Bisindolylmaleimide IV is a cell permeable inhibitor of protein kinase C (PKC) with IC50 values reported to range from 0.10 to 0.55 µM.1,2,3,4 Bisindolylmaleimide IV was designed to be more discriminative than its parent compound, the non-selective PKC inhibitor, staurosporine (Catalog No. 81590). However, bisindolylmaleimide IV also inhibits protein kinase A with IC50 values ranging from 2 to 11.8 µM.1,2
1
Davis, P.D., Hill, C.H., Lawton, G., et al. Inhibitors of protein kinase C. 1.1 2,3-bisarylmaleimides. J Med Chem35177-184(1992).
2
Toullec, D., Pianetti, P., Coste, H., et al. The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C. J Biol Chem266(24)15771-15781(1991).
3
Fabre, S., and Prudhomme, M. Protein kinase C inhibitors; structure-activity relationships in K252c-related compounds. Bioorg Med Chem1(3)193-196(1993).
4
Lazareno, S., Popham, A., and Birdsall, N.J.M. Muscarinic interactions of bisindolylmaleimide analogues. Eur J Pharmacol360281-284(1998).
Davis, P.D., Hill, C.H., Lawton, G., et al. Inhibitors of protein kinase C. 1.1 2,3-bisarylmaleimides. J Med Chem35177-184(1992).
Toullec, D., Pianetti, P., Coste, H., et al. The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C. J Biol Chem266(24)15771-15781(1991).
Fabre, S., and Prudhomme, M. Protein kinase C inhibitors; structure-activity relationships in K252c-related compounds. Bioorg Med Chem1(3)193-196(1993).
Lazareno, S., Popham, A., and Birdsall, N.J.M. Muscarinic interactions of bisindolylmaleimide analogues. Eur J Pharmacol360281-284(1998).