bisindolylmaleimide viii

Bisindolylmaleimide VIII is a potent and selective small molecule inhibitor of protein kinase C (PKC), with IC50 values in the low nanomolar range for several PKC isoforms (notably PKC-alpha, PKC-beta I/II, PKC-gamma, and PKC-epsilon)[1][5][8]. It displays higher selectivity for PKC-alpha over other isoforms. The compound also acts as an antagonist of cyclin-dependent kinase 2 (CDK2) at higher concentrations[5]. Mechanistically, Bisindolylmaleimide VIII inhibits the ATP-binding site of these kinases. It has been shown to facilitate Fas-mediated apoptosis and enhance DR5-mediated apoptosis via activation of JNK and p38 MAPK pathways[8]. This compound is used primarily as a research tool in cell signaling studies related to apoptosis, cell cycle regulation, and kinase signaling pathways. It is not approved for clinical or therapeutic use in humans.

Other names

bisindolylmaleimide viii acetate1H-Pyrrole-2,5-dione, 3-[1-(3-aminopropyl)-1H-indol-3-yl]-4-(1-methyl-1H-indol-3-yl)-