| Identification | Back Directory | [Name]
3-(1-Methyl-1H-indol-3-yl)-4-[1-[1-(2-pyridinylmethyl)-4-piperidinyl]-1H-indol-3-yl]-1H-pyrrole-2,5-dione hydrochloride | [CAS]
365253-37-8 | [Synonyms]
Enzastaurin 2HCl
LY-317615 dihydrochloride
LY317615 /Enzastaurin 2HCL
Enzastaurin 2HCL (LY317615)
Enzastaurin dihydrochloride
3-(1-methylindol-3-yl)-4-[1-[1-(pyridin-2-ylmethyl)piperidin-4-yl]indol-3-yl]pyrrole-2,5-dione:dihydrochloride
3-(1-Methyl-1H-indol-3-yl)-4-[1-[1-(2-pyridinylmethyl)-4-piperidinyl]-1H-indol-3-yl]-1H-pyrrole-2,5-dione hydrochloride | [Molecular Formula]
C32H30ClN5O2 | [MDL Number]
MFCD20524900 | [MOL File]
365253-37-8.mol | [Molecular Weight]
552.08 |
| Hazard Information | Back Directory | [Uses]
Enzastaurin (LY317615) dihydrochloride is a potent and selective PKCβ inhibitor with an IC50 of 6 nM, showing 6- to 20-fold selectivity over PKCα, PKCγ and PKCε[1]. | [References]
[1] Graff JR, et al. 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, 2005, 65(16), DOI:10.1158/0008-5472.CAN-05-0071
[2] Rovedo MA, et al. Inhibition of glycogen synthase kinase-3 increases the cytotoxicity of enzastaurin. J Invest Dermatol, 2011, 131(7), 1442-1449. DOI:10.1038/jid.2011.70
[3] Podar K, et al. Targeting PKC in multiple myeloma: in vitro and in vivo effects of the novel, orally available small-molecule inhibitor enzastaurin (LY317615.HCl). Blood, 2007, 109(4), 1669-1677. DOI:10.1182/blood-2006-08-042747 |
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