Bisindolylmaleimide I (hydrochloride)

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 (Item No. 81590).¹ 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).² It also competitively antagonizes the serotonin (5-HT) receptor subtype 5-HT₃ with a K_i value of 61 nM.³

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1. Toullec, D., Pianetti, P., Coste, H., et al. The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C. The Journal of Biological Chemisty 266(24), 15771-15781 (1991).

2. Hers, I., Tavaré, J.M., and Denton, R.M. The protein kinase C inhibitors bisindolylmaleimide I (GF 109203x) and IX (Ro 31-8220) are potent inhibitors of glycogen synthase kinase-3 activity. FEBS Lett. 460(3), 433-436 (1999).

3. Coultrap, S.J., Sun, H., Tenner, T.E., et al. Competitive antagonism of the mouse 5-hydroxytryptamine receptor by bisindolylmaleimide I, a "selective" protein kinase C inhibitor. J. Pharmacol. Exp. Ther. 290(1), 76-82 (1999).