.DOVRLQKLELWHG'1$3.ZLWKDQ
IC50 of 2 nM, but not mTORC1 and mTORC2. PIK-75-mediated anti-inflammatory effects are associated with
GUDPDWLFLQKLELWLRQRI$.7SKRVSKRU\ODWLRQ,..DFWLYDWLRQDQG1)%WUDQVFULSWLRQ
Size Price

Synonyms:
ZM 252868, AG 1517, Tyrphostin AG 1517 S1523 XL765 Page 55
Synonyms:

SAR245409
N
N
Br
N
N
S
O
O
NO
2
HCl

S1263 CHIR-99021
&+,5 LV D *6. LQKLELWRU WKDW KDV DQWLSUROLIHUDWLYH DFWLYLW\ LQ YLWUR DQG LQ YLYR &+,5 LQKLELWV
GSK-3 with IC50 at 7 nM. In a series of carcinoma cell lines, the IC50 of CHIR99021 for proliferation is about
0 &+,5 GRHV QRW H[KLELW FURVVUHDFWLYLW\ DJDLQVW &'.V ZLWK IROG VHOHFWLYLW\ WRZDUG *6.
compared to CDKs .
Synonyms:

CT-99021
Size Price
N
N
HN
N
H
N Cl
Cl
HN
N N
S1075 SB 216763
6%LQKLELWHGKXPDQ*6.ZLWK,&VRIQ0ZKHQDVVD\HGLQWKHSUHVHQFHRIP0$73
6%LQKLELWHG*6.LQDQ$73FRPSHWLWLYHPDQQHU6%LQKLELWHG*6.ZLWK.LVRIQ0
,QWKHSUHVHQFHRIP0$7306%LQKLELWHG*6.NLQDVHDFWLYLW\E\,QFRQWUDVWWKLV
compounds exhibited little or no inhibition of the other 24 members of the kinase selectivity panel.
Size Price
N
NH
O
O
Cl
Cl

PHT-427 inhibited Akt and PDPK1 signaling and their downstream targets in sensitive but not resistant cells
and tumor xenografts. When given orally, PHT-427 inhibited the growth of human tumor xenografts in
LPPXQRGHILFLHQWPLFHZLWKXSWRLQKLELWLRQLQWKHPRVWVHQVLWLYHWXPRUVDQGVKRZHGJUHDWHUDFWLYLW\WKDQ
analogues with C4, C6, or C8 alkyl chains. Inhibition of PDPK1 was more closely correlated to antitumor
activity than Akt inhibition.
Size Price
S
O
H
N
O
N
N
S
S1556 PHT-427

5/
25mg
100mg
5mg
10mg
25mg
5mg
25mg
100mg
5mg
10mg
50mg
5mg
50mg
200mg
10mg
mTOR / DNA-PK / GSK-3 / PDK-l Pl3K/A|l
Toll Free:(877)796-6397 www.selleckchem.com info@selleckchem.com
Phone:+1-832-582-8158
---USA and Canada only---
ATM (Ataxia telangiectasia-mutated protein kinase)
Akt

S1092 KU-55933
KU-55933 is an ATP-competitive inhibitor, inhibits ATM with an IC50 of 13 nmol/L and a Ki of 2.2 nmol/L.
Exposure of cells to KU-55933 resulted in a significant sensitization to the cytotoxic effects of ionizing radiation
and to the DNA double-strand break-inducing chemotherapeutic agents. Derivatives of this molecule may
serve as novel radio- and chemosensitizors in clinical settings. KU-55933 is capable of suppressing the
replication of HIV-1.
Size Price

S1570 KU-60019
KU-60019 is 10-fold more effective than KU-55933 at blocking radiation-induced phosphorylation of key ATM
targets in human glioma cells. A-T fibroblasts were not radiosensitized by KU-60019, strongly suggesting that
the ATM kinase is specifically targeted. Furthermore, KU-60019 reduced basal S473 AKT phosphorylation.
Synonyms:

Torisel, CCI-779
Size Price
S
S
O
O N
O
S
O
O
N
H
N
O
N
O
O
Data from JBC. December 9, 2010 using our product.
Effect of ATM inhibitor in etoposide-induced
cell death. The cells were pretreated with
KU55933 (2 nM) for 1 hr before etoposide treatment.
S1092 KU-55933
Feed

S1558 AT7867
AT7867 is a potent and oral AKT and p70 S6 kinase inhibitor with an IC50 of 17 nM. Administration of AT7867
to athymic mice implanted with the PTEN-deficient U87MG human glioblastoma xenograft model caused
inhibition of phosphorylation of downstream substrates of both AKT and p70S6K and induction of apoptosis.
Size Price
NH
HN N
Cl

S1078 MK-2206
MK-2206, a highly selective non-ATP competitive allosteric Akt inhibitor, has nM IC50. MK-2206 is a potent
allosteric Akt inhibitor with IC50 at 8 nM, 2 mM, 65 mM for Akt1, Akt2 and Akt3 respectively. MK-2206 is
JHQHUDOO\ ZHOO WROHUDWHG DW GRVHV XS WR PJ 42' ZLWK SODVPD FRQFHQWUDWLRQV WKDW SRUWHQG DFWLYLW\ LQ
preclinical models.
Size Price
N
N
HN N
O
H
2
N
2HCl
Synonyms:
ZM 252868, AG 1517, Tyrphostin AG 1517 S1556 PHT-427 Page 56
80*FHOOVZHUHWUHDWHGZLWK00.IRU
1 hr prior to IR, and then irradiated with 6 Gy. Total
cell lysate was harvested 1 hr after IR and subjected
to Western blot analysis with the indicated antibody.
Cells without IR treatment were used as a control.
&HOOVZHUHWUHDWHGZLWKYHKLFOHFRQWURORU00.IRUKU
then irradiated with indicated dosage. 4 hr after IR, cells were fed
with drug-free medium, and incubated for another 20 hr at 37C,
after which they were trypsinized and seeded for clonogenic
survival assay. Colony-forming efficiency was determined 14 d later.
S1078 MK-2206
Feed
S1037 Perifosine
Feed
Data from Radiation Oncology 2009, 4:43 using our product.
Solutions to Signal Transduction Research
58
10mg
50mg
5mg
50mg
200mg
10mg
50mg
200mg
10mg
10mg
25mg
5mg
Pl3K/A|l ATI / AkI
5mg
10mg
25mg

S1037 Perifosine
Perifosine inhibits Akt activation, targeting cellular membranes, modulates membrane permeability,
membrane lipid composition, phospholipid metabolism, and mitogenic signal transduction, resulting in cell
differentiation and inhibition of cell growth. This agent also inhibits the anti-apoptotic MAPK pathway and
modulates the balance between the MAPK and SAPK/JNK pathways, thereby inducing apoptosis.
Synonyms:

KRX-0401, NSC 639966
Size Price
N
+
O
P
O
-
O
O
100
120
HePC
Edelfosine
ErPC
48 h treatment
(


o
f

c
o
n
t
r
o
l)
60
80
ErPC
Perifosine
C
e
ll
g
r
o
w
t
h

20
40
60
0 20 40 60 80
0
20
APL concentration ( 0
Inhibition curves in HepG2 cells exposed to
different concentrations of alkylphospholipids.
Cells growing in log-phase were incubated with
0(0)%6LQWKHDEVHQFHRUSUHVHQFHRI
different concentrations of APLs for 48 h. Cell
number was determined by the crystal violet
staining assay and expressed as percentage
of control (no addition) cells.
Data from British Journal of Pharmacology (2010),
160, 355366 using our product.
Alkylphospholipid-induced morphological
changes in HepG2 cells. Cell morphology
was examined with an inverted microscope
(20 original magnification). The morphology
RI+HS*FHOOVLQFXEDWHGZLWK0(0
FBS is shown in the absence of any addition.
Data from British Journal of Pharmacology
(2010), 160, 355366 using our product.
59
Hormones
lrlraproslal|cArdrodersardArdroder-Redu|aled0ereExpress|orPers|sl
allerTesloslerore3uppress|or:T|erapeul|clrp||cal|orsloraslral|or-Res|slarl
ProslaleCarcer.
Elahe A. Mostaghel et al. Cancer Res, 2007(67):5033
Nor-ruc|ear eslroder receplor s|dra||rd proroles card|ovascu|ar prolecl|or
oulroluler|reororeaslcarcerdroWl||rr|ce.
Ken L. Chambliss et al. J Clin Invest, 2010;120(7):23192330
Steroid hormone receptors function classically as transcription factors. More
recently, it has become apparent that steroid hormones also initiate nonge-
nomic responses via activation of a subpopulation of these receptors that are
non-nuclear. Estrogen activation of non-nuclear estrogen receptors, resulting
in rapid signaling in cell types in culture as diverse as oocytes, osteoblasts,
osteoclasts, breast cancer cells, adipocytes, and endothelial cells. However,
because it is difficult to discriminate between extranuclear-initiated and
nuclear-initiated ER actions, it remains unknown whether non-nuclear signal-
ing by ER, or any other SHR, is operative and biologically relevant in vivo.
Androgens are important mediators of transcriptional pathways controlling
the proliferation, differentiation, and apoptosis of normal and neoplastic pros-
tate cells and play a critical role in the development and progression of pros-
tate cancer. Androgen deprivation therapy (ADT) is considered standard
systemic treatment for advanced prostate cancer, and is being increasingly
used in neoadjuvant and adjuvant protocols for the treatment of high-risk,
early-stage disease.
Androgen Receptor

S1174 Ostarine
Ostarine, a non-steroidal agent, is selective androgen receptor modulator (SARM) with anabolic activity. This
agent is designed to work like testosterone, thus promoting and/or maintaining libido, fertility, prostate growth,
and muscle growth and strength. Mimicking testosterones action, this agent may increase lean body mass,
thereby ameliorating muscle wasting in the hypermetabolic state of cancer cachexia.
Synonyms:

GTx-024, MK-2866
Size Price
O
N
H
OH
F
F
F
N
O
N
S1585 17 -propionate
17 alpha-propionate is a new topical and peripherally selective androgen antagonist. Although it displayed a
strong local antiandrogenic activity in hamsters flank organ test, it did not exhibit antiandrogenic activity in rats
after subcutaneous injection, nor did it affect gonadotropins hypersecretion when injected to parabiotic rats.
Size Price
S1140 Andarine
Andarine (S-4) is an investigational selective androgen receptor modulator for treatment of conditions such as
muscle wasting, osteoporosis and benign prostatic hypertrophy, using the non-steroidal androgen antagonist
bicalutamide as a lead compound. Andarine is an orally active partial agonist for androgen receptors. It is less
potent in both anabolic and androgenic effects than other SARMs.
Size Price
O
H
H H
O
O
HO
O
O
N
H
OH
O
H
N
O
F
F
F
N
+
O
O
-

S1190 Bicalutamide
Bicalutamide is an oral non-steroidal anti-androgen used in the treatment of prostate cancer and hirsutism.
Bicalutamide acts as a pure anti-androgen by binding to the androgen receptor (AR) and preventing the
activation of the AR and subsequent upregulation of androgen responsive genes by androgenic hormones. In
addition, bicalutamide accelerates the degradation of the androgen receptor.
Synonyms:

Casodex, Cosudex, Calutide, Kalumid
Size Price

S2460 Dehydroepiandrosterone
Dehydroepiandrosterone is a 19-carbon endogenous natural steroid hormone. It is the major secretory
steroidal product of the adrenal glands and is also produced by the gonads and the brain. It acts on the
androgen receptor both directly and through its metabolites, which include androstenediol and
androstenedione, which can undergo further conversion to produce the androgen testosterone and the
estrogens estrone and estradiol.
Synonyms:

DHEA
Size Price
O
HN
OH
S O O
F
F
F
F
N
S1250 MDV3100
MDV3100 is an androgen-receptor antagonist that blocks androgens from binding to the androgen receptor
and prevents nuclear translocation and co-activator recruitment of the ligand-receptor complex. It also induces
tumour cell apoptosis, and has no agonist activity.
Size Price
N F
H
N
O
N
O
S
F
F
F
N
HO
H
O
H H
Estrogen Receptor
S1972 Tamoxifen Citrate
7DPR[LIHQ&LWUDWH1ROYDGH[LVDQHVWURJHQUHFHSWRUDQWDJRQLVWZLWKDQ,&RI0IRUWKH0&)FHOOV,Q
some tissues such as the endometrium, it behaves as an agonist, hence tamoxifen may be characterized as
a mixed agonist/antagonist. It has been the standard endocrine (anti-estrogen) therapy for hormone-positive
early breast cancer in pre-menopausal women, although aromatase inhibitors have been proposed.
Synonyms:

Nolvadex, Istubal, Valodex
Size Price

S1776 Toremifene Citrate
Toremifene Citrate is an oral selective estrogen receptor modulator which helps oppose the actions of
estrogen in the body. Chemically related to tamoxifen, toremifene is a selective estrogen receptor modulator.
This agent binds competitively to estrogen receptors, thereby interfering with estrogen activity. Toremifene
also has intrinsic estrogenic properties, which are manifested according to tissue type or species.
Synonyms:

Fareston, Acapodene
Size Price

O
N
HO2C CO2H
CO2H
OH
O
N
Cl
HO O
O
O HO
OH
OH
Solutions to Signal Transduction Research
60
50mg
200mg
10mg
50mg
200mg
10mg
100mg
200mg
50mg
200mg
250mg
100mg
50mg
200mg
10mg
50mg
200mg
10mg
10mg
25mg
5mg
50mg
100mg
25mg
lorrores Androqen RecepIor / EsIroqen RecepIor

Aromatase
S2473 Hexestrol
+H[HVWUROLVDQRYHOW\SHRIK\GUR[\VWHURLGGHK\GURJHQDVH$.5&DQG$.5&SRWHQWLQKLELWRUZLWK
,&RI0UHVSHFWLYHO\DQGH[KLELWVVWURQJDIILQLW\IRUHVWURJHQUHFHSWRUV7KHHQ]\PHZDV
potently inhibited by diethylstilbestrol, hexestrol and zearalenone. The inhibitory potencies of
GLHWK\OVWLOEHVWURO,&0KH[HVWURO,&0DQG]HDUDOHQRQH,&0IRU+6'
were lower than those for TBER1.
Synonyms:

Bibenzyl, Cycloestrol, Dihydro-stilbestro, Dihydrostilbestrol, Estra-Plex
Size Price
S1598 LY500307
/<LVDSRWHQWVHOHFWLYHHVWURJHQUHFHSWRUDJRQLVWZLWKDQ(&RIQ0,WLVVHOHFWLYHIROG
WRZDUG(5DQGVKRZVIXOODJRQLVWIXQFWLRQLQERWK(5DQG(5DVVD\VUHODWLYHHIILFDF\/<
is a drug used to treat prostate diseases.
Size Price
O
OH
HO
H
H
OH
OH
S1191 Fulvestrant
Fulvestrant is a synthetic estrogen receptor antagonist or selective estrogen receptor down-regulator.
Fulvestrant binds competitively to estrogen receptors in breast cancer cells, resulting in estrogen receptor
deformation and decreased estrogen binding. Fulvestrant is used for the treatment of hormone receptor
positive metastatic breast cancer in postmenopausal women with disease progression following
anti-estrogen therapy.
Synonyms:

Faslodex, ICI 182780
Size Price
HO
OH
S
O
F
F
F
F
F
H
H
H

S1227 Evista
Raloxifene has estrogen and tamoxifen-like effects on bone and serum cholesterol levels in ovariectomized
UDWV 5DOR[LIHQH SUHYHQWHG WKLV ORVV RI ERQH ZLWK (& PJNJGD\ IRU ERWK WKH D[LDO DQG DSSHQGLFXODU
skeleton. Raloxifene is demonstrated an extremely low IC50 value of 2.9 nM for phthalazine oxidase in human
liver cytosol.
Synonyms:

Raloxifene Hydrochloride, keoxifene
Size Price

S
HO
OH
O
N
O
.
HCl

S2466 Estriol
Estriol is a G-protein coupled estrogen receptor antagonist. It is one of the three main estrogens produced by
the human body. It may play a role in the development of breast cancer, but based on in vitro research does
appear to act as an antagonist to the G-protein coupled estrogen receptor.
Synonyms:

