Enzastaurin

Enzastaurin is a potent inhibitor of PKCbeta (IC50 = 6 nM), with modest selectivity over PKCalpha, PKCgamma, and PKCepsilon (IC50 = 39, 83, and 110 nM, respectively). At 3 µM, enzastaurin also inhibits signaling through the Akt pathway. It suppresses angiogenesis, induces apoptosis, and reduces proliferation of cultured tumor cells. Because of these effects, enzastaurin has potential antineoplastic activity.Formal Name: 3-(1-methyl-1H-indol-3-yl)-4-[1-[1-(2-pyridinylmethyl)-4-piperidinyl]-1H-indol-3-yl]-1H-pyrrole-2,5-dione. CAS Number: 170364-57-5. Synonyms: LY317615. Molecular Formula: C32H29N5O2. Formula Weight: 515.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 16.6 mg/ml, DMF:PBS (pH 7.2)(1:3): 0.25 mg/ml, DMSO: 10 mg/ml. lambdamax: 285, 377, 467 nm. SMILES: O=C(N1)C(C2=CN(C3CCN(CC4=NC=CC=C4)CC3)C5=C2C=CC=C5)=C(C6=CN(C)C7=C6C=CC=C7)C1=O. InChi Code: InChI=1S/C32H29N5O2/c1-35-19-25(23-9-2-4-11-27(23)35)29-30(32(39)34-31(29)38)26-20-37(28-12-5-3-10-24(26)28)22-13-16-36(17-14-22)18-21-8-6-7-15-33-21/h2-12,15,19-20,22H,13-14,16-18H2,1H3,(H,34,38,39). InChi Key: AXRCEOKUDYDWLF-UHFFFAOYSA-N.