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Datasheet of Deguelin

Description:
Deguelin, a naturally occurring rotenoid, is known to be an Akt inhibitor and to have an anti-tumor effect on several cancers;
decrease levels of phosphorylated Akt. in vitro: Deguelin in a dose and time dependent manner inhibited the growth of
MDA-MB-231, MDA-MB-468, BT-549 and BT-20 cells. Deguelin administration causes a significant HNSCC cell death.
Deguelin induces both cell apoptosis and autophagy by modulating multiple signaling pathways in cultured HNSCC cells.
Deguelin inhibits Akt signaling, and down-regulates survivin and cyclin-dependent kinase 4 (Cdk4) expressions, by disrupting
their association with heat shock protein-90 (Hsp-90). Deguelin induces ceramide production through de novo synthase pathway
to promote HNSCC cell death. Importantly, increased ceramide level activates AMP-activated protein kinase (AMPK), which
then directly phosphorylates Ulk1 and eventually leads to cell autophagy. Deguelin inhibited the proliferation of MPC-11 cells in
a concentration- and time-dependent manner and caused the apoptotic death of MPC-11 cells. Following exposure to deguelin,
the phosphorylation of Akt was decreased. The inhibition of cell growth may be associated with decreased levels of
phosphorylated Akt. Deguelin-induced apoptosis was characterized by the upregulation of Bax, downregulation of Bcl-2 and
activation of caspase-3. in vivo: Deguelin (2 or 4 mg/kg body weight), when injected intraperitoneally, reduced the in vivo tumor
growth of MDA-MB-231 cells transplanted subcutaneously in athymic mice. Moreover it was nontoxic as evident from daily
observations on mobility, food and water consumption and comparison of bodyweight and other visceral organ weights with
those in control animals at the termination of the study. In the colon cancer xenograft model, the volume of the tumor treated
withdeguelin was significantly lower than that of the control, and the apoptotic index for deguelin-treated mice was much higher.

Chemical Information
Catalog

DC9337

Purity of current batch:

>98%

Molecular Weight (MW)

394.42

Molecular Formula

C23H22O6

CAS No.

522-17-8

Solubility (25C)

DMSO

Storage

Store at -20C (desiccating conditions).

Handling:
Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months.
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in

advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable
for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room
temperature for at least 1 hour.