2-[1-(3-Dimethylaminopropyl)-1H-indol-3-yl]-3-(1H-indol-3-yl)-maleimide Gö 6850 GF 109203X Deep orange solid. A highly selective, cell-permeable, and reversible protein kinase C (PKC) inhibitor (Ki = 10 nM) that is structurally similar to staurosporine. Acts as a competitive inhibitor for the ATP-binding site of PKC. Shows high selectivity for PKCa-, bI-, bII-, g-, d-, and e- isozymes. Potently inhibits GSK-3 in primary adipocyte lysates (IC50 = 360 nM) and in GSK-3b immunoprecipitates (IC50 = 170 nM). May inhibit protein kinase A at a much higher concentration (Ki = 2 µM). Purity: ≥95% by HPLC. CAS 133052-90-1. Ref.: 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. Sold under license of U.S. Patent 5,380,746. |