Chelerythrine. Protein Kinase C Inhibitor. Chelerythrine is a potent, cell-permeable inhibitor of protein kinase C (IC50 = 660nM) that binds to the catalytic domain of 5/PKC. Chelerythrine is at least 100-fold more selective for 5/PKCs than for other kinases
In platelets, Chelerythrine inhibits thromboxane formation and phosphoinositide metabolism. It has an inhibitory effect on ACh-induced current in PC12 cells.
Chelerythrine induces apoptotic cell death in polymorphonuclear leukocyte through activation of caspase-3. Furthermore, Chelerythrine treated cells underwent apoptosis, with features that suggest involvement of the mitochondrial pathway, and through a mechanism that involves inhibition of the anti-apoptotic inhibitor BclXL. Protein Kinase Inhibitors and Activators; 5/PKC Inhibitor.