Oestriol
Size Price
HO
H H
H
OH
OH
6l

S1235 Letrozole
&*6PD[LPDOO\LQKLELWVHVWUDGLROSURGXFWLRQLQYLWURLQ/+VWLPXODWHGKDPVWHURYDULDQWLVVXHDW0
ZLWK DQ ,& RI 0 DQG GRHV QRW VLJQLILFDQWO\ DIIHFW SURJHVWHURQH SURGXFWLRQ XS WR 0 ,Q
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(10,000 times higher than the IC50 for estradiol production); no significant effect on corticosterone production
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Synonyms:

CGS 20267, Femara, Piroxicam Size Price
N
CN
CN
N
N

S1188 Anastrozole
Anastrozole inhibits the enzyme aromatase, which is responsible for converting androgens to estrogens.
Anastrozole binds reversibly to the aromatase enzyme through competitive inhibition. Elevated levels of
estrogens may increase the severity of breast cancer, as sex hormones can cause hyperplasia and
differentiation at estrogen receptor sites.
Synonyms:

Arimidex, AstraZeneca
Size Price
N
N
N
NC
CN

S1196 Exemestane
Exemestane is an irreversible, oral steroidal aromatase inhibitor used in the adjuvant treatment of
hormonally-responsive breast cancer in postmenopausal women. Its structure was related to the natural
substrate androstenedione and it acts as a false substrate for the aromatase enzyme. The estrogen
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found to inhibit human placental aromatase with IC50 of 42 nM.
Synonyms:

Aromasin
Size Price
O
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25mg
50mg
10mg
200mg
100mg
50mg
100mg
25mg
200mg
250mg
100mg
50mg
200mg
10mg
100mg
200mg
50mg
50mg
100mg
25mg
50mg
100mg
10mg
EsIroqen RecepIor / AromaIase lorrores
Toll Free:(877)796-6397 www.selleckchem.com info@selleckchem.com
Phone:+1-832-582-8158
---USA and Canada only---
UHGXFWDVH
S1202 Dutasteride
Dutasteride is a 5-alpha-reductase inhibitor that inhibits the conversion of testosterone into dihydrotestosterone
(DHT). Dutasteride inhibits both isoforms of 5-alpha reductase (5aR1 and 5aR2) to a similar extent (IC50
6nmol/l and 7 nmol/l, respectively), while finasteride only inhibits Type II. Dutasteride competed for binding the
/1&D3FHOO$5ZLWKDQ,&DSSUR[LPDWHO\0
Synonyms:

Avodart
Size Price

N
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S1197 Finasteride
Finasteride, a synthetic 4-azasteroid antiandrogen compound, is a specific inhibitor of steroid Type II 5
UHGXFWDVHDQLQWUDFHOOXODUHQ]\PHWKDWFRQYHUWVWKHDQGURJHQWHVWRVWHURQHLQWR'+7,QEHQLJQSURVWDWLF
hyperplasia, finasteride inhibits 5-alpha-reductase activity in epithelium for Ki of 10nM, significantly lower than
LQVWURPD.LQ0
Synonyms:

Proscar, Propecia
Size Price
N
H
O
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HN
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GPR (glycoprotein receptor)

S2149 GSK1292263
GSK1292263 is a novel GPR119 receptor agonist used for the treatment of type 2 diabetes. In the intravenous
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were reported in the GSK1292263 treatment group, compared with values in the vehicle control cohort.
Synonyms:

KRX-0401, NSC 639966
Size Price

N
S
O
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N
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Solutions to Signal Transduction Research
62
25mg
100mg
10mg
1g
200mg
50mg
200mg
10mg
lorrores 5--reducIase / GPR
63
Integrase/CCR5
NeW lrealrerl opl|ors lor ll\ sa|vade pal|erls: Ar overv|eW ol secord derera-
l|orPls,NNRTls,|rledrase|r||o|lorsardCCR5arlador|sls.
Amelia Hughes et al. J Infect, 2008(57):1e10
Preverl|or ol \ad|ra| 3ll\ Trarsr|ss|or |r R|esus Vacacues T|roud| lr||o|-
l|orolCCR5.
Michael M. Lederman et al. Science, 2004(306):485
Remarkable progress has been made since integrase was recognized as a
rational therapeutic target for the treatment of HIV infection. The mechanism
of inhibition by the specific strand-transfer inhibitors fits the model of interfa-
cial inhibitors of proteinnucleic acid interactions, as these drugs block a tran-
sition state of the integrase-DNA complex. Counterscreens with related
enzymes, such as HIV RNase H, might be useful to assess the selectivity of
integrase inhibitors, and could lead to the discovery of RNase H inhibitors that
are therapeutically active against HIV and AIDS.
The chemokine receptor CCR5 serves as an essential cofactor for HIV entry
and acquisition of infection. Thus, persons whose cells lack surface CCR5
expression because of mutation are almost completely protected from acquir-
ing HIV infection. Furthermore, viruses that utilize CCR5 predominate in early
stages of mucosal transmission, which suggests that mucosal transmission
may selectively involve CCR5. Hence, inhibition of CCR5 has been proposed
as a possible microbicide strategy for prevention of HIV infection.
64
S2004 Vicriviroc Malate
Potential of novel antiretrovirals to modulate expression and function of drug transporters in vitro.
Nadine Ccile Luise Zembruski et al. J Antimicrob Chemother, 2011;66(4): 802-812.
S2001 Elvitegravir(GS-9137)
Identification and Characterization of Persistent Intracellular Human Immunodeficiency Virus
Type 1 Integrase Strand Transfer Inhibitor Activity.
Yasuhiro Koh et al. Antimicrobial Agents and Chemotherapy, 2011; 55(1): 42-49
Susceptibility of the human retrovirus XMRV to antiretroviral inhibitors.
Robert A Smith et al. Retrovirology, 2010(7):70
Potential of novel antiretrovirals to modulate expression and function of drug transporters in vitro.
Nadine Ccile Luise Zembruski et al. J Antimicrob Chemother, 2011;66(4): 802-812.
Papers
Using Selleck Products

S2001 Elvitegravir
EVG exerted potent anti-HIV activity against not only wild-type strains but also drug-resistant clinical isolates.
EVG also showed antiviral activity against murine leukemia virus and simian immunodeficiency virus. EC50
Q0+,9,,,%+,9(+2+,952'(9*LQKLELWHGWKHLQWHJUDWLRQRIWKH+,9EDVHGYHFWRU
used as a positive control for the luciferase assay (EC50 values of 0.8 nM), as observed in the MAGI assay
with HIV-1IIIB.
Synonyms:

EVG, GS-9137, JTK-303
Size Price
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S2001 Elvitegravir
Feed
Effect of antiretrovirals and positive control rifampicin
(at 10 mmol/L) on ABCB1 function in LS180 cells after
3 and 7 days (d) of treatment. ABCB1 function was
normalized to the medium control . Data are
expressed as means+SEM for n4. **P,0.01.
Data from Journal of Antimicrobial Chemotherapy using our product.
65
S1366 BMS-707035
BMS-707035 is an HIV-1 integrase inhibitor. BMS-707035 was scheduled to be evaluated in a Phase II study
to assess the antiretroviral activity, safety, pharmacodynamics, and pharmacokinetics in 50 HIV-infected
subjects using a 10-day randomized, double-blind, placebo-controlled, ascending multiple-dose study design.
Synonyms:

BMS707035
Size Price
F
H
N
O
N
N
HO
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S2005 Raltegravir
Raltegravir is a novel HIV-1 integrase strand transfer inhibitor with potent in vitro activity against wild-type and
PXOWLFODVVUHVLVWDQW+,9YLUXVLQYLWUR,&IRU+,9LQQRUPDOKXPDQVHUXPQ05DOWHJUDYLULV
not a potent inhibitor or inducer of cytochrome P450 3A4.
Synonyms:

MK-0518, Isentress, Raltegravir potassium
Size Price
N
N
O
OH
H
N
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CCR5 (C-C chemokine receptor type 5)
5mg
10mg
50mg
5mg
25mg
100mg
Maraviroc was active (IC90) at low nanomolar concentrations against HIV-1 Ba-L when measured in a 5-day
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1.7 nM). Maraviroc inhibited MIP-1 (IC50, 3.3 nM) and RANTES (IC50, 5.2nM) binding to cell membrane
preparations of CCR5-expressing HEK-293.
Synonyms:

Selzentry, UK-427857, Celsentri
Size Price
Vicriviroc showed equally potent inhibition of the chemotactic response to MIP-1 with IC50 values below 1 nM.
Vicriviroc potently inhibited RANTES-induced signaling with mean IC50s of 4.2 nM. Vicriviroc is highly
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p-glycoprotein Substrate in vitro.
Size Price
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S2003 Maraviroc
S2004 Vicriviroc Malate
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Effect of antiretrovirals and positive control rifampicin


(at 10 mmol/L) on ABCB1 function in LS180 cells after
3 and 7 days (d) of treatment. ABCB1 function was
normalized to the medium control . Data are
expressed as means+SEM for n4. **P,0.01.
Data from Journal of Antimicrobial Chemotherapy using our product.
Integrase
50mg
200mg
10mg
50mg
200mg
10mg
10mg
50mg
5mg
CCR5 / InIeqrase lrledrase/CCR5
Toll Free:(877)796-6397 www.selleckchem.com info@selleckchem.com
Phone:+1-832-582-8158
---USA and Canada only---
66
Ererd|rdro|esolproleases|rluroursuppress|or.
Carlos Lpez-Otn et al. Nat Rev Canc, 2007(7):800-808
0ualerrarvdvrar|csardp|asl|c|lvurder||esra|||eals|oc|prole|rc|aperore
lurcl|or.
Florian Stengel et al. PNAS, 2010;107(5): 20072012
The function of intracellular proteases in signalling cascades is generally
associated with the removal of damaged or undesirable products. Lyso-
somal cysteine and aspartyl cathepsins mediate the degradation of endocy-
tosed proteins. The cysteine proteases of the caspase family function in a
tightly regulated cascade of proteolytic activities those result in apoptosis.
Conversely, extracellular proteases are thought to be actively involved in
facilitating tumorigenesis. These enzymes are frequently overexpressed in
malignant tissues, often as a result of the activation of oncogenic transcrip-
tional pathways. The prevailing view that proteases promote tumour
progression and metastasis led to the development of small-molecule inhibi-
tors for the treatment of cancer, in particular of molecules targeting matrix
metalloproteinases (MMPs) and plasminogen activators. However, clinical
trials
Small Heat Shock Proteins (sHSPs) are one of the least well understood
classes of molecular chaperones, proteins which act to prevent or reverse
improper protein associations. The importance of the sHSPs is evidenced
by their almost ubiquitous expression, the presence of multiple sHSP genes
in most organisms, and their dramatic up-regulation under stress conditions
making them among the most abundant of cellular proteins. They are impli-
cated in a range of disease states including cataract, cancer, myopathies,
motor neuropathies, and neurodegeneration.
Proteases/HSP90/HSP70
6/
S1013 Bortezomib
The clinically approved proteasome inhibitor PS-341 efficiently blocks influenza A virus and
vesicular stomatitis virus propagation by establishing an antiviral state.
Dudek SE et al. J Virol, 2010; 84(18):9439-9451.
Hepatitis B virus induces expression of antioxidant response element-regulated genes by
activation of Nrf2.
Schaedler S et al. J Biol Chem, 2010; 285(52):41074-41086
Secretory phospholipase A2-IIa is involved in prostate cancer progression and may potentially
serve as a biomarker for prostate cancer.
Zhongyun Dong et al. Carcinogenesis, 2010;31(11): 1948-1955.
Rotavirus Replication Requires a Functional Proteasome for Effective Assembly of Viroplasms
R. Contin et al. Journal of Virology, 2011;85(6):2781-2792
Papers
Using Selleck Products
Proteasome

S1013 Bortezomib
The dipeptide boronic acid inhibitor bortezomib effectively inhibits proteasome activity (Ki-0.6 nM) but has little
affinity for other proteases (e.g., for chymotrypsin, Ki=320 nM, and for thrombin, Ki=13,000 nM). The level of
apoptosis was 80% to 90% in cells treated with bortezomib plus SN-38, vs. 10% with either agent alone.
Synonyms:

Velcade, MG-341, PS-341
Size Price
10mg
N
N
N
H
O
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Solutions to Signal Transduction Research
68
Proleases/l3P90/l3PZ0 ProIeasome / HSP-/0
S2181 MLN9708
MLN9708 is an orally bioavailable second generation proteasome inhibitor with potential antineoplastic
activity. MLN9708 rapidly hydrolyzes to MLN2238, the biologically active form. It has a shorter proteasome
dissociation half-life and improved pharmacokinetics, pharmacodynamics, and antitumor activity compared
with bortezomib. MLN9708 showed a correlation between greater pharmacodynamic responses and
improved antitumor activity.
Size Price

S2180 MLN 2238
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nM. Proteasome activity was significantly inhibited in both blood and tumor following a single dose of
MLN2238 administered IV at 14 mg/kg or SC at 4 mg/kg. It is active in preclinical models of lymphoma, and
that MLN2238 has antitumor activity in a model of lymphoma that is refractory to bortezomib treatment.
Size Price

65LWRQDYLU
Ritonavir is an inhibitor of HIV protease used to treat HIV infection and AIDS. More specifically, ritonavir is
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(CYP3A4). The drugs molecular structure inhibits CYP3A4, so a low dose can be used to enhance other
protease inhibitors. This discovery has drastically reduced the adverse effects and improved the efficacy of
PIs and HAART.
Synonyms:

Norvir, Norvir Softgel
Size Price
N
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HO
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N
O
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S1380 Lopinavir
Lopinavir (ABT-378) is an antiretroviral of the protease inhibitor class. As a component of combination therapy
to treat HIV/AIDS. Inhibition of HIV-1 protease prevents cleavage of the viral polyprotein precursor and results
in the release of immature, noninfectious virions.
Synonyms:

ABT-378
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Atazanavir is an antiretroviral drug of the protease inhibitor class. Like other antiretrovirals, it is used to treat
infection of human HIV. Atazanavir is distinguished from other PIs in that it can be given once-daily and has
lesser effects on the patients lipid profile. Like other protease inhibitors, it is used only in combination with
other HIV medications.
Synonyms:

Reyataz, BMS-232632
Size Price
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N
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HSP-70 (Heat shock proteins-70)
6(OHVFORPRO
Elesclomol is a small molecule that induces apoptosis via the mitochondrial apoptotic pathway in cancer
cells by increasing oxidative stress. It is a pro-apoptotic agent that demonstrates anti-tumor activity against a
broad range of cancer cell types. It promotes apoptosis in Hs294T melanoma cells treated with 100 nmol/L
for six hours by rapidly generating reactive oxygen species and inducing the transcription of Hsp70 and
metallothionein.
Synonyms:

STA-4783
Size Price
N
S
N
H
O
N
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PJ
100mg
10mg
10mg
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S1013 Bortezomib
Feed
HER/HER2-PI3K-Akt-NF-jB signaling regulates sPLA2-IIa promoter activity. (A) Human sPLA2-IIa promoter sequence
(accession numberNC_000001). The C/EBP-binding site in the core promoter region is indicated by bold letter.
The consensus sequence of the NF-jB site located at _782 bp was indicated by underline. Most NF-jB sites appear
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Gefitinib (20 lM), Lapatinib (20 lM), CI-1033 (8 lM), LY294002(20 lM) and Bortezomib (20 lM) without or with EGF
(100 ng/ml) for 24 h. Luciferase assay was performed according to a standard protocol with Renilla luciferase as
an internal control. Data are presented as the mean (SD) of duplicate values of a representative experiment that
was independently repeated for five times.
Data from Carcinogenesis vol.31 no.11 pp.1948-1955,2010 using our products.
DPP-4 (Dipeptidyl peptidase-4)

S4002 Sitagliptin phosphate
Sitagliptin abolished sDPP-IV effects on splenic CD4+ T-cell migration whereas incretins decreased migration
of lymph node, but not splenic, CD4+ T-cells. Sitagliptin decreases migration of splenic CD4+ T-cells through
a pathway involving Rac1/VASP, whereas its inhibitory effects on the migration of lymph node CD4+ T-cells
LQYROYHLQFUHWLQDFWLYDWLRQRIWKH1)%SDWKZD\
Synonyms:

