货号 | 9841S |
供应商 | CST |
背景 | Bisindolylmaleimide I (BIS) is a potent inhibitor of PKC (1,2). In vitro the IC50 of BIS is 10-20 nM for PKCα/β/γ and 100-200 nM for PKCδ/ε isoforms. The in vitro IC50 for PKCζ is about 6 μM, indicating that BIS is a very weak inhibitor for this isoform. In in vivo cellular assays the IC50 of BIS for PKC is between 0.2-2 μM (1,3). |
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参考文献 | Toullec, D. et al. (1991) J. Biol. Chem. 266, 15771-15781. Martiny-Baron, G. et al. (1993) J. Biol. Chem. 268, 9194-9197. Heikkilä, J. et al. (1993) Biochem. Biophys. Res. Commun. 197, 1185-1193. |
Bisindolylmaleimide I structure | |
Western blot analysis of extracts from A172 cells, untreated or treated with indicated concentrations of Bisindolylmaleimide I for 30 minutes, followed by stimulation with 200 nM TPA for 10 minutes. The phosphorylation of PEA-15 was detected by using Phospho-PEA-15 (Ser104) Antibody #2776 (upper). PEA-15 Antibody #2780 was used as a loading control (lower). Bisindolylmaleimide I-mediated inhibition of TPA-induced PKC phosphorylation of PEA-15 at Ser104 is shown. |