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bisindolylmaleimide I
- Development stage
- Unknown
- Modality
- Small Molecules
01
Overview
Bisindolylmaleimide I is a potent, cell-permeable, and reversible small molecule inhibitor of protein kinase C (PKC), with high selectivity for several PKC isoforms (notably PKCα, PKCβI, PKCβII, and PKCγ) at nanomolar concentrations. It acts as a competitive inhibitor at the ATP-binding site of these kinases. Bisindolylmaleimide I also inhibits other kinases such as glycogen synthase kinase 3 (GSK‑3) at higher concentrations and may weakly inhibit protein kinase A. The compound is structurally related to staurosporine but offers greater selectivity for PKC isoforms. It is widely used in research to study signal transduction pathways involving serine/threonine kinases[1][2][3][4][5].
- Other names
- bisindolylmaleimide I2-[1-(3-dimethylaminopropyl)-1H-indol-3-yl]-3-(1H-indol-3-yl)-maleimide
02
Targets
GSK3 (Glycogen synthase kinase 3 beta)HTR3A (5-hydroxytryptamine receptor 3A)PRKCG (Protein kinase C gamma)PRKCA (Protein kinase C alpha)PRKCB (Protein kinase C beta)PRKCD (Protein kinase C delta)PRKCE (Protein Kinase C epsilon)
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