Bisindolylmaleimide I (hydroch

一种高选择性、细胞通透性和可逆性的PKC抑制剂(Ki=14nM)；PKC的ATP结合位点的竞争性抑制剂；对PKCα、β1、β2、γ、δ和ε同工酶具有高选择性；抑制原代脂肪细胞裂解物中的GSK3(IC50=360nM)和大鼠附睾脂肪细胞衍生的GSK3β免疫沉淀物中的GSK3(IC50=170nM)；竞争性拮抗5-HT3受体，Ki值为61nM。A highly selective, cell-permeable, and reversible PKC inhibitor (Ki = 14 nM); competitive inhibitor for the ATP binding site of PKC; highly selective for PKCα, β1, β2, γ, δ, and ε isozymes; inhibits GSK3 in primary adipocyte lysates (IC50 = 360 nM) and in GSK3β immunoprecipitates derived from rat epididymal adipocytes (IC50 = 170 nM); competitively antagonizes the 5-HT3 receptor with a Ki value of 61 nM.