MK-0431, Januvia
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HSP-90 (Heat shock proteins-90)

S1141 17-AAG
17-AAG is a less toxic analogue of the geldanamycin which binds to Hsp90 and alters its function. This agent
displays a 100-fold higher affinity for HSP90 derived from tumor cells compared to HSP90 from normal cells.
17-AAG binds into the ATP binding pocket in Hsp90 and induces the degradation of proteins that require this
chaperone for conformational maturation. 17-AAG inhibits Akt activation.
Synonyms:

Tanespimycin, Geldanamycin
Size Price
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S1142 17-DMAG
17-DMAG, a watersoluble geldanamycin analog belonging to the class of benzoquinones, is a selective Hsp90
inhibitor. 17-DMAG binds to the N-terminal domain ATP binding site of Hsp90, inhibiting Hsp90 chaperone
activity. 17-DMAG demonstrates greater potency and water solubility than other geldanamycin analogs such
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$OYHVSLP\FLQ.2616&
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S1498 NVP-BEP800
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to the NH
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tolerability, and pharmaceutical properties, NVP-BEP800 is an exciting new oral Hsp90 inhibitor warranting
further development.
Synonyms:

9(5
Size Price

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6%,,%
BIIB021 is a novel fully synthetic inhibitor of Hsp90. It binds competitively with geldanamycin in the
ATP-binding pocket of Hsp90 (Ki=1.7nM). BIIB021 induced the degradation of Hsp90 client proteins (including
HER-2, AKT, and Raf-1) and up-regulated expression of the heat shock proteins Hsp70 and Hsp27. BIIB021
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CNF2024
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%06&*35H\DWD]=ULYDGD
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$8<9(5
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69
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nM for LAP, PuSA, aminopeptidase N, aminopeptidase B, PILSAP, LTA4 hydrolase and MetAP2,
respectively. It has demonstrated anti-tumour activity in a number of models of cancer, both as a single
agent and in synergy with cytotoxic agents such as carboplatin and paclitaxel.
Synonyms:

Tosedostat
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Bestatin
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with potent in vitro activity.
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VCH222
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HCV RNA (-3.6 logs after 48 hours from a single 100 mg) dosefollowing a single dose in patients chronically
infected with HCV genotype 1.
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S1183 Danoprevir
Danoprevir is a highly potent, orally absorbed inhibitor of the NS3/4A protease for treating chronic HCV
infections. In biochemical assays using HCV NS3/4A protease domains derived from genotypes 1b, 1a, 2, or
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5*,70152
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variants that are resistant to other protease inhibitors in development.
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treatment for hepatitis C. Specifically, it inhibits the hepatitis C virus NS3.4A serine protease.
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Proleases/l3P90/l3PZ0 AminopepIidase / HCV proIease
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Naoko Takebe et al. Nat Rev Clin Oncol, 2011(8):97-106
Notch signaling has a critical role in regulating cell to cell communication
during embryogenesis, cellular proliferation, differentiation, and apoptosis.
Notch signaling is also critical for normal hematopoiesis, breast develop-
ment, colorectal epithelial maturation, immune regulation, and neural stem
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communication between adjacent cells. The extra cellular region of the
notch receptor contains numerous epidermal growth factor like domains that
mediate interactions with notch ligands. Affinity between the notch ligand
and receptor depends on the extent of epidermal growth factor domain
fucosylation by the Fringe proteins.
The Hh signaling pathway controls tissue polarity, patterning maintenance,
and stem cell maintenance during embryonic development. Hyperactivation
of this pathway, by either mutation or deregulation, has recently been recog-
nized to cause tumorigenesis in a wide variety of tissues. Hh pathway
involvement has been observed in other types of nonmutation driven, para-
crine deregulation of signaling.
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ligands for the Frizzled transmembrane receptor. During embryogenesis,
wnt proteins direct cell fate determination at various stages of development
and their signaling acts to regulate the development of a variety of organ
systems including cardiovascular, central nervous system, renal, and lung.
In adults, wnt signaling has a key role in the regulation of tissue selfrenewal,
particularly in intestinal crypts, hair follicles, and bone growth plates.
Hedgehog
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nM. It targets the Hedgehog signaling pathway, blocking the activities of the Hedgehog-ligand cell surface
receptors PTCH and/or SMO and suppressing Hedgehog signaling. It inhibits the growth of primary
pancreatic xenografts without non-specifically inhibiting pancreatic cell proliferation in vitro and has recently
entered the clinic.
Synonyms:

HhAntag691, Vismodegib
Size Price

S1146 Cyclopamine
Cyclopamine inhibits the hedgehog signaling pathway by influencing the balance between the active and
inactive forms of the Smoothened protein. It antagonizes Smo activity by binding to its heptahelical bundle.
Thus, it can block pathway activation resulting in any of the two upstream events of Smo.
Synonyms:

11-deoxojervine
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of the destruction complex and stabilizes axin by inhibiting the poly-ADP-ribosylating enzymes tankyrase 1
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to GS and blocks activation of Notch receptors. RO4929097 inhibits Notch processing in tumor cells. This
leads to reduced expression of the Notch transcriptional target gene Hes 1. RO4929097 does not block tumor
cell proliferation or induce apoptosis but instead produces a less transformed, flattened, slower-growing
phenotype.
Synonyms:

RO-4929097
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Research on laboratory rats suggest that the soluble form of this peptide is a causative agent in the
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responsible for APP proteolysis.
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Jak/Stat
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Peter J. Murray. J Immunol, 2007(178):2623-2629.
The current model of Jak-Stat signaling holds that cytokine receptor
engagement activates the associated Jak combination, which in turn phos-
phorylates the receptor cytoplasmic domain to allow recruitment of a Stat,
which in turn is phosphorylated, dimerizes and moves to the nucleus to bind
specific sequences in the genome and activate gene expression. Cytoplas-
mic domains of cytokine receptors associate with Jaks via Jak binding sites
located close to the membrane. Regardless of the when and where cytokine
receptors and Jaks associate, their close apposition at the membrane is
required to stimulate the kinase activity of the Jak following cytokine binding.
At this stage in the activation of the pathway, we understand next to nothing
about the structural basis of the Jak-receptor interaction, how receptor intra-
cellular domains reorient upon cytokine binding and physically contact the
Jak to receive the phosphorylation modification.
Jak-mediated phosphorylation of the receptor creates binding sites for the
Src homology 2 (SH2) domains of the Stats. Stat recruitment is followed by
tyrosine, and in some cases, serine phosphorylation on key residues (by the
Jaks and other closely associated kinases) that leads to transit into the
nucleus. This brief summary of the activation of the Jak-Stat pathway omits
numerous unresolved details: the Stat monomer to dimer transition has
been questioned, as has the role of phosphorylation in dimerization and
nuclear transit. Furthermore, it is unclear how many configurations of Stat
homo- and heterocomplexes are present in cells before, during, and after
cytokine stimulation.
Stat (Signal transducer and activator of transcription)

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antibacterial and anti-inflammatory activity and acts as an antidiabetes and antiobesity agent via activation of
AMPK. It also improves cognitive impairment in Alzheimers disease transgenic mice by inhibition of
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peptide generation.
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activities. Furthermore, S31-201 inhibits growth and induces apoptosis preferentially in tumor cells that contain
persistently activated Stat3. S31-201 inhibits the expression of the Stat3-regulated genes encoding cyclin D1,
BcI-xL, and survivin and inhibits the growth of human breast tumors in vivo.
Synonyms:

16&
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tests using Ba/F3 cells expressing either wild type or V617F mutant JAK2, it potently inhibited the JAK2
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The somatic activating JAK2 V617F is detectable in most patients with polycythemia vera. Enzymatic assays
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respectively, when compared with JAK3. JAK2V617F-bearing cells were almost 10-fold more sensitive to
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Synonyms:

Tasocitinib
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accumulation of cAMP response element-binding protein bound to the Bcl-xL promoter as measured by
chromatin immunoprecipitation assay.
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Synonyms:

Tyrphostin AG490
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Ca/cAMP/Lipid
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Carine Rosse et al. Nat Rev Mol Cell Bio, 2010(11):103-112.
All PKC isoforms share a highly conserved carboxy-terminal kinase
domain that is linked by a hinge region to a more divergent amino-
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pseudosubstrate sequence that is present in the regulatory domain,
which occupies the substrate binding pocket in the otherwise func-
tional kinase domain. PKC is activated when second messengers
and/or allosteric effectors bind to its regulatory domain, typically at the
plasma membrane. This disrupts the docking of the regulatory kinase
domain, which displaces the bound pseudosubstrate region from the
active site, allowing the activation of PKC.
The modular nature of this family-PKCs have a conserved kinase
domain coupled to a series of differentially activated regulatory domains
- allows PKC activity to be deployed with spatial and temporal specificity.
It also allows PKC activity to be directed by multiple inputs, including
localized (membrane limited) second messenger production and
interaction with membrane-anchored small G proteins, scaffolds and
accessory proteins. As a result the PKC family is centrally involved in
the spatial control of signal transduction in cells.
PKC (Protein kinase C)

S1292 Chelerythrine Chloride
Chelerythrine is a benzophenanthridine alkaloid extracted from the plant Greater celandine (Chelidonium
PDMXV ,W LV D SRWHQW VHOHFWLYH DQG FHOOSHUPHDEOH 3.& LQKLELWRU ,& Q0 ,W KDV D ZLGH UDQJH RI
biological activities, including antiplatelet, anti-inflammatory, antibacterial and antitumor effects.
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Synonyms:

Sophoretin, Meletin, Quercetine
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of cultured tumor cells.
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It displays anti-inflammatory, antipyretic and analgesic effects and has a neuroprotective role against
colchicine-induced cognitive impairment and oxidative stress.
Synonyms:

Anaprox, Miranax, Naprelan, Naposin, Antalgin
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used to relieve the symptoms of rheumatoid and osteoarthritis, primary dysmenorrhoea, postoperative pain;
and acts as an analgesic, especially where there is an inflammatory component.
Synonyms:

Feldene, Roxam
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CGRP (Calcitonin gene-related peptide)
COX

60.+&O
MK3207 hydrochloride is a potent and orally bioavailable CGRP receptor antagonist. In vitro, it is a potent
antagonist of the human and rhesus CGRP receptors (Ki = 0.024 nM). In common with other CGRP receptor
antagonists MK-3207 displays lower affinity for CGRP receptors from other species including canine and
rodent.
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primary mechanism responsible for its anti-inflammatory, antipyretic, and analgesic action is inhibition of
prostaglandin synthesis by inhibition of COX, and it appears to inhibit DNA synthesis.
Synonyms:

Voltaren, Solaraze, Ecofenac, Benfofen
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and COX-2, respectively. It is used for its antipyretic, analgesic, and anti-inflammatory properties by
inhibiting COX-1 and COX-2 enzymes reversibly. Robenacoxib was COX-2 selective, diclofenac and
meloxicam were only weakly COX-2 preferential, and ketoprofen was COX-1 selective.
Synonyms:

Orudis, Oruvail, Ketoflam, Orudis KT
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antiplatelet drugs. Ibuprofen, indomethacin, and meclofenamate were potent inhibitors of the microsomal
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prostacyclin formation by aortic endothelial cells. This elevated activity was efficiently inhibited by pharmacologically
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radical scavengers.
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Ying E Zhang. Cell Res, 2009(19):128139.
Transforming growth factor (TGF) is the prototype of a family of secreted
polypeptide growth factors. To date, up to 33 TGFrelated genes have been
identified in mammalian genomes as the result of genome sequencing proj-
ects; these include bone morphogenic proteins, activin/inhibin, growth and
differentiation factors, nodal, and anti-Mllerian hormone. These cytokines
play very important roles during development, as well as in normal physi-
ological and disease processes, by regulating a wide array of cellular
processes, such as cell growth, differentiation, migration, apoptosis, and
extracellular matrix production. However, in a different cellular context, TGF
can also promote tumor growth because it is able to induce changes in tran-
scriptional activities that re-program epithelial cells into mesenchymal cells,
thereby facilitating tumor metastasis and invasion.
Over a decade ago, genetic studies in worms and fruitflies uncovered a
group of genes, later dubbed as Smads, which appear to play a crucial role
in mediating the intracellular responses to TGF and/or its related factors.
Subsequent biochemical characterization demonstrated that Smads are
transcription factors that constantly shuttle between the cytoplasm and the
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changes that allow direct binding of Smads and their phosphorylation by the
kinase activities of the cytoplasmic domains of the type I receptors. This
results in the accumulation of Smads in the nucleus to regulate target gene
transcription. The identification of Smads elated the field of TGF signaling,
but it also instigated a perplexing dilemma in terms of reconciling the diverse
functions of the TGF family with the simplicity of the Smad signaling model.
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kinase pathways or on components of the signaling.
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PJ
200mg
10mg
T0F-/3rad TGF-
8l
GPCR
0prole|r-coup|edreceplorr|croarravslordrudd|scoverv.
Fang Y et al. Drug Discov Today, 2003;8(16):755-761.
GPCRs (Guanine Nucleotide BindingProtein Coupled Receptors) comprise
large and diverse gene families in fungi, plants, and the animal kingdom.
Also termed serpentine receptors, GPCRs are polytopic membrane proteins
that share a common structure with seven transmembrane segments, but
sequence similarity is minimal among the most distant GPCRs. Their principal
function is to transmit information about the extracellular environment to the
interior of the cell, and they do this by interacting with the G-proteins. GPCRs
recognize a variety of ligands and stimuli including peptide and non-peptide
hormones and neurotransmitters, chemokines, prostanoids and proteinases,
biogenic amines, nucleosides, lipids, growth factors, odorant molecules and
light. These receptors affect the generation of small molecules that act as
intracellular mediators or second messengers, and can regulate a highly
interconnected network of biochemical routes. The intracellular signaling
pathways activated by GPCR signaling include cAMP/ PKA pathway,
Ca
2+
/PKC pathway, Ca
2+
/NFAT pathway, PLC pathway, PTK pathway,
PKC/MEK pathway, p43/p44MAPK pathway, p38 MAP pathway, PI3K pathway,
NO-cGMP pathway, Rho pathway, NF-KappaB pathway and JAK/ STAT
pathway.
Vasopressin Receptor

S1990 Capsaicin
Capsaicin is an active component of chili peppers. Capsaicin, as a member of the vanilloid family, binds to a
receptor called the vanilloid receptor subtype 1. By binding to the VR1 receptor, the capsaicin molecule
produces the same sensation that excessive heat or abrasive damage would cause, explaining why the
spiciness of capsaicin is described as a burning sensation.
Synonyms:

Qutenza, Vanilloid
Size Price
HO
O
H
N
O
200mg
500mg
100mg
Angiotensin Receptor


S1578 Candesartan
Candesartan is an angiotensin II receptor antagonist with an IC50 of 15 g/kg. It reduced the risk of developing
hypertension by nearly two-thirds during this period. In the last two years of the study, all participants were
switched to placebo. By the end of the study, candesartan had significantly reduced the risk of hypertension,
by more than 15%.
Synonyms:

Atacand, Blopress, Amias, Ratacand
Size Price

S1587 Olmesartan
Olmesartan is an angiotensin II receptor antagonist with an IC50 of 7.7 nM. Olmesartan works by blocking the
binding of angiotensin II to the AT1 receptors in vascular muscle; it is therefore independent of angiotensin II
synthesis pathways, unlike ACE inhibitors. By blocking binding rather than synthesis of angiotensin II,
olmesartan inhibits the negative regulatory feedback on renin secretion.
Synonyms:

Benicar, Olmetec
Size Price

S1539 Tasosartan
Angiotensin II receptor antagonists are selective blockers of the renin-angiotensin system and represent an
alternative to angiotensin-converting enzyme inhibitors in the treatment of hypertension. Tasosartan is a newly
developed nonpeptide AT1 receptor blocker. IC50s were determined from log-dose response curves by
nonlinear regression analysis.
Synonyms:

DB01349
Size Price
10mg
50mg
100mg
S1894 Valsartan
Valsartan is an angiotensin II receptor antagonist with IC50 of ranging from 39.5 to116 M. By blocking the
action of angiotensin, valsartan dilates blood vessels and reduces blood pressure. In the Value trial, the
angiotensin II receptor blocker valsartan produced a statistically significant 19% (p=0.02) relative increase in
the prespecified secondary end point of myocardial infarction compared with amlodipine.
Synonyms:

