Bisindolylmaleimide I 1PC X 250UG

Description 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, βI, βII, 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-, βI-, βII-, 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. Packaging 1 mg in Plastic ampoule 250 μg in Plastic ampoule Biochem/physiol Actions Cell permeable: yes Primary Target PKC Product competes with ATP. Reversible: yes 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 Warning Toxicity: Standard Handling (A) 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. 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.