Staurosporine (Stsp) is potent inhibitor of protein kinase C (PKC) from rat brain, exhibiting an IC50 value of 2.7 nM.1 It inhibits rat recombinant PKC-α approximately 100- and 1,000-fold better than PKC-δ and PKC-ζ, respectively.2 However, Stsp is non-selective in that it also inhibits the activity of a variety of other protein kinases, not only PKC isoforms.3 The biological effects of Stsp include cytotoxicity, relaxation of smooth muscle, and regulation of eNOS gene expression.3,4
1
Tamaoki, T., Nomoto, H., Takahashi, I., et al. Staurosporine, a potent inhibitor of phospholipid/Ca++ dependent protein kinase. Biochem Biophys Res Commun135397-402(1986).
2
McGlynn, E., Liebetanz, J., Reutener, S., et al. Expression and partial characterization of rat protein kinase C-δ and protein kinase C-ζ in insect cells using recombinant baculovirus. J Cell Biochem49239-250(1992).
3
Ruegg, U.T., and Burgess, G.M. Staurosporine, K-252 and UCN-01: Potent but nonspecific inhibitors of protein kinases. Trends Pharmacol Sci10218-220(1989).
4
Li, H., and Förstermann, U. Structure-activity relationship of staurosporine analogs in regulating expression of endothelial nitric-oxide synthase gene. Mol Pharmacol57427-35(1999).
Li, H., and Förstermann, U. Structure-activity relationship of staurosporine analogs in regulating expression of endothelial nitric-oxide synthase gene. Mol Pharmacol57427-35(1999).
Tamaoki, T., Nomoto, H., Takahashi, I., et al. Staurosporine, a potent inhibitor of phospholipid/Ca++ dependent protein kinase. Biochem Biophys Res Commun135397-402(1986).
Ruegg, U.T., and Burgess, G.M. Staurosporine, K-252 and UCN-01: Potent but nonspecific inhibitors of protein kinases. Trends Pharmacol Sci10218-220(1989).
McGlynn, E., Liebetanz, J., Reutener, S., et al. Expression and partial characterization of rat protein kinase C-δ and protein kinase C-ζ in insect cells using recombinant baculovirus. J Cell Biochem49239-250(1992).