Diovan
Size Price
25mg
50mg
10mg
25mg
100mg
10mg
N
N
N HN
N
N
OH
O
O
N
N
N
N
HN
N
HO
O
O
O
O
O
N N
N
N
N
H
N
N
O
N
O OH
O
H
N
N HN
N
CB1 Receptor
S1595 AM 281
AM 281 is a potent, selective CB1 cannabinoid receptor antagonist with an Ki of 12 nM and 4200 nM for CB1
and CB2 receptors respectively. It increases locomotor activity following systemic administration in vivo.
Size Price
Cl
Cl
N
N
O
NH
N
O
I
10mg
50mg
100mg
Solutions to Signal Transduction Research
82
0PCR Vasopressin RecepIor / AnqioIensin RecepIor / CBl RecepIor
25mg
50mg
10mg
5mg
10mg
1mg
100mg
200mg
25mg
100mg
200mg
50mg


S2509 Sotalol HCl
Sotalol(Betapace) is a non-selective beta blocker and a potassium channel blocker with an IC50 of 43 M.
Sotalol definitely distinctly located binding site to interfere with K
+
permeation; both enantiomers associated
with a rate close to 510
5
/mol/ sec with the open pore thereby flicker-blocking cardiac K
+
/ATP channels.
Synonyms:

Betapace, Betapace AF, Berlex Laboratories, Sotalex
Size Price
NH
S
O
O
HN
HO
HCl
Smoothened
mGluR2/mGluR3
25mg
50mg
10mg
Synonyms:

NVP-LDE225
S2151 LDE225
LDE225(NVP-LDE225) is a novel and specific, orally bioavailable Smo inhibitor with an IC50 of 11 nM. It has
been shown to potentially inhibit Hh-and Smo-dependent proliferation in vivo. It also induced the regression of
SUHIRUPHGEDVDORLGOHVLRQVZLWKDQ,&RIQPROODQGDOPRVWFRPSOHWHUHJUHVVLRQDWPROO
Size Price
N
N O HN
O
F
3
CO
50mg
200mg
10mg
S6001 LY2140023
LY404039 is a selective metabotropic glutamate receptor group II subtypes mGluR2 and mGluR3 agonist with
Ki of 149 and 92nM for mGlu2 and mGlu3, respectively.Functional activity of LY404039 at group II and group
III mGlu receptors is measured by the inhibition of forskolin-stimulated cAMP formation. It is nanomolar potent
agonists at human mGlu2 and mGlu3 receptors, as indicated by the inhibition of forskolin-stimulated cAMP
formation (LY404039: mGlu2, EC50 =23 nM; mGlu3, EC50 = 48 nM).
Size Price
UHFHSWRU

S1549 Nebivolol HCl
1HELYROROLVDUHFHSWRUEORFNHUZLWKDQ,&RI0,WKDVQLWULFR[LGHSRWHQWLDWLQJYDVRGLODWRU\HIIHFW
used in treatment of hypertension. Nebivolol was compared with DETA-NO and SNAP, two nitric oxide donor
agents, and DFMO, a known inhibitor of ODC. All four test agents inhibited RASMC proliferation in a
concentration-dependent manner, with nebivolol being the most potent (IC(50) = 4.5 microM).
Synonyms:

Bystolic, R-67145
Size Price
O
F
H
N O
OH
H H
F
OH
HCl

S1206 Bisoprolol Fumarate
%LVRSURORO LV D EHWDDGUHQRFHSWRU EORFNLQJ GUXJ EHWDEORFNHU 0RUH VSHFLILFDOO\ LW LV D VHOHFWLYH W\SH
adrenergic receptor blocker. Bisoprolol can be used to treat cardiovascular diseases such as hypertension,
coronary heart disease, arrhythmias, is chemic heart diseases and treatment of myocardial infarction after the
acute event.
Synonyms:

Zebeta
Size Price
O
OH
NH
O
O
OH
OH
O
O
83
0PCR
l recepIor / SmooIhened
S
HOOC
H
H
COOH
H
NH
2
O
O
Toll Free:(877)796-6397 www.selleckchem.com info@selleckchem.com
+1-832-582-8158
---USA and Canada only---
Feed
S600 LY2140023
Top:The glutamate agonist LY404,039 inhibited the
binding of 2 nM [
3
H]domperidone on dopamine D2
Long
receptors (in
CHO cells). The inhibition occurred in two concentration phases of
LY404,039, with 15.5% inhibition for the high-affinity phase. 120
mM NaCl present. Data points are mean values (with SE; n = 3).
The inhibition of 15.5% occurred at D2
High
receptors, all of which
were converted to low-affinity D2Low receptors in the presence of
GN (200 M guanylylimidodiphosphate). The dissociation constant,
K
i
High
, of LY404,039 was 8.2 1 nM. Nonspecific binding was
defined in the presence of 10 M S-sulpiride. Bottom: LY404,039
stimulated the incorporation of [
35
6@*736LQWRGRSDPLQH'
Long
receptors with 50% incorporation occurring at 80 15 nM. The
maximum amount of stimulation was 43% of that caused by 10 M
dopamine. The stimulation was blocked by 10 M S-sulpiride. Data
points are means SE (n = 3).
Data from SYNAPSE 63:935939 (2009), using our product.
Synonyms:

LY404039
84
Ion Channel
lorc|arre|s|rdeal|ardd|llererl|al|orolproslalecarcerce||s.
N Prevarskaya et al. Cell Death Differ, 2007(14):12951304;
Historically, the first important role ascribed to plasma membrane ion chan-
nels, over 60 years ago, was their participation in cellular electrogenesis and
electrical excitability. However, numerous subsequent studies have firmly
established the contribution of ion channels to virtually all basic cellular
behaviors, including such crucial ones for maintaining tissue homeostasis
as proliferation, differentiation, and apoptosis. The major mechanisms via
which ion channels contribute to these crucial processes include: providing
the influx of essential signaling ions, regulating cell volume, and maintaining
membrane potential. Malignant transformation of cells resulting from
enhanced proliferation, aberrant differentiation, and impaired ability to die is
the prime reason for abnormal tissue growth, which can eventually turn into
uncontrolled expansion and invasion, characteristic of cancer. Such trans-
formation is often accompanied by changes in ion channel expression and,
consequently, by abnormal progression of the cellular responses with which
they are involved.
S1747 Nimodipine
Nimodipine inhibits the transmembrane influx of calcium ions in response to depolarization in smooth muscle
cells, thereby inhibiting vascular smooth muscle contraction and inducing vasodilatation. Nimodipine has a
greater effect on cerebral arteries than on peripheral smooth muscle cells and myocardial cells, probably
because this agent can cross the blood brain barrier due to its lipophilic nature.
Synonyms:

Nimotop
Size Price
S1748 Nisoldipine
Nisoldipine is a calcium channel blocker. It works by affecting the movement of calcium into the cells of the
heart and blood vessels. As a result, it relaxes blood vessels and increases the supply of blood and oxygen to
the heart while reducing its workload.
Synonyms:

Sular, Zadipina, Bay k 5552, Baymycard
Size Price
S2491 Nitrendipine
Nitrendipine is a dihydropyridine calcium channel blocker with an IC50 of 95 nM. Nitrendipine and BRL 38227
cause concentration-related inhibitions of the inositol phosphate response to histamine (100 M). Similar
maximal inhibitions were caused by each agent (55-58%). Inhibitory effect of BRL 38227 was reduced in
potency (IC50 = 5.5 M), but not magnitude, in the presence of glibenclamide (0.5 M).
Size Price
H
N
NO2
O
O
O
O
H
N
NO2
O
O
O
O
O
N
+
O
-
O
N
H
O
O
O
O
CFTR
S1144 VX-770
VX-770 is a CFTR potentiator with an IC50 of 43 38 nM. In recombinant cells VX-770 increased CFTR
channel open probability in both the F508del processing mutation and the G551D gating mutation. VX-770
also increased Cl- secretion. Furthermore, VX-770 reduced excessive Na+ and fluid absorption to prevent
dehydration of the apical surface and increased cilia beating in these epithelial cultures.
Size Price
OH
H
N
O
H
N
O
Calcium channel
S1885 Felodipine
Felodipine is a calcium channel blocker with an IC50 of 3 M for the formyl-Met-Leu-Phe-induced cytosolic
calcium increase. It is a drug used to control hypertension. Grapefruit juice contains bergamottin which is
found to have an inhibiting effect over this enzyme and as a result the bioavailability of the drug increases,
raising the risk for abnormal side effects.
Synonyms:

Plendil, Renedil, Feloday
Size Price
S1662 Isradipine
,VUDGLSLQHLVDFDOFLXPFKDQQHOEORFNHUZLWKDQ,&RI01RUPDOKXPDQJLQJLYDOILEUREODVW*LQFHOOV
were used. The [Ca
2+
]
i
was measured with the Ca
2+
-sensitive fluorescent dye fura-2/AM. Changes in the
fluorescence intensity of fura-2 in the cells were recorded with a video-imaging analysis system.
Synonyms:

DynaCirc, Prescal, PN-200-110, Clivoten, Esradin
Size Price
S1813 Amlodipine besylate
Amlodipine besylate is a long-acting dihydropyridine calcium channel blocker. Amlodipine is a calcium channel
blocking agent. The decrease in intracellular calcium inhibits the contractile processes of the myocardial
smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the
myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure and decreased
afterload.
Synonyms:

Istin, Norvasc
Size Price
S1905 Amlodipine
Amlodipine is a long-acting calcium channel blocker with an IC50 of 1.9 nM used as an anti-hypertensive and
in the treatment of angina. Amlodipine acts by relaxing the smooth muscle in the arterial wall, decreasing total
peripheral resistance and hence reducing blood pressure; in angina it increases blood flow to the heart
muscle.
Synonyms:

Istin, Norvasc
Size Price
N
H
O
O
Cl
O
O
Cl
HN
O
O
O
H2N
O O
Cl
S
HO
O
O
N
O
N
N
H
O
O
O
O
85
HN
O
O
O
H
2
N
O O
Cl
10mg
50mg
200mg
10mg
25mg
50mg
10mg
50mg
100mg
25mg
50mg
100mg
10mg
25mg
50mg
200mg
500mg
1g
25mg
50mg
100mg
10mg
25mg
50mg
lorC|arre|
CFTR / Calcium channel
Toll Free:(877)796-6397 www.selleckchem.com info@selleckchem.com
+1-832-582-8158
---USA and Canada only---
S1354 Lansoprazole
Lansoprazole is a proton-pump inhibitor which prevents the stomach from producing gastric acid.It is used to
treat duodenal and gastric ulcers, erosive esophagitis, and gastroesophageal reflux diseas. Lansoprazole is
also used to treat Zollinger-Ellison syndrome, which is a condition where the stomach produces too much acid.
Synonyms:

Prevacid, Prevacid NapraPAC, Prevacid SoluTab
Size Price
S1389 Omeprazole
Omeprazole is a proton pump inhibitor used in the treatment of dyspepsia, peptic ulcer disease (PUD),
gastroesophageal reflux disease (GORD/GERD), laryngopharyngeal reflux, and Zollinger-Ellison syndrome.
Synonyms:

Losec, Omesec, Prilosec, Zegerid
Size Price
N
H
N
S
O N
O
F
F F
N
H
N
O
S
O
N
O
Proton pump
S1293 Cilnidipine
Cilnidipine is a calcium channel blocker. It is a dual blocker of L-type voltage-gated calcium channels in
vascular smooth muscle and N-type calcium channels in sympathetic nerve terminals that supply blood
vessels.
Synonyms:

FRC 8653
Size Price
NO2
H
N
O
O
O
O
O
S1743 Esomeprazole magnesium
Esomeprazole magnesium is a proton pump inhibitor which reduces gastric acid secretion through inhibition
of H+/K+-ATPase in gastric parietal cells. By inhibiting the functioning of this enzyme, the drug prevents
formation of gastric acid.
Synonyms:

Nexium
Size Price
N
O
S
O
N
N
-
N
O
S
O
N
N
-
O
O
Mg
++
Solutions to Signal Transduction Research
86
20mg
50mg
500mg
10mg
25mg
50mg
1g
5g
10g
500mg
1g
5g
lorC|arre| Calcium / ProIon pump
8/
Cytochrome P450
Cvloc|roreP150p|arracoderel|csardcarcer.
C Rodriguez-Antona et al. Oncogene, 2006(25):16791691
The cytochromes P-450 (CYP) are a superfamily of heme-thiolate enzymes,
some of which play major roles in the metabolism of drugs and other xenobi-
otics, although endogenous compounds can also be their substrates. In
humans and other mammalian species, CYP1, CYP2 and CYP3 families are
primarily associated with the Phase 1 metabolism of exogenous compounds.
Over 90% of all drug metabolism in man is P-450-mediated
The cytochromes P450 (CYPs) are key enzymes in cancer formation and
cancer treatment. They mediate the metabolic activation of numerous precar-
cinogens and participate in the inactivation and activation of anticancer
drugs. Since all CYPs that metabolize xenobiotics are polymorphic, much
emphasis has been put on the investigation of a relationship between the
distribution of specific variant CYP alleles and risk for different types of
cancer, but a consistent view does not yet exist.
S2140 Cytochrome P450 14a-demethylase inhibitor 1f
Cytochrome P450 14a-demethylase inhibitor 1f exhibits higher activity against nearly all fungi tested except
Aspergillus fumigates than fluconazole. It shows higher activity than that of the other positive controls. Its
MIC80 against Candida tropicalis and Candida Krusei is 62.5 ng/ml.
Size Price
S2141 Cytochrome P450 14a-demethylase inhibitor 1g
Cytochrome P450 14a-demethylase inhibitor 1g is exhibits higher activity against nearly all fungi tested except
Aspergillus fumigates than fluconazole. It shows higher activity than that of the other positive controls. Its
MIC80 against Cryptococcus neoformans, Candida parapsilosis and Candida tropicalis and Trichophyton
rubrum is 0.25 g/ml.
Size Price
F
F
N
N
N
OH
N
Cl
F
F
N
N
N
OH
N
Cl
14a-demethylase
S2135 Cytochrome P450 14a-demethylase inhibitor 1a
&\WRFKURPH3DGHPHWK\ODVHLQKLELWRUDLVDQDQWLIXQJDODJHQWDQGDQDQDORJRIXFRQD]ROHZLWKDQ
MIC80 of 3.9 ng/ml against Candida albicans and Microsporum gypseum. It shows 128 times higher activity
than that of fluconazole against Candida albicans and also shows higher activity than that of the other positive
controls.
Size Price
S2136 Cytochrome P450 14a-demethylase inhibitor 1b
Cytochrome P450 14a-demethylase inhibitor 1b exhibits higher activity against nearly all fungi tested except
Aspergillus fumigates than fluconazole. It shows 128 times higher activity than that of fluconazole against
Candida albicans and also shows higher activity than that of the other positive controls. Its MIC80 against
Candida parapsilosis and Candida Krusei is 15.6 ng/ml.
Size Price
F
F
N
N
N
OH
N
F
F
N
N
N
OH
N
F

S2137 Cytochrome P450 14a-demethylase inhibitor 1c
Cytochrome P450 14a-demethylase inhibitor 1c exhibits higher activity against nearly all fungi tested except
Aspergillus fumigates than fluconazole. It shows higher activity than that of the other positive controls. Its
MIC80 against Candida parapsilosis and Candida Krusei is 62.5 ng/ml.
Size Price
S2138 Cytochrome P450 14a-demethylase inhibitor 1d
Cytochrome P450 14a-demethylase inhibitor 1d exhibits higher activity against nearly all fungi tested except
Aspergillus fumigates than fluconazole. It shows higher activity than that of the other positive controls. Its
MIC80 against Candida parapsilosis, Candida Krusei , Cryptococcus neoformans and Candida tropicalis is
62.5 ng/ml.
Size Price
S2139 Cytochrome P450 14a-demethylase inhibitor 1e
Cytochrome P450 14a-demethylase inhibitor 1e exhibits higher activity against nearly all fungi tested except
Aspergillus fumigates than fluconazole. It shows higher activity than that of the other positive controls. Its
MIC80 against Candida parapsilosis, Candida Krusei and Microsporum gypseum is 62.5 ng/ml.
Size Price
F
F
N
N
N
OH
N
F
F
F
N
N
N
OH
N
F
F


