Enzastaurin

Cat. No. 5994new

Enzastaurin C32H29N5O2 [170364-57-5]

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Alternative Name: LY317615

Chemical Name: 3-(1-Methyl-1H-indol-3-yl)-4-[1-[1-(2-pyridinylmethyl)-4-piperidinyl]-1H-indol-3-yl]-1H-pyrrole-2,5-dione

Biological Activity

Potent PKCβ inhibitor (IC50 values are 6, 39, 83 and 110 nM for PKCβ, PKCα, PKCγ and PKCε, respectively). Suppresses proliferation and induces apoptosis in HCT116 colon carcinoma and U87MG glioblastoma cells in vitro. Reduces tumor growth and exhibits antiangiogenic activity in HT-29 colon carcinoma xenografts in mice. Also suppresses growth of HCT116 and U87MG xenografts in mice. Orally active.

Technical Data

M.Wt:
515.6
Formula:
C32H29N5O2
Solubility:
Soluble to 20 mM in DMSO
Purity:
>98 %
Storage:
Store at -20°C
CAS No:
170364-57-5

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Graff et al (2005) The protein kinase Cβ-selective inhibitor, Enzastaurin (LY317615.HCl), suppresses signaling through the AKT pathway, induces apoptosis, and suppresses growth of human colon cancer and glioblastoma xenografts. Cancer Res. 65 7462. PMID: 16103100 .

Teicher et al (2001) Antiangiogenic and antitumor effects of a protein kinase Cβ inhibitor in human HT-29 colon carcinoma and human CaKi1 renal cell carcinoma xenografts. Anticancer Res. 21 3175. PMID: 11848470.

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Keywords: Enzastaurin, supplier, Potent, PKCbeta, PKCb, PKCβ, inhibitors, inhibits, antitumor, orally, active, protein, kinases-C, Tocris Bioscience, Protein Kinase C Inhibitor products

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