Description
Enzastaurin (LY317615) can inhibit PKCalpha, PKCbeta, PKCgamma and PKCepsilon with IC50 of 39 nM, 6 nM, 83 nM and 110 nM.
Storage
2 years at -20centigrade Powder
Targets
PKCalpha, PKCbeta, PKCgamma, PKCepsilon
Molecular Formula
C32H29N5O2
Chemical Name
3-(1-methyl-1H-indol-3-yl)-4-(1-(1-(pyridin-2-ylmethyl)piperidin-4-yl)-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Solubility
DMSO 30 mg/mL Water
In vitro
LY317615 is a PKCbeta inhibitor. Enzastaurin (LY317615.HCl) can suppress angiogenesis. As ctivation of PKCbeta has now also been implicated in tumor cell proliferation, apoptosis, and tumor invasiveness, enzastaurin has a direct effect on human tumor cells, inducing apoptosis and suppressing the proliferation of cultured tumor cells. Enzastaurin treatment also suppresses the phosphorylation of GSK3betaser9, ribosomal protein S6(S240/244), and AKT(Thr308).
In vivo
LY317615 can significantly decrease plasma VEGF levels in mice bearing SW2 SCLC and Caki-1 renal cell carcinoma. VEGF plasma levels remained suppressed after termination of LY317615 treatment. Plasma VEGF levels in mice bearing HCT116 xenografts were not altered by LY317615 treatment and plasma bFGF and TGF-beta were not altered by LY317615 in any of the animals. As shown by CD31 immunohistochemical staining, LY317615 decreased intratumoral vessel density by nearly 40% in all three tumors. Only the Caki-1 tumor responded to single-agent LY317615 therapy with a measurable tumor growth delay.
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