F
N
N
N
OH
N
Cl
S1123 Abiraterone
Abiraterone is a steroidal CYP17 inhibitor. In preclinical studies, Abiraterone has demonstrated the ability to
selectively inhibit the target enzyme (IC50 4 nM for hydroxylase), resulting in nhibition of testosterone
production in both the adrenals and the testes.
Synonyms:

CB-7598, CB7598
Size Price
N
H
HO
H H
Solutions to Signal Transduction Research
88
10mg
50mg
200mg
10mg
50mg
200mg
10mg
50mg
200mg
10mg
50mg
200mg
10mg
50mg
200mg
10mg
50mg
200mg
10mg
50mg
200mg
10mg
50mg
200mg
Cvloc|roreP150 l4a-demeIhylase
F
F
N
N
N
OH
N
NO2
F
F
N
N
N
OH
N
Cl
Cl
S2147 Cytochrome P450 14a-demethylase inhibitor 1m
Cytochrome P450 14a-demethylase inhibitor 1m exhibits higher activity against nearly all fungi tested except
Aspergillus fumigates than fluconazole. It shows higher activity than that of the other positive controls. Its
MIC80 against Microsporum gypseum is 62.5 g/ml.
Size Price
S2148 Cytochrome P450 14a-demethylase inhibitor 1n
Cytochrome P450 14a-demethylase inhibitor 1n exhibits higher activity against nearly all fungi tested except
Aspergillus fumigates than fluconazole. It shows higher activity than that of the other positive controls. Its
MIC80 against Candida tropicalis and Candida Krusei and is 0.25 g/ml.
Size Price
S2146 Cytochrome P450 14a-demethylase inhibitor 1l
Cytochrome P450 14a-demethylase inhibitor 1L exhibits higher activity against nearly all fungi tested except
Aspergillus fumigates than fluconazole. It shows higher activity than that of the other positive controls. Its
MIC80 against Microsporum gypseum is 15.6 g/ml.
Size Price
F
F
N
N
N
OH
N
S2142 Cytochrome P450 14a-demethylase inhibitor 1h
Cytochrome P450 14a-demethylase inhibitor 1h exhibits higher activity against nearly all fungi tested except
Aspergillus fumigates than fluconazole. It shows higher activity than that of the other positive controls. Its
MIC80 against Cryptococcus neoformans, Candida parapsilosis, Candida Krusei and Trichophyto nrubrum is
0.25 g/ml.
Size Price
F
F
N
N
N
OH
N
Br
S2143 Cytochrome P450 14a-demethylase inhibitor 1i
Cytochrome P450 14a-demethylase inhibitor 1i exhibits higher activity against nearly all fungi tested except
Aspergillus fumigates than fluconazole. It shows higher activity than that of the other positive controls. Its
MIC80 against Cryptococcus neoformans, Candida parapsilosis, Candida tropicalis, and Trichophyto nrubrum
is 0.25 g/ml.
Size Price
S2144 Cytochrome P450 14a-demethylase inhibitor 1j
Cytochrome P450 14a-demethylase inhibitor 1j exhibits higher activity against nearly all fungi tested except
Aspergillus fumigates than fluconazole. It shows higher activity than that of the other positive controls. Its
MIC80 against Candida albicans is 15.6 g/ml.
Size Price
S2145 Cytochrome P450 14a-demethylase inhibitor 1k
Cytochrome P450 14a-demethylase inhibitor 1k exhibits higher activity against nearly all fungi tested except
Aspergillus fumigates than fluconazole. It shows higher activity than that of the other positive controls. Its
MIC80 against Microsporum gypseum is 15.6 g/ml.
Size Price
F
F
N
N
N
OH
N
Br
F
F
N
N
N
OH
N
F
F
N
N
N
OH
N
89
10mg
50mg
200mg
10mg
50mg
200mg
10mg
25mg
50mg
10mg
25mg
50mg
10mg
25mg
50mg
10mg
25mg
50mg
10mg
25mg
50mg
Cvloc|roreP150 l4a-demeIhylase
Toll Free:(877)796-6397 www.selleckchem.com info@selleckchem.com
+1-832-582-8158
---USA and Canada only---
90
Others
FaclorXa..........................................................................................
31PReceplor..................................................................................
sPLA2...............................................................................................
P-d|vcoprole|r...................................................................................
Reverselrarscr|plase.......................................................................
Xarl||reox|dase..............................................................................
3erolor|rreupla|e...........................................................................
P|osp|od|eslerase...........................................................................
Acelv|c|o||reslerase.........................................................................
Adrererd|creceplor..........................................................................
l|slar|re..........................................................................................
0A8A................................................................................................
91
91
91
91
92
93
93
91
95
9
9Z
98
P-glycoprotein
S1481 LY335979
LY335979 is a selective Pgp inhibitor with a Ki of 59 nM, and does not modulate MRP-mediated resistance by
MRP1 and MRP2. LY335979 significantly enhanced the survival of mice implanted with Pgp-expressing
murine leukemia (P388/ADR) when administered in combination with either daunorubicin, doxorubicin or
etoposide. LY335979 was without significant effect on the pharmacokinetics of these anticancer agents.
Synonyms:

Zosuquidar trihydrochloride, RS-33295-198
Size Price
N
O
N
N
OH
F F
HCl HCl HCl
Factor Xa
S1P Receptor Agonist
S5002 FTY720
Synonyms:

Fingolimod, Gilenia
Page 12

S1593 Apixaban
Apixaban is a direct factor Xa inhibitor with an IC50 of 0.220.02 M. It is a compound being investigated as
an anticoagulant. Apixaban has similar affinity for human and rabbit factor Xa (FXa). Oxidative metabolism of
[14C] apixaban by liver microsomes was approximately 20 times faster in rabbits than in rats or humans.
Synonyms:

BMS-562247-01
Size Price


S1571 BMS-740808
BMS-740808 is a highly potent, selective, efficacious, and orally bioavailable blood coagulation factor Xa
LQKLELWRUZLWKD.LRIS0,WKDVDUDSLGRQVHWRILQKLELWLRQ0VLQYLWURVHOHFWLYH!IROG
over other proteases), efficacious in the AVShunt thrombosis model, and orally bioavailable inhibitor of blood
coagulation factor Xa.
Size Price

S3002 Rivaroxaban
Rivaroxaban inhibits clot-associated,free FXa activity, and prothrombinase activity, in addition, it reduces
thrombin generation. The activated serine protease FXa plays a central role in the blood coagulation cascade.
%$<VKRZHGDVLPLODUDIILQLW\WRSXULILHGKXPDQDQGUDEELW);D,&DQG0
respectively), but was less potent against purified rat FXa.
Synonyms:

Xarelto, BAY 59-7939
Size Price
N N
N
O
H2N O
N
O
O
N
N
N
O
O
N
NH2
F3C
N
OH
N O
O
N
O
O
NH
O
S
Cl
sPLA2
S1110 LY315920
LY315920 is a selective inhibitor of human, group IIA, nonpancreatic secretory PLA2. In a chromogenic
isolated enzyme assay, Varespladib inhibited sPLA2 activity with an IC50 of 9.6 1 nM or 7.3 10
-6
mole
fraction. The use of Varespladib have a beneficial effect in preventing various inflammatory disease states.
Size Price
N
O
H
2
N
O
O
O
OH
9l
10mg
50mg
200mg
10mg
50mg
200mg
10mg
50mg
200mg
10mg
50mg
200mg
10mg
50mg
0l|ers FacIor Xa / SlP RecepIor AqonisI / sPLA2 / P-qlycoproIein
Toll Free:(877)796-6397 www.selleckchem.com info@selleckchem.com
+1-832-582-8158
---USA and Canada only---
Reverse Transcriptase


S1704 Emtricitabine
(PWULFLWDELQH LV D QXFOHRVLGH UHYHUVH WUDQVFULSWDVH LQKLELWRU ZLWK DQ ,& RI 0 7KH GUXJ ZRUNV E\
inhibiting reverse transcriptase, the enzyme that copies HIV RNA into new viral DNA. Both of these changes
are associated with healthier immune systems and decreased likelihood of serious illness.
Synonyms:

Emtriva, Coviracil, Truvada, Atripla
Size Price

S1400 Tenofovir Disoproxil Fumarate
Tenofovir disoproxil fumarate belongs to a class of antiretroviral drugs known as nucleotide analogue reverse
transcriptase inhibitors (nRTIs), which block reverse transcriptase, an enzyme crucial to viral production in
HIV-infected people.
Synonyms:

Viread
Size Price

S1398 Stavudine
Stavudine is a nucleoside analog reverse transcriptase inhibitor active against HIV. Stavudine is an analog of
thymidine. It is phosphorylated by cellular kinases into active triphosphate. Stavudine triphosphate inhibits the
HIV reverse transcriptase by competing with natural substrate, thymidine triphosphate. It also causes
termination of DNA synthesis by incorporating into it.
Synonyms:

Zerit
Size Price
S1742 Nevirapine
Nevirapine is a non-nucleoside reverse transcriptase inhibitor used to treat HIV-1 infection and AIDS.
Nevirapine is not effective against HIV-2, as the pocket of the HIV-2 reverse transcriptase has a different
structure, which confers intrinsic resistance to the NNRTI class.
Synonyms:

Viramune, BI-RG 587
Size Price
N N
H
2
N
F
O
O
S
OH
O
HO
N
N
H
O
O
N
N
N
N
NH2
O
P
O
O
O
O
O
O
O
O
O
CO2H
HO2C
N
NH
N N
O
S1718 Adefovir Dipivoxil
Adefovir Dipivoxil works by blocking reverse transcriptase, an enzyme that is crucial for the HBV to reproduce
in the body. It is approved for the treatment of chronic hepatitis B in adults with evidence of active viral
replication and either evidence of persistent elevations in serum aminotransferases or histologically active
disease.
Synonyms:

Bis-POM PMEA, Preveon, Hepsera
Size Price
S1702 Didanosine
'LGDQRVLQHLVDUHYHUVHWUDQVFULSWDVHLQKLELWRUZLWKDQ,&RI0,WLVHIIHFWLYHDJDLQVW+,9DQGXVHGLQ
combination with other antiretroviral drug therapy as part of highly active antiretroviral therapy.
Synonyms:

2',3'-dideoxyinosine, DDI, NSC 612049
Size Price
S1401 Tenofovir
TENOFOVIR is a drug used to treat human HIV infection. Tenofovir is an antiviral drug called a nucleotide
reverse transcriptase inhibitor. Tenofovir may reduce the amount of HIV in the blood and increase the number
of CD4 cells (T-cells) in the blood. Tenofovir is used in combination with other drugs to treat the HIV virus.
Tenofovir will not cure or prevent HIV infection or AIDS.
Synonyms:

Viread
Size Price
N
N
N
N
NH
2
O
PO
3
H
2
O
HO
N
N
N
NH
O
N
N
N
N
O P
O
O
O O
O
NH2
O
O
Solutions to Signal Transduction Research
92
10mg
25mg
50mg
25mg
50mg
100mg
5mg
20mg
50mg
50mg
100mg
500mg
5mg
25mg
50mg
S1706 Lamivudine
Lamivudine is a potent nucleoside analog reverse transcriptase inhibitor with an IC50 of 2.7 mM. The
pH-driven uptake of TEA by BBMV (pHin = 6.0, pHout = 7.5) was inhibited by lamivudine. The IC50 value for
the concentration-dependent effect of lamivudine on TEA uptake by BBMV after 30 s was 2668 M whereas
IC50 values for cimetidine and trimethoprim were < 2.5 M and < 25 M, respectively.
Synonyms:

3TC, Zeffix, Heptovir, Epivir, Epivir-HBV
Size Price
N N
O
H2N
O
S
OH 25mg
50mg
100mg
10mg
50mg
100mg
5mg
10mg
25mg
0l|ers Reverse TranscripIase
Serotonin reuptake


S1372 Citalopram HBr
Citalopram (Celexa, Cipramil) is an antidepressant drug of the selective serotonin reuptake inhibitor (SSRI)
class. Most often used to treat major depression, it is also used on occasion in the treatment of body
dysmorphic disorder, anxiety, and panic disorder.
Synonyms:

Celexa, Cipramil
Size Price

S1869 Dapoxetine HCl
Dapoxetine hydrochloride is a short-acting novel selective serotonin reuptake inhibitor marketed for the
treatment of premature ejaculation in men. The treatment of PE consists of primarily off-label use of oral
selective serotonin reuptake inhibitors (SSRIs) via either on-demand or daily delivery.
Synonyms:

Priligy, LY-210448 hydrochloride
Size Price

S1336 Fluvoxamine maleate
Fluvoxamine is a potent and selective serotonin reuptake inhibitor with approximately 100-fold affinity for the
serotonin transporter over the norepinephrine transporter. It has negligible affinity for the dopamine transporter
RUDQ\RWKHUUHFHSWRUZLWKWKHVROHH[FHSWLRQRIWKHVLJPDUHFHSWRU
Synonyms:

Luvox
Size Price

S1333 Fluoxetine HCl
Fluoxetine is an antidepressant of the selective serotonin reuptake inhibitor class. Fluoxetine is used to the
treatment of major depression (including pediatric depression), obsessive-compulsive disorder, bulimia
nervosa, panic disorder and premenstrual dysphoric disorder.
Synonyms:

Prozac, Sarafem
Size Price
S1436 Tianeptine sodium
Tianeptine is a selective serotonin reuptake enhancer drug used for treating major depressive episodes.
Unlike conventional tricyclic antidepressants, tianeptine enhances the reuptake of serotonin instead of
inhibiting it, opposite to the action of SSRIs. Moreover, it enhances the extracellular concentration of dopamine
in the nucleus accumbens and modulates the D2 and D3 dopamine receptors. There is also action on the
NMDA and AMPA receptors.
Synonyms:

Stablon, Coaxil, Tatinol
Size Price

F
O
N
N
HBr
O
O
O
N
HCl
O
F
F
F
N
H
HCl
F
F
F
N
O
NH2
O
CO2H
CO2H
S
N
O
O
NH
O
NaO
Cl

S1719 Zalcitabine
Zalcitabine is a NARTI. It is a derivative of the naturally existing deoxycytidine, made by replacing the hydroxyl
group in position 3 with hydrogen. This active metabolite works as a substrate for HIV reverse transcriptase,
and also by incorporation into the viral DNA, hence terminating the chain elongation due to the missing
hydroxyl group.
Synonyms:

Hivid, Dideoxycytidine, NSC 606170
Size Price
HO
O
N
N
NH2
O
Xanthine oxidase
S1631 Allopurinol Sodium
Allopurinol Sodium (Aloprim) is a xanthine oxidase inhibitor with an IC50 of 7.820.12 M. It is a structural
isomer of hypoxanthine. It inhibits conversion of xanthine to uric acid and increases reutilization of
hypoxanthine and xanthine for nucleic acid synthesis, thereby decreasing uric acid levels in both serum and
urine.
Synonyms:

Lopurin, Zyloprim, Aloprim
Size Price
S1630 Allopurinol
Allopurinol (Zyloprim) is a xanthine oxidase inhibitor with an IC50 of 7.820.12 M. The inhibition of XO activity
by 6-aminopurine (IC50=10.890.13 M) and its analogues was compared with that by allopurinol
(IC50=7.820.12 M). Among these analogues, 2-chloro-6(methylamino) purine (IC50=10.190.10 M) and
4-aminopyrazolo[3,4-d] pyrimidine (IC50=30.260.23 M) were found to be potent inhibitors of XO.
Synonyms:

Aloprim, Lopurin, Zyloprim
Size Price
N
H
N
HN
N
O
Na
+
N
N
N
H
NH
O
S1547 Febuxostat
Febuxostat is a non-purine selective XAO inhibitor with IC50 of 114 -210 nM. It works by non-competitively
blocking the channel leading to the active site on xanthine oxidase. Xanthine oxidase is needed to
successively oxidize both hypoxanthine and xanthine to uric acid. Hence, febuxostat inhibits xanthine oxidase,
therefore reducing production of uric acid.
Synonyms:

