Chelerythrine is a potent, cