Bisindolylmaleimide I

Biochem/physiol Actions

Target IC₅₀: 10 nM against protein kinase C (PKC); 360 nM, 170 nM against GSK-3 in primary adipocyte lysates and in GSK-3β immunoprecipitates, respectively

Reversible: yes

Product competes with ATP.

Primary TargetPKC

Cell permeable: yes

General description

A highly selective cell-permeable protein kinase C (PKC) inhibitor (IC₅₀ = 10 nM) that is structurally similar to staurosporine. Acts as a competitive inhibitor for the ATP-binding site of PKC. Shows high selectivity for PKCα, β_I, β_II, γ, δ, and ε isozymes. May inhibit protein kinase A at a much higher concentration (IC₅₀ = 2 µM). Also inhibits telomerase activity in quercetin, H-89, or herbimycin A treated NPC-076 cells.

A highly selective, cell-permeable, and reversible protein kinase C (PKC) inhibitor (IC₅₀ = 10 nM) that is structurally similar to staurosporine. Acts as a competitive inhibitor for the ATP-binding site of PKC. Shows high selectivity for PKCα-, β_I-, β_II-, γ-, δ-, and ε- isozymes. Potently inhibits GSK-3 in primary adipocyte lysates (IC₅₀ = 360 nM) and in GSK-3β immunoprecipitates (IC₅₀ = 170 nM). May inhibit protein kinase A at a much higher concentration (IC₅₀ = 2 µM). A 1 mg/ml solution of Bisindolylmaleimide I (Cat. No. 203293) in anhydrous DMSO is also available.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Hers, I., et al. 1999. FEBS Lett.460, 433.Ku, W.-C., et al. 1997. Biochem. Biophys. Res. Commun. 241, 730.Gekeler, V., et al. 1996. Br. J. Cancer 74, 897.Kiss, Z., et al. 1995. Biochim. Biophys. Acta 1265, 93.Toullec, D., et al. 1991. J. Biol. Chem. 266, 15771.

Packaging

1 mg in Plastic ampoule

250 µg in Plastic ampoule

Preparation Note

Further dilute with aqueous buffers just prior to use.

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). DMSO stock solutions are stable for up to 4 months at -20°C.

Warning

Toxicity: Standard Handling (A)