TMX-67, Adenuric, Uloric
Size Price
N
O
S
N OH
O
93
100mg
200mg
500mg
10mg
50mg
200mg
10mg
50mg
200mg
10mg
25mg
50mg
25mg
50mg
200mg
25mg
50mg
100mg
25mg
50mg
100mg
100mg
200mg
1g
10mg
50mg
100mg
0l|ers
Reverse TranscripIase / XanIhine oxidase / SeroIonin reupIake
Toll Free:(877)796-6397 www.selleckchem.com info@selleckchem.com
+1-832-582-8158
---USA and Canada only---
Phosphodiesterase


S1673 Aminophylline
Aminophylline is a competitive nonselective phosphodiesterase inhibitor with an IC50 of 0.12 mM and also a
nonselective adenosine receptor antagonist. It is a bronchodilator. It is a compound of the bronchodilator
theophylline with ethylenediamine in 2:1 ratio.
Synonyms: Somopphyllin, Aminocadol, Phyllocontin, Truphylline Size Price

S1455 Cilomilast
&LORPLODVWLVDPRQJWKHILUVWRIDQHZJHQHUDWLRQRI3'(LQKLELWRUV.LQ0&LORPLODVWLQKLELWV+3'(
DQG/3'(FDWDO\WLFDFWLYLW\ZLWKHTXDOSRWHQF\.LQ06%DQGUROLSUDPDUHHTXLSRWHQWDJDLQVW
LPDE4, but Cilomilast is 100-fold less potent against HPDE4. This profile suggests that Cilomilast(SB-207499)
retain the anti-inflammatory activity of rolipram yet have a decreased tendency to produce side effects.
Synonyms: Ariflo, SB-207499
Size Price


S2312 Icariin
,FDULLQ LV D IODYRQRO DQG 3'( LQKLELWRU ZLWK ,& RI DQG 0 IRU 3'($ $ DQG $
respectively. It enhances the production of bioactive nitric oxide, as well as mimicking the effects of
testosterone. It also shows antioxidant, antidepressant and nootropic effects.
Size Price
S2320 Luteolin
Luteolin is a PDE4 inhibitor and a general phosphodiesterase inhibitor, and an Interleukin 6 inhibitor. It
significantly reversed the xylazine/ketamine-induced anesthesia in mice. Luteolin is thought to play an
important role in the human body as an antioxidant, a free radical scavenger, an agent in the prevention of
inflammation, a promoter of carbohydrate metabolism, and an immune system modulator.
Synonyms:

3',4',5,7-Tetrahydroxyflavone, Luteoline, Luteolol
Size Price
S2484 Milrinone
Milrinone is a potent and selective phosphodiesterase 3 inhibitor with an IC50 of 0.42 M for the inhibition of
FIII PDE. It potentiates the effect of cAMP. It also enhances relaxation of the left ventricle by increasing
Ca2+-ATPase activity on the cardiac sarcoplasmic reticulum. It is used in the management of heart failure only
when conventional treatment with vasodilators and diuretics has proven insufficient.
Synonyms:

Primacor
Size Price
S1895 Dipyridamole
Dipyridamole, a phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes
and vascular endothelial cells. Dipyridamole also potentiates the antiaggregating action of prostacyclin.
Dipyridamole likely inhibits both adenosine deaminase and phosphodiesterase, preventing the degradation of
cAMP, an inhibitor of platelet function.
Synonyms: Permole, Persantine, Dipyridan
Size Price
N
N
N
N
N N
N
N
OH
OH
HO
OH
N
N
N
H
N
O
O
N
N
N
H
N
O
O
H2N
NH2
O
O
NC
COOH
H
O
OH
O O
O
O
OH
OH
HO
OH
OH
OH
OH O
O
N
N
H
O
N
O HO
OH O
OH
OH
S2131 Roflumilast
Roflumilast is a selective, long-acting the enzyme PDE-4 inhibitor with an IC50 of 0.8 nM. It has
antiinflammatory effects. Roflumilast produced several dose-limiting side effects including nausea, diarrhoea
and headache, and development is continuing in an attempt to minimise the incidence of side effects while
retaining clinical efficacy.
Synonyms:

Daxas
Size Price
S1430 Rolipram
Rolipram is a PDE4-inhibitor. Like most PDE4-inhibitors, it is an anti-inflammatory drug. Rolipram is being
studied as a possible alternative to current antidepressants. Recent studies show that rolipram may have
antipsychotic effects.
Synonyms:

ZK 62711, SB 95952, ME-3167, Adeo
Size Price

S2127 S-(+)-Rolipram
S-(+)-Rolipram is a less active enantiomer of the PDE4 inhibitor with an EC50 of 1.0 M. It is an
anti-inflammatory drug. Rolipram is being studied as a possible alternative to current antidepressants. Recent
studies show that rolipram may have antipsychotic effects. It displays activity 10-fold less than R-rolipram at
inhibition of PDE IV.
Size Price
N
Cl
Cl
N
H
O
O
O F
F
O
NH
O
O
O
O
NH
O
Solutions to Signal Transduction Research
94
10mg
25mg
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5mg
10mg
25mg
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50mg
100mg
5mg
10mg
25mg
10mg
25mg
50mg
10mg
50mg
200mg
10mg
25mg
100mg
25mg
50mg
100mg
10mg
25mg
50mg
0l|ers PhosphodiesIerase

Acetylcholinesterase


S2251 (-)-Huperzine A
+XSHU]LQH$LVDQ$FHW\OFKROLQHVWHUDVHLQKLELWRUDQG10'$UHFHSWRUDQWDJRQLVWZLWKDQ,&RI0IRU
NMDA-induced current. The IC50 values of huperzine A were neither altered by changing the concentrations
RIJO\FLQH0DQGS+LQWKHH[WHUQDOVROXWLRQQRUE\DGGLWLRQRI=Q0DQGGLWKLRWKUHLWRO
(5 mM) to the external solution.
Size Price
NH
2
H
HN
O

S2340 Papaverine HCl
Papaverine hydrochloride, an alkaloid found in opium but not closely related to the other opium alkaloids in its
structure or pharmacological actions. It is a direct-acting smooth muscle relaxant used in the treatment of
impotence and as a vasodilator, especially for cerebral vasodilation. It apparently can inhibit
phosphodiesterases and it may have direct actions on calcium channels.
Synonyms:

Pavabid, Artegodan, Cepaverin, Optenyl, Pavagrant
Size Price

S1431 Sildenafil citrate
Sildenafil citrate is a drug used to treat erectile dysfunction and pulmonary arterial hypertension. It acts by
inhibiting cGMP specific phosphodiesterase type 5, an enzyme that regulates blood flow in the penis. Sildenafil
has been the prime treatment for erectile dysfunction.
Synonyms:

Viagra, Revatio
Size Price
S1504 Dyphylline
Dyphylline is a xanthine derivative with bronchodilator and vasodilator effects. It is used in the treatment of
respiratory disorders like asthma, cardiac dyspnea, and bronchitis. It acts as an adenosine receptor antagonist
and phosphodiesterase inhibitor.
Synonyms:

Neothylline, Lufyllin, diprophylline
Size Price
N
O
O
O
O
HCl
S
N
O
O
N
O
N
HN
O
N
N
OH
OH
OH
O
HO
O
O
N
N
N
N
O
O
OH
OH
95
S2515 Vardenafil
Vardenafil is a new type PDE inhibitor with IC50 of 0.7 and 180 nM for PDE5 and PDE1, respectively. Chronic
vardenafil treatment improves erectile function via structural maintenance of penile corpora cavernosa in rats
with acute arteriogenic erectile dysfunction.
Synonyms:

Vivanza
Size Price

S1512 Tadalafil
Tadalafil is a PDE inhibitor. Tadalafil, which has demonstrated a high level of selectivity for PDE5 over the
other phosphodiesterases, has shown efficacy in improving erectile function and sexual satisfaction in phase
III trials. PDE11A3, PDE11A2, and PDE11A1, which contain progressively shorter N-termini, were more
sensitive than PDE11A4 to inhibition by Tadalafil.
Synonyms:

Cialis, GF 196960, IC 351, ICOS 351
Size Price
S1550 Pimobendan
Pimobendan is a Ca2+ sensitizer with an IC50 of 26 M and a selective phosphodiesterase III inhibitor with an
IC50 of <1 M. Pimobendan decreased the catecholamine secretion (IC(50)=29.5 M) elicited by carbachol,
an agonist at nicotinic acetylcholine receptors, but not that elicited by veratridine, an activator of
voltage-dependent Na(+) channels, or by high K+, an activator of voltage-dependent Ca2+ channels.
Synonyms:

Vetmedin, Acardi, pimobendane
Size Price
N
N
S
O O
O
N
N
HN
O
N
N
NH
HN N
O
O
N
N
N
H
O
O
O
O
H
50mg
100mg
500mg
10mg
25mg
50mg
100mg
200mg
500mg
10mg
50mg
10mg
25mg
50mg
1mg
2.5mg
5mg
0l|ers PhosphodiesIerase / AceIylcholinesIerase
S2462 Donepezil HCl
Donepezil hydrochloride is a centrally acting reversible acetylcholinesterase inhibitor with an IC50 of 12.3 nM.
Its main therapeutic use is in the treatment of Alzheimers disease where it is used to increase levels of cortical
acetylcholine. It has an oral bioavailability of 100% and easily crosses the blood-brain barrier.
Synonyms:

Aricept
Size Price
O
O
O
N
HCl
10mg
25mg
50mg
S2285 Cryptotanshinone Page 74
Toll Free:(877)796-6397 www.selleckchem.com info@selleckchem.com
+1-832-582-8158
---USA and Canada only---
10mg
25mg
50mg
S1608 Pyridostigmine Bromide
Pyridostigmine Bromide is a parasympathomimetic and a reversible cholinesterase inhibitor. It is a quaternary
carbamate inhibitor of cholinesterase that does not cross the blood-brain barrier, and it is taken daily in
anticipation of an attack, which carbamylates about 30% of peripheral cholinesterase enzyme.
Synonyms:

Mestinon, Regono
Size Price
N
+
O N
O
Br
-
Adrenergic receptor
Solutions to Signal Transduction Research
96
10mg
50mg
100mg

S2516 Xylazine
;\OD]LQHLVFODVVRIDGUHQHUJLFUHFHSWRUDJRQLVW,WDFWVRQSUHV\QDSWLFDQGSRVWV\QDSWLFUHFHSWRUVRIWKH
central and peripheral nervous systems as an a 2-adrenergic agonist. It is used primarily for sedation,
anesthesia, analgesia and muscle relaxation.
Synonyms:

Rompun
Size Price
S2507 Salbutamol sulfate
6DOEXWDPROLVDVKRUWDFWLQJDGUHQHUJLFUHFHSWRUDJRQLVWZLWKDQ,&RI07KHWHUWLDU\EXW\OJURXS
LQVDOEXWDPROPDNHVLWPRUHVHOHFWLYHIRUUHFHSWRUV7KHGUXJLVVROGDVDUDFHPLFPL[WXUHPDLQO\EHFDXVH
the S isomer blocks metabolism pathways while the R isomer shows activity.
Synonyms:

Albuterol, Ventolin, Aerolin, Ventorlin, Asthalin, Asthavent
Size Price
OH
OH
OH
H
N
H
2
SO
4
H
N
S
N

S1206 Bisoprolol Fumarate
Synonyms:

Zebeta
Page 83

S2458 Clonidine HCl
&ORQLGLQH K\GURFKORULGH LV D GLUHFWDFWLQJ DGUHQHUJLF DJRQLVW ZLWK DQ (' RI PJNJ ,W KDV
VSHFLILFLW\ WRZDUGV WKH SUHV\QDSWLF UHFHSWRUV LQ WKH YDVRPRWRU FHQWHU LQ WKH EUDLQVWHP 7KLV ELQGLQJ
decreases presynaptic calcium levels, and inhibits the release of norepinephrine.
Synonyms:

Catapres,Clonidine
Size Price

S2126 Naftopidil
1DIWRSLGLO ELQGV VSHFLILFDOO\ WR DGUHQRFHSWRUV 7KH .L YDOXHV LV Q0 IRU QDIWRSLGLO 7KH DIILQLWLHV RI
QDIWRSLGLOWRDQGEHWDDGUHQRFHSWRUVLWHVDUHYHU\ORZ!DQG!Q01DIWRSLGLOUHOD[HVDRUWLF
strips precontracted with norepinephrine concentration-dependently, and it shifts the concentration-response
curve of norepinephrine in a parallel manner to the right.
Synonyms:

Flivas, KT-611, BM-15275, Avishot
Size Price

S1324 Doxazosin mesylate
'R[D]RVLQPHV\ODWHDTXLQD]ROLQHFRPSRXQGLVDQDGUHQHUJLFUHFHSWRUEORFNHUXVHGWRWUHDWKLJKEORRG
SUHVVXUHDQGEHQLJQSURVWDWLFK\SHUSODVLD,WLQKLELWVWKHELQGLQJRIQRUHSLQHSKULQHWRWKHUHFHSWRUVRQWKH
membrane of vascular smooth muscle cells.
Synonyms:

Cardura, Carduran, Cardura XL
Size Price
S2495 Oxymetazoline HCl
2[\PHWD]ROLQHK\GURFKORULGHLVDQDQGDGUHQHUJLFUHFHSWRUDJRQLVW,WLVDYDLODEOHRYHUWKHFRXQWHUDV
a topical decongestant in nasal sprays. The action of oxymetazoline results in vasoconstriction. In addition,
the local application of the drug also results in vasoconstriction due to its action on endothelial postsynaptic
UHFHSWRUV
Size Price

Cl
H
N
Cl
HN
N
HCl
N
N
H2N
O
O
N N
O
O O
S
O HO
O
O N
OH
N
O
HO N
H
N
HCl
10mg
25mg
50mg
100mg
200mg
1g
25mg
50mg
100mg
25mg
50mg
100mg
100mg
200mg
250mg
10mg
25mg
50mg
0l|ers AceIylcholinesIerase / Adrenerqic recepIor
Histamine


S1291 Cetirizine di HCl
Cetirizine, an antihistamine, is a major metabolite of hydroxyzine, and a racemic selective H1 receptor inverse
agonist used in the treatment of allergies, hay fever, angioedema, and urticaria.
Synonyms:

Zyrtec, Reactine
Size Price


S1816 Chlorpheniramine maleate
Chlorpheniramine maleatea histamine H1 antagonist used in allergic reactions, hay fever, rhinitis, urticaria,
and asthma. It is one of the most widely used of the classical antihistaminics. It blocks the action of
endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by
histamine.
Synonyms:

Chlor-Trimeton, Allergisan, Piriton, Teldrin
Size Price
S1845 Cimetidine
Cimetidine, a histamine congener, it competitively inhibits histamine binding to histamine H2 receptors. It
inhibits gastric acid secretion, as well as pepsin and gastrins output. It also blocks the activity of cytochrome
P-450 which might explain proposals for use in neoadjuvant therapy.
Synonyms:

Tagamet, SKF-92334, Tratul, Tametin, Dyspamet, Acinil
Size Price
S1847 Clemastine Fumarate
Clemastine is a selective histamine H1 antagonist and binds to the histamine H1 receptor. It blocks the action
of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on
by histamine.
Synonyms:

Tavist, Xolamin, Agasten, Aloginan
Size Price
N
Cl
N
O
OH
O
2HCl
N HN
S
HN
N
HN
CN
Cl
O N
HO
OH
O
O
N
N
Cl
C4H4O4
S1245 Dimebon
Latrepirdine is an antihistamine drug. Latrepirdine operates through multiple mechanisms of action, blocking
the action of neurotoxic beta-amyloid proteins, inhibiting L-type calcium channels, modulating the action of
AMPA and NMDA glutamate receptors, exerting a neuroprotective effect by blocking a novel target that
LQYROYHVPLWRFKRQGULDOSRUHVEORFNLQJDQXPEHURIRWKHUUHFHSWRUVLQFOXGLQJDGUHQHUJLF+7&+7$
and 5-HT6.
Synonyms:

Latrepirdine, Dimebolin
Size Price
S1866 Diphenhydramine HCl
Diphenhydramine hydrochloride, a histamine H1 antagonist used as an antiemetic, antitussive, for dermatoses
and pruritus. Diphenhydramine competes with free histamine for binding at HA-receptor sites. This
antagonizes the effects of histamine on HA-receptors, leading to a reduction of the negative symptoms
brought on by histamine HA-receptor binding.
Synonyms:

Benadryl, Dimedrol, Daedalon
Size Price

S1358 Loratadine
Loratadine is an antihistamine drug used to treat allergies, and marketed for its non-sedating properties.
Loratadine is a tricyclic antihistamine, which selectively antagonizes peripheral histamine H1-receptors.
Loratadine has a long-lasting effect.
Synonyms:

Alavert, Claritin
Size Price


S1890 Nizatidine
Nizatidine is a histamine H2-receptor antagonist with and IC50 of 6.7 nM for AChE. The relative anti-AChE
SRWHQF\ZDVLQWKHIROORZLQJRUGHUQHRVWLJPLQH!QL]DWLGLQH!FLPHWLGLQH!!IDPRWLGLQH7KHLQKLELWLRQRI$&K(
by nizatidine was noncompetitive, with a Ki value of 7.4 x 10 nM.
Synonyms:

Tazac, Axid, Axid AR
Size Price

N
N
N
2HCl
O
N
HCl
S
N
S
HN
CHNO
2
HN
N
N
Cl
N
O O
9/
200mg
500mg
1g
100mg
200mg
500mg
200mg
500mg
1g
25mg
50mg
100mg
5mg
25mg
100mg
10mg
25mg
50mg
100mg
1g
5g
10mg
50mg
200mg
0l|ers HisIamine anIaqonisI
Toll Free:(877)796-6397 www.selleckchem.com info@selleckchem.com
+1-832-582-8158
---USA and Canada only---
S2494 Olopatadine HCl
Olopatadine hydrochloride is a histamine blocker and mast cell stabilizer with an IC50 of 559 M for the
release of histamine. Evaluation of the interaction of olopatadine with histamine receptors revealed a relatively
high affinity for the H1 receptor (Ki = 31.6 nM, pKi = 7.5 0.1) but lower affinities for H2 receptors (Ki = 100
M, pKi = 4.0 0.19) and H3 receptors (Ki = 79.4 M, pKi = 4.1 0.16,).
Synonyms:

Opatanol, Pataday, Patanase, Allelock
Size Price
S1801 Ranitidine HCl
Ranitidine hydrochloride(Zantac) is a histamine H2-receptor antagonist with IC50 of 3.3 1.4 M. It inhibits
stomach acid production. It is also used alongside fexofenadine and other antihistamines for the treatment of
skin conditions such as hives. It has 10% the affinity that cimetidine has to CYP450 so it causes fewer side
effects, but other H2 blockers famotidine and nizatidine have no CYP450 significant interactions.
Synonyms:

Zantac, AH 19065, Azantac
Size Price
O
N
OH
O
HCl
N
O
S
H
N
NO
2
H
N
HCl
GABA

S1338 Gabapentin HCl
Gabapentin Hydrochloride is a GABA analogue. It was used for the treatment of epilepsy, and currently,
gabapentin is widely used to relieve pain, especially neuropathic pain.
Synonyms:

Gabarone, Neurontin
Size Price


S2133 Gabapentin
Gabapentin is a pharmaceutical drug, specifically a GABA analogue. It was originally developed for the
treatment of epilepsy, and currently, gabapentin is widely used to relieve pain, especially neuropathic pain.
Synonyms:

Fanatrex, Gabarone, Neurontin
Size Price
S1589 SKF 89976A HCl
6.) $ LV D *$%$ WUDQVSRUWHU W\SH LQKLELWRU ZLWK ,& RI DQG 0 IRU K*$7
rGAT-2, hGAT-3 and hBGT-1 respectively. It is selective for GAT-1. It inhibits transport current competitively
.L 0 DQG WUDQVPLWWHUJDWHG FXUUHQW QRQFRPSHWLWLYHO\ .L Q0 $EOH WR SDVV WKH %%% DIWHU
systemic administration and is active in vivo.
Size Price

S1329 Etomidate
Etomidate is a GABAA receptors agonist at GABAA receptors. Etomidate is a short acting intravenous
anaesthetic agent used for the induction of general anaesthesia and for sedation for short procedures such as
reduction of dislocated joints and cardioversion.
Synonyms:

Amidate
Size Price
S2269 Baicalin
Baicalin is a known prolyl endopeptidase inhibitor and affects the GABA receptors. It is a flavone, a type of
flavonoid. It is found in several species in the genus Scutellaria, including Scutellaria lateriflora. There are 10
mg/g baicalin in Scutellaria galericulata leaves. It is a component of Chinese medicinal herb Huang-chin.
Size Price
O
O
HO
O
OH O
OH
HO
HO
O OH
NH
2
OH O

NH
2
OH O
.
HCl
N
O
OH
HCl
N
N
O
O
Solutions to Signal Transduction Research
98
25mg
50mg
100mg
10mg
25mg
50mg
10mg
25mg
50mg
10mg
50mg
500mg
1g
10g
25mg
50mg
100mg
10mg
50mg
100mg
0l|ers HisIamine anIaqonisI / GABA
99
Peptide inhibitors
C0K.................................................................................................
8c|-2.................................................................................................
p38VAPK.........................................................................................
JNK...................................................................................................
0xvloc|rreceplor..............................................................................
0|vcoprole|rreceplor........................................................................
vasopress|rreceplor.........................................................................
LlRlR/0rRlR................................................................................
PTlR.................................................................................................
Ve|arocorl|r-1receplor....................................................................
PKC...................................................................................................
3NAPR...............................................................................................
NKR...................................................................................................
80KR/K0R........................................................................................
TRlreceplor......................................................................................
CRFreceplor......................................................................................
0RF-R................................................................................................
0|re||rreceplor..................................................................................
lac|v||r|rNK1receplor.....................................................................
Ard|olers|rreceplor..........................................................................
3ecrel|rreceplor................................................................................
33TR.................................................................................................
0C0R................................................................................................
0l3R.................................................................................................
100
100
100
100
100
101
101
101
102
103
103
103
103
103
101
101
101
101
105
105
105
105
105
10
Solutions to Signal Transduction Research
l00
Pepl|des CDK / Bcl-2 / p38 IAPK / 1NK / OxyIocin recepIor
Size Price
1mg

P1029 Oxytocin
Oxytocin is a nine amino acid peptide that is synthesized in hypothalamic neurons and transported down
axons of the posterior pituitary for secretion into blood. It is released in large amounts after distension of the
cervix and vagina during labor, and after stimulation of the nipples, facilitating birth and breastfeeding.
Synonyms:

Pitocin, Syntocinon
Size Price
P1025 Atosiban
Atosiban is an inhibitor of the hormones oxytocin (IC50=59 nM) and vasopressin. Atosiban had nanomolar
affinity for rat and human oxytocin receptors but was much less selective vs. vasopressin receptors. Atosiban
was found to be 70-fold more potent at human recombinant V1a receptors than at human OT receptors and
was only 10-fold and 30-fold selective for human OT vs. human V1b and V2 receptors.
Synonyms:

Tractocile, Antocin
Size Price
P1081 JIP-1(153-163) Page 100
c[Mpa-D-Tyr(Et)-Ile-Thr-Asn-
Cys]-Pro-Orn-Gly-NH
2
AcOH
Cys-Tyr-Ile-Gln-Asn-Cys-
Pro-Leu-Gly-NH
2
AcOH
(Disulfide bridge: Cys1-Cys6)
JNK
Oxytocin receptor
CDK
Bcl-2
p38 MAPK
P1077 [Ala92]-p16 (84-103)
[Ala92]-p16 (84-103) is a peptide derived from the tumor suppressor protein p16. [Ala92]-p16 (84-103) can
bind to cdk6. The aberrant p16 RNA transcripts encoded key peptides (amino acids 84-103) involved in
binding with CDK4. Over-expression of these aberrant p16 RNA transcripts resulted in decreased cell
proliferation rate, enlargement of cell shape and reduced level of hyperphosphorylated forms of pRb.
Asp-Ala-Ala-Arg-Glu-Gly-Phe-
Leu-Ala-Thr-Leu-Val-Val-Leu-
His-Arg-Gly-ArgAcOH
1mg
Size Price
Size Price
Size Price
1mg
1mg

P1078 Bax inhibitor peptide P5
Bax inhibitor peptide P5 is a cell-permeable synthetic Bax peptide inhibitor. Bax inhibitor peptide P5 is
designed from Ku70 that is suggested to suppress the mitochondrial translocation of Bax. Bax inhibitor peptide
P5 inhibits Bax-mediated apoptosis in vitro.

P1080 Bax inhibitor peptide
Bax inhibitor peptide,negative control is a negative control peptide for the Bax inhibitor peptides V5 and P5,
which inhibit Bax translocation to mitochondria and Bax-mediated apoptosis in vitro.

P1079 Bax inhibitor peptide V5
Bax inhibitor peptide V5 is a cell-permeable synthetic Bax peptide inhibitor. Bax inhibitor peptide V5 is
designed from Ku70 that is suggested to suppress the mitochondrial translocation of Bax. Bax inhibitor
peptide V5 inhibits Bax-mediated apoptosis in vitro.

Pro-Met-Leu-Lys-GluAcOH
Val-Pro-Met-Leu-LysAcOH
Ile-Pro-Met-Ile-LysAcOH
Size Price
1mg
P1081 JIP-1(153-163)
Peptide inhibitor of c-Jun N-terminal kinase (JNK), based on residues 153-163 of JNK-interacting protein-1
(JIP-1). Binds to JNK with affinity in the micromolar range and minimally inhibits p38 and ERK.
Arg-Pro-Lys-Arg-Pro-Thr-Thr-
Leu-Asn-Leu-Phe-NH
2
AcOH
100mg
500mg
1g
100mg
500mg
1g
l0l
Pepl|des
GlycoproIein recepIor / Arqinine vasopressin recepIor
/ GonadoIropin-releasinq hormone recepIor
Gonadotropin-releasing hormone receptor
P1028 Ornipressin
Ornipressin is a vasopressin agonist specific for the V1 receptor. It is a synthetic analog of vasopressin with
ornithine in position 8 of the cyclic nonapeptide.
P1034 Terlipressin
Terlipressin is similar to a naturally occurring hormone present in the body, known as ADH or vasopressin and
contains 12 amino acids. Terlipressin is an analogue of vasopressin used as a vasoactive drug in the
management of hypotension. Terlipressin is also a nonselective agonist of V1 vasopressin receptors, but it has
a longer half-life and a lower incidence of ischaemic complications.
Synonyms:

Glypressin, Haemopressin, Variquel
P1020 Vasopressin
Vasopressin is a synthetic analog of the pituitary hormone. Its action is mediated by the vasopressin receptor
V2. It has prolonged antidiuretic activity, but little pressor effects. It also modulates levels of circulating factor
VIII and von willebrand factor.
Synonyms:

Arginine vasopressin, argipressin, antidiuretic hormone
Synonyms:
ZM 252868, AG 1517, Tyrphostin AG 1517 P1015 Lypressin
Lypressin is a synthetic analog of the pituitary hormone, argipressin. Its action is mediated by the vasopressin
receptor V2. It modulates levels of circulating Factor VIII and Von Willebrand factor. Lypressin is a hormone
used to prevent or control the frequent urination, increased thirst, and loss of water associated with diabetes
insipidus.
Synonyms:

Lysine Vasopressin
25mg
500mg
1g
P1023 Alarelin
Alarelin is a synthetical nonapeptide similarity of LHRH. It is used to treat endmometriosis. The inhibitory effect
RI/+5+$PVPLJKWEHHTXDOWRWKDWRIRYDULRWRP\DWDGRVHRIJNJG7KHPD[LPXPLQKLELWRU\HIIHFWRQ
cell proliferation was achieved a concentration of 10 mM and it acted in a dose-dependent manner.
Size Price
Size Price
Size Price
Size Price
Size Price
Synonyms:

BMS-582664
1mg
5mg
500mg
P1019 Cetrorelix Acetate
Cetrorelix Acetate is a potent GnRH receptor antagonist (KD = 0.2 nM, IC50 = 1.2 nM). It suppresses
production of luteinizing hormone and follicle-stimulating hormone from the pituitary gland, which inhibits
ovulation and exhibits antiproliferative effects and displays efficacy against hormone-sensitive cancers in vivo.
Size Price
Synonyms:

Cetrotide
Glycoprotein receptor
Arginine vasopressin receptor



P1011 Eptifibatide
Eptifibatide is a 6 amino acid peptide. It binds to the platelet receptor glycoprotein IIb/IIIa of human platelets
and inhibits platelet aggregation. One study shows the inhibition of platelet glycoprotein IIb/IIIa in acute
coronary syndromes.
Synonyms:

Integrilin
Size Price
P1025 Atosiban
Synonyms:

Tractocile, Antocin
Page 100
P1047 Felypressin
Felypressin is a Vasopressin 1 agonist and a peptide containing eight amino acids including cystine. It will thus
have affects at all Arginine vasopressin receptor 1As. It will, however, have its main physiological effects on
vascular SMCs due to the form in which it is administered.
Synonyms:

felypressin, Octapressin
Size Price
c(Map-Har-Gly-Asp-Trp-
Pro-Cys)-NH
2
AcOH
H-[Cys-Phe-Phe-Gln-Asn-
Cys]-Pro-Lys-Gly-NH
2
AcOH
Cys-Tyr-Phe-Gln-Asn-Cys-
Pro-Lys-Gly-NH
2
AcOH
(Disulfide bridge: Cys1-Cys6)
c[Cys-Tyr-Phe-Gln-Asn-Cys]-
Orn-Gly-NH
2
AcOH
Cly-Cly-Gly-Cys-Tyr-Phe-
Gln-Asn-Cys-Pro-Lys-Gly-
NH
2
AcOH
Cys-Tyr-Phe-Gln-Asn-Cys-
Pro-Arg-Gly-NH
2
AcOH
(Disulfide bridge: Cys1-Cys5)
Glp-His-Trp-Ser-Tyr-D-Ala-
Leu-Pro-NHEtAcOH
Ac-3-(2-naphthyl)-D-Ala-4-
Chloro-D-Phe-3(3-pyridyl)-
D-Ala-Ser-Tyr-D-Cit-Leu-
Arg-Pro-D-Ala-NH
2
100mg
500mg
1g
100mg
500mg
1g
25mg
100mg
500mg
100mg
500mg
1g
100mg
500mg
1g
10mg
25mg
50mg
Toll Free:(877)796-6397 www.selleckchem.com info@selleckchem.com
+1-832-582-8158
---USA and Canada only---
Solutions to Signal Transduction Research
l02
Parathyroid hormone receptor


P1060 Lecirelin
Lecirelin is a synthetic GnRH analogue. Lecirelin is a nonapeptide, while the natural compound is a
decapeptide; moreover the glycine aminoacid in the 6th position has been substituted by leucine.
Size Price



P1026 Gonadorelin
Gonadorelin is a tropic peptide hormone responsible for the release of FSH and LH from the anterior pituitary.
It is synthesized and released from neurons within the hypothalamus. After a transient increase, continuous
administration results in downregulation of LH and FSH levels followed by a suppression of ovarian and
testicular steroid biosynthesis.
Synonyms:

Factrel
Size Price
P1061 Nafarelin
Nafarelin is a GnRH agonist which acts as an analog of GnRH and is a synthetic decapeptide. Nafarelin
increases the release of FSH and LH by the anterior pituitary, which in turn leads to an increase of
estrogen/progesterone. When administered, Nafarelin has the purpose of causing increase estrogen that will
negatively feed back upon hypothalamus to decrease GnRH.
Size Price
P1013 Leuprorelin
Leuprorelin is a gonadotropin-releasing hormone agonist. It acts at pituitary GnRH receptors. It down regulates
the secretion of gonadotropins LH and FSH leading to a dramatic reduction in estradiol levels. It is a drug that
mimics the action of a hormone called gonadotrophin releasing hormone.
Synonyms:

Lucrin,Lupron,Prostap
Size Price

P1048 Fertirelin
Fertirelin is a synthetic LHRH analogue, and it is a potent LHRH agonist. After a transient increase, continuous
administration results in downregulation of LH and FSH levels followed by a suppression of ovarian and
testicular steroid biosynthesis.
Size Price

P1021 Deslorelin
Deslorelin is a potent LHRH and GnRH agonist, and induces ovulatin in mares. It is commonly used to induce
ovulation in cycling mare. Deslorelin acetate was more effective in inducing ovulation in the July and August
(95.4%) and September and October (95.7%) than in the March and April (81.1%). Mares treated in May
through October also experienced shorter intervals to ovulation than mares treated in March and April.
Synonyms:

Ovuplant
Size Price
Synonyms:
ZM 252868, AG 1517, Tyrphostin AG 1517 P1037 Triptorelin
Triptorelin is a synthetic analogue of gonadorelin with amino acid (D-tryptophan) substitution in position 6 to
inhibit rapid degradation for long activity. Triptorelin is a GnRH agonist. By causing constant stimulation of the
pituitary, it decreases pituitary secretion of gonadotropins LH and FSH.
Synonyms:

Decapeptyl, Dekapeptil, Diferelin, Diphereline
P1033 Teriparatide
Teriparatide is recombinant parathyroid hormone, identical to the 34 N-terminal amino acids of human
parathyroid hormone. It reduces bone turnover, stimulates the formation of new bone, and increases bone
mass. It binds to the same receptors as PTH and is known to exert effects identical to that of PTH on the bone
and the kidney.
Synonyms:

hPTH 1-34, Parathar
Size Price
Size Price
Pyr-His-Trp-Ser-Tyr-D-
Trp-Leu-Arg-Pro-NHEt
AcOH
Pyr-His-Trp-Ser-Tyr-Gly-
Leu-Arg-Pro-NHEtAcOH
Glp-His-Trp-Ser-Tyr-Gly-Leu-
Arg-Pro-Gly-NH
2
AcOH
Pyr-His-Trp-Ser-Tyr-D-
Tle-Leu-Arg-Pro-NHEt
AcOH
Pyr-His-Trp-Ser-Tyr-D-
Leu-Leu-Arg-Pro-NHEt
AcOH
Pyr-His-Trp-Ser-Tyr-D-2-
Nal-Leu-Arg-Pro-Gly-NH
2
AcOH
Pry-His-Trp-Ser-Tyr-D-
Trp-Leu-Arg-Pro-Gly-NH
2
Ser-Val-Ser-Glu-Ile-Gln-Leu-Met-
His-Asn-Leu-Gly-Lys-His-Leu-Asn-
Ser-Met-Glu-Arg-Val-Glu-Trp-Leu-
Arg-Lys-Lys-Leu-Gln-Asp-Val-His-
Asn-PheAcOH
100mg
500mg
1g
10mg
25mg
50mg
100mg
500mg
1g
1mg
10mg
25mg
100mg
500mg
1g
100mg
500mg
1g
100mg
500mg
1g
25mg
100mg
500mg
Pepl|des LHRHR/GnRHR / ParaIhyroid hormone recepIor
l03
Melanocortin-1 receptor
Protein kinase C
Soluble nsf attachment protein receptor
Neurokinin receptor
Bradykinin receptor/Kappa opioid receptor

P1001 Argireline
Argireline Acetate is a synthetic anti-aging cosmetic derived from natural proteins. NAP receptor complex s
necessary for the contraction of muscles. It also slows or even stops the excessive release of catecholamine,
which is known to help in wrinkle formation.
Synonyms:

Acetyl hexapeptide-3
Size Price
Ac-Glu-Glu-Met-Gln-Arg-
Arg-NH
2



P1044 Eledoisin
Eledoisin Acetate is an acetate salt form of Eledoisin which is a decapeptide from the posterior salivary gland
of a species of snail and a nonselective neurokinin receptor agonist. It has vasodilator, hypotensive and
extravascular smooth muscle stimulant properties.
Size Price
pGlu-Pro-Ser-Lys-Asp-Ala-
Phe-Ile-Gly-Leu-Met-NH
2
AcOH



P1043 Dynorphin A(1-13)
Dynorphin A (1-13) Acetate is an acetate salt form of Dynorphin A (113) which is an extraordinarily potent
opioid peptide and acts on the bradykinin receptor and a major metabolite of Dynorphin A. The N-terminal
tyrosine of dynorphin A is necessary to activate opioid receptors such as KOR, but is unnecessary in binding
to bradykinin receptors.
Size Price
Tyr-Gly-Gly-Phe-Leu-Arg-
Arg-Ile-Arg-Pro-Lys-Leu-
AcOH
P1064 PT-141
PT-141 is an agonist of the melanocortin-1 receptor which is located on melanocyte cells but it does not bind
well to any other receptors. It is a cyclic hepta-peptide lactam analog of alpha-melanocyte-stimulating
hormone.
Size Price
P1073 Melanotan I
Melanotan I is a synthetic analog of the naturally occurring melanocortin peptide hormone alpha-melanocyte
VWLPXODWLQJKRUPRQH06+WKDWKDVEHHQVKRZQWRLQGXFHVNLQSLJPHQWDWLRQWKURXJKPHODQRJHQHVLVDQG
thereby subsequently reduce UV damage to UV exposed skin in preliminary studies.
Synonyms:

afamelanotide
Size Price
Synonyms:

Bremelanotide,PT141
Ac-Ser-Tyr-Ser-Nle-Glu-
His-D-Phe-Arg-Trp-Gly-Lys-
Pro-Val-NH
2
AcOH
Ac-Nle-Asp-His-D-Phe-Arg-
Trp-Lys-OHAcOH
Asp-Lys
1mg
P1083 ZIP
=,3 LV D QRYHO FHOOSHUPHDEOH LQKLELWRU RI SURWHLQ NLQDVH 0 D FRQVWLWXWLYHO\ DFWLYH DW\SLFDO 3.& LVR]\PH
LQYROYHGLQ/73PDLQWHQDQFH6HOHFWLYHO\EORFNV3.0LQGXFHGV\QDSWLFSRWHQWLDWLRQLQKLSSRFDPSDOVOLFHVLQ
YLWUR5HYHUVHVODWHSKDVH/73,&0DQGSURGXFHVSHUVLVWHQWORVVRIGD\ROGVSDWLDOPHPRU\
following central administration in vivo.
Size Price
Myr-Ser-Ile-Tyr-Arg-Arg-
Gly-Ala-Arg-Arg-Trp-Arg-
LeuAcOH
5mg
10mg
25mg
10mg
50mg
500mg
500mg
1g
10mg
5mg
10mg
25mg
5mg
25mg
100mg
Pepl|des
IelanocorIin-l / ProIein kinase C / Soluble nsI aIIachmenI proIein recepIor
/ Neurokinin recepIor / Bradykinin recepIor/Kappa opioid recepIor
Toll Free:(877)796-6397 www.selleckchem.com info@selleckchem.com
+1-832-582-8158
---USA and Canada only---
Solutions to Signal Transduction Research
l04
Growth-hormone-releasing factor receptor
Ghrelin receptor
P1042 CRF(ovine) AcF
3
10mg
50mg
200mg
CRF is a hypothalamic peptide which stimulates ACTH release from the anterior lobe of the pituitary gland. It
is a preferential CRF1 receptor agonist. In the placenta, CRH is a marker that determines the length of
gestation and the timing of parturition and delivery. A rapid increase in circulating levels of CRH occurs at the
onset of parturition.
P1072 CJC-1295
25mg
50mg
100mg
CJC-1295 is a long-acting GHRH analog and stimulates GH and IGF-1 secretion. It will keep a steady increase
of HGH and IGF-1 with no increase in prolactin. CJC-1295 represents a very exciting new compound that has
the potential to increase growth hormone and IGF-I secretion and effects, with a built-in safeguard to limit
excessive elevations of GH and IGF-1 levels.
P1058 GRF (human)
GRF is a hypothalamic hormone which regulates the synthesis and secretion of growth hormone from the
anterior pituitary. It is a 44-amino acid peptide hormone produced in the arcuate nucleus of the hypothalamus.
Anterior pituitaries from the dwarf mouse strain "little" did not release growth hormone or accumulate
adenosine 3,5-monophosphate (cyclic AMP) in response to human and rat growth hormone-releasing factor.
Size Price
Size Price
Size Price
5mg
10mg
25mg
P1059 Hexarelin
Hexarelin is a powerful GH-releasing peptide and capable of causing profound GH release. (ED50 = 0.48
0.02 g/kg) Hexarelin is a six-amino acid peptide. It activates G-protein-coupled receptors (GPCRs) and
stimulates growth hormone (GH) secretion from pituitary somatotropes.
Size Price
Thyrotropin-releasing hormone receptor
Corticotropin releasing factor receptor
P1041 CRF(human, rat)
CRF is a 41-peptide amide which stimulates the release of ACTH. It inhibits food intake in mammals. CRF
plays a potent role in decreasing food intake in avian species. The suppressive effect on food intake was
strongest for CRF followed by urotensin I, then urocortin.
Size Price
P1066 Taltirelin
Taltirelin is a TRH analog, which mimics the physiological actions of TRH, but with a much longer half-life and
duration of effects, and little development of tolerance following prolonged dosing. It displays 30 - 100-fold
more potent CNS activity and 50-fold weaker endocrine activity than TRH.
Synonyms:

L-Prolinamide, Taltirelin hydrate, TA-0910
Size Price
1-methyl-4,5-dihydroorotyl-
His-Pro-NH
2
AcOH
H-Ser-Glu-Glu-Pro-Pro-Ile-Ser-
Leu-Asp-Leu-Thr-Phe-His-Leu-
Leu-Arg-Glu-Val-Leu-Glu-Met-
Ala-Arg-Ala-Glu-Gln-Leu-Ala-
Gln-Gln-Ala-His-Ser-Asn-Arg-
Lys-Leu-Met-Glu-Ile-Ile-NH
2
AcOH
H-Ser-Gln-Glu-Pro-Pro-Ile-Ser-
Leu-Asp-Leu-Thr-Phe-His-Leu-
Leu-Arg-Glu-Val-Leu-Glu-Met-
Thr-Lys-Ala-Asp-Gln-Leu-Ala-
Gln-Gln-Ala-His-Ser-Asn-Arg-
Lys-Leu-Leu-Asp-Ile-Ala-NH
2
AcF
3
Tyr-D-Ala-Asp-Ala-Ile-Phe-Thr-
Gln-Ser-Tyr-Arg-Lys-Val-Leu-
Ala-Gln-Leu-Ser-Ala-Arg-Lys-
Leu-Leu-Gln-Asp-Ile-Leu-Ser-
Arg-NH
2
H-Tyr-Ala-Asp-Ala-Ile-Phe-Thr-
Asn-Ser-Tyr-Arg-Lys-Val-Leu-
Gly-Gln-Leu-Ser-Ala-Arg-Lys-
Leu-Leu-Gln-Asp-Ile-Met-Ser-
Arg-Gln-Gln-Gly-Glu-Ser-Asn-
Gln-Glu-Arg-Gly-Ala-Arg-Ala-
Arg-Leu-NH
2
AcOH
His-D-2-Me-Trp-Ala-Trp-
D-Phe-Lys-NH
2
AcOH
100mg
500mg
1g
100mg
500mg
1g
10mg
50mg
200mg
Pepl|des
TRH recepIor / CorIicoIropin releasinq IacIor recepIor
/ GrowIh-hormone-releasinq IacIor recepIor / Ghrelin recepIor
Ghrelin receptor
l05
Pepl|des
Ghrelin / Tachykinin NKl recepIor / AnqioIensin recepIor / SecreIin recepIor
/ SomaIosIaIin recepIor / Glucaqon recepIor

P1075 Ipamorelin
Ipamorelin is a selective growth hormone secretagogue and agonist of the ghrelin receptor. In pentobarbital
anaesthetised rats, ipamorelin released GH with a potency and efficacy comparable to GHRP-6 (ED50 =
8042 nmol/kg and Emax = 1545250 ng GH/ml vs 11536nmol/kg and 1167120ng GH/ml).
Size Price
Synonyms:

NNC-26-0161
Aib-His-D-2-Nal-D-Phe-
Lys-NH
2
AcOH
Tachykinin NK1 receptor
Angiotensin receptor
Secretin receptor
Somatostatin receptor
Glucagon receptor


P1024 Angiotensin
Angiotensin is an oligopeptide and causes blood vessels to constrict, and drives blood pressure up. It is part
of the renin-angiotensin system, which is a major target for drugs that lower blood pressure. It also stimulates
the release of aldosterone from the adrenal cortex.
Synonyms:

Gabarone, Neurontin
Size Price


P1038 Secretin
Secretin is a hormone that controls the secretions into the duodenum, and an orexin-A binding to
phospholipase C inhibitor (with IC50 in the range from 30 to 100 nM). Its effect is to regulate the pH of the
duodenal contents via the control of gastric acid secretion and buffering with bicarbonate.
Size Price
P1039 Somatostatin
Somatostatin acetate is an inhibitor of growth and suppresses the release of a variety of other hormones
involved in the regulation of important physiological functions of the gastrointestinal tract. It is a peptide
hormone that regulates the endocrine system and affects neurotransmission and cell proliferation via
interaction with G-protein-coupled somatostatin receptors and inhibition of the release of numerous secondary
hormones.
Size Price
P1056 Glucagon HCl
*OXFDJRQ LV D SURWHLQ KRUPRQH VHFUHWHG E\ FHOOV RI WKH SDQFUHDV ZKLFK SOD\V D UROH LQ FDUERK\GUDWH
metabolism. Glucagon has often been called the hyperglycemic-glycogenolytic factor because it causes the
breakdown of liver glycogen to sugar and thereby increases the concentration of sugar in the bloodstream.
Synonyms:

Glukagon novo
Size Price
P1068 Vapreotide
Vapreotide is a long-acting somatostatin analog, possesses an analgesic effect. It reduces splanchnic blood
flow and inhibits growth hormone release, and inhibits the release of peptides and vasoactive compounds
from neuroendocrine tumors.
Synonyms:

RC-160, Octastatin
Size Price
H-D-Phe-Cys-Tyr-D-Trp-
Lys-Val-Cys-Trp-NH
2
AcOH
Asp-Arg-Val-Tyr-His-Pro-
PheAcOH
His-Ser-Asp-Gly-Thr-Phe-
Thr-Ser-Glu-Leu-Ser-Arg-
Leu-Arg-Asp-Ser-Ala-Arg-
Leu-Gln-Arg-Leu-Leu-Gln-
Gly-Leu-Val-NH
2
AcOH
Ala-Gly-c[Cys-Lys-Asn-Phe-
Phe-Trp-Lys-Thr-Phe-Thr-
Ser-Cys]AcOH
H-His-Ser-Gln-Gly-Thr-Phe-
Thr-Ser-Asp-Tyr-Ser-Lys-Tyr-
Leu-Asp-Ser-Arg-Arg-Ala-Gln-
Asp-Phe-Val-Gln-Trp-Leu-Met-
Asn-Thr-OHAcOH
25mg
100mg
200mg
50mg
100mg
500mg
100mg
500mg
1g
25mg
100mg
500mg
100mg
500mg
1g
1mg
5mg
25mg
Toll Free:(877)796-6397 www.selleckchem.com info@selleckchem.com
+1-832-582-8158
---USA and Canada only---
Solutions to Signal Transduction Research
l06
100mg
500mg
1g
100mg
500mg
1g
Growth hormone secretagogue receptor
P1049 GHRP-2
GHRP-2 is a true hGH secretagogue. It is a synthetic agonist of ghrelin, the newly-discovered gut peptide
which binds to the GH secretagogue receptor. Ghrelin has two major effects, stimulating both GH secretion
and appetite/meal initiation. GHRP-2 has been extensively studied for its utility as a GHS.
Synonyms:

GH Releasing Peptide-2
Size Price
P1075 Ipamorelin Synonyms:

NNC-26-0161 Page 105
GHRP-6 is a peptide in the growth factor family. It has strong effect on the release of Growth Hormone. Its
main use is to promote food intake by stimulating hunger and aid in energy metabolism. It has also been
discovered that when GHRP-6 and insulin are used simultaneously, GH response to GHRP-6 is increased.
Synonyms:

Growth hormone releasing peptide 6
Size Price P1054 GHRP-6
H-D-Ala-D-2-Nal-Ala-Trp-
D-Phe-Lys-NH
2
AcOH
H-His-D-Trp-Ala-Trp-D-
Phe-Lys-NH
2
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