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Description

A cell permeable, reversible, selective protein kinase C (PKC) inhibitor (IC50 = 158 nM for rat brain PKC) that acts at the ATP binding site of PKC. Does not inhibit the tyrosine phosphorylation or the activation of phospholipase Cgamma1. Exhibits some degree of PKC isozyme specificity (IC50 = 53 nM for PKCalpha, 195 nM for PKCbetaI, 163 nM for PKCbetaII, 213 nM for PKCgamma, and 175 nM for PKCepsilon). Inhibits carbachol-evoked noradrenaline release (IC50 = 600 nM)., A cell-permeable, reversible, selective protein kinase C (PKC) inhibitor that acts at the ATP binding site of PKC (IC50 = 158 nM for rat brain PKC). Does not inhibit the tyrosine phosphorylation or the activation of phospholipase Cgamma1 unlike staurosporine and other serine/threonine kinase inhibitors. IC50 values for individual PKC isozymes are as follows: 53 nM for PKCalpha, 195 nM for PKCbetaI, 163 nM for PKCbetaII, 213 nM for PKCgamma, and 175 nM for PKCepsilon. Inhibits carbachol-evoked noradrenaline release (IC50 = 0.6 µ,M).