BISINDOLYLMALEIMIDE I HYDROCHLORIDE

Description

Bisindolylmaleimide I (BIM I) is a highly selective, cell-permeable, and reversible PKC inhibitor (K_i = 14 nM) that is structurally similar to the poorly selective PKC inhibitor staurosporine . It acts as a competitive inhibitor for the ATP binding site of PKC and shows high selectivity for PKCα, β1, β2, γ, δ, and ε isozymes. BIM I directly inhibits glycogen synthase kinase 3 (GSK3) in primary adipocyte lysates (IC₅₀ = 360 nM) and in GSK3β immunoprecipitates derived from rat epididymal adipocytes (IC₅₀ = 170 nM). It also competitively antagonizes the serotonin (5-HT) receptor subtype 5-HT₃ with a K_i value of 61 nM.

Uses

GF 109203X hydrochloride has been used to inhibit protein kinase C in human neuroblastoma-derived kelly cells.

General Description

GF 109203X prevents collagen-triggered adenosine and three phosphate (ATP) secretion. It also inhibits collagen and α-thrombin-induced platelet aggregation. It functions as an inhibitor of glycogen synthase kinase-3 (GSK-3). GF 109203X also functions as an anti-inflammatory agent.

Biochem/physiol Actions

Inhibitor of protein kinase C; potent inhibitor of GSK-3.