K252a (99533-80-9) is a potent pan-specific protein kinase inhibitor: PKA (Ki = 18 nM), PKC (Ki = 25 nM) PKG (Ki = 20 nM)1. K252a inhibits CaMK (Ki = 1.8 nM)2 and phosphorylase kinase (IC50 = 1.7 nM)3 as well as other kinases4. Induces apoptosis5. Cell permeable.
1) Kase et al. (1987), K-252 compounds, novel and potent inhibitors of protein kinase C and cyclic nucleotide-dependent protein kinases; Biochem. Biophys. Res. Commun., 142 436
2) Hashimoto et al. (1991), Potent and preferential inhibition of Ca2+/calmodulin-dependent protein kinase II by K252a and its derivative KT5926; Biochem. Biophys. Res. Commun., 181 423
3) Berg et al. (1992), K-252a inhibits nerve growth factor-induced trk proto-ooncogene tyrosine phosphorylation and kinase activity; J. Biol. Chem., 267 13
4) Ruegg et al. (1989), Staurosporine, K-252 and UCN-01: potent but non-specific inhibitors of protein kinases; Trends Pharmacol. Sci., 10 218
5) Mohri et al. (1999), K252a induces cell cycle arrest and apoptosis by inhibiting Cdc2 and Cdc25c; Cancer Invest., 17 391