Bisindolylmaleimide I

Bisindolylmaleimide I (BIM I) is a highly selective, cell-permeable, and reversible PKC inhibitor (Ki = 14 nM) that is structurally similar to the poorly selective PKC inhibitor staurosporine (Cay-81590). It acts as a competitive inhibitor for the ATP binding site of PKC and shows high selectivity for PKCalpha, beta1, beta2, gamma, delta, and epsilon isozymes. BIM I directly inhibits glycogen synthase kinase 3 (GSK3) in primary adipocyte lysates (IC50 = 360 nM) and in GSK3beta immunoprecipitates derived from rat epididymal adipocytes (IC50 = 170 nM). It also competitively antagonizes the serotonin (5-HT) receptor subtype 5-HT3 with a Ki value of 61 nM.Formal Name: 3-[1-[3-(dimethylamino)propyl]-1H-indol-3-yl]-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione. CAS Number: 133052-90-1. Synonyms: BIM I, GF 109203X, Gö 6850. Molecular Formula: C25H24N4O2. Formula Weight: 412.5. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 3 mg/ml, DMSO: 5 mg/ml, DMSO:PBS (pH 7.2) (1:10): 0.1 mg/ml. lambdamax: 279, 374, 461 nm. SMILES: CN(C)CCCn1cc(C2=C(C(=O)NC2=O)c2c[nH]c3ccccc23)c2ccccc12. InChi Code: InChI=1S/C25H24N4O2/c1-28(2)12-7-13-29-15-19(17-9-4-6-11-21(17)29)23-22(24(30)27-25(23)31)18-14-26-20-10-5-3-8-16(18)20/h3-6,8-11,14-15,26H,7,12-13H2,1-2H3,(H,27,30,31). InChi Key: QMGUOJYZJKLOLH-UHFFFAOYSA-N.