Potent PKCβinhibitor (IC50values are 6, 39, 83 and 110 nM for PKCβ, PKCα, PKCγand PKCε, respectively). Suppresses proliferation and induces apoptosis in HCT116 colon carcinoma and U87MG glioblastoma cellsin vitro. Reduces tumor growth and exhibits antiang
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Protein kinase C beta inhibitor
Note
卖完停产,不再备货
Product Description
Enzastaurin (LY317615) is a potent PKCβ selective inhibitor with IC50 of 6 nM, 6- to 20-fold selectivity against PKCα, PKCγ and PKCε. A potent inhibitor of PKCβ, PKCα, PKCγ and PKCε.
1.Teicher BA, Alvarez E, Menon K, Esterman MA, Considine E, Shih C, Faul MM. (2002) Antiangiogenic effects of a protein kinase Cbeta-selective small molecule.. Cancer Chemother Pharmacol, 49 (1):(69-77). [PMID:11855754]
2.Faul MM, Gillig JR, Jirousek MR, Ballas LM, Schotten T, Kahl A, Mohr M. (2003) Acyclic N-(azacycloalkyl)bisindolylmaleimides: isozyme selective inhibitors of PKCbeta.. Bioorg Med Chem Lett, 13 (11):(1857-9). [PMID:12749884]
3.Graff JR, McNulty AM, Hanna KR, Konicek BW, Lynch RL, Bailey SN, Banks C, Capen A, Goode R, Lewis JE et al.. (2005) The protein kinase Cbeta-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 (16):(7462-9). [PMID:16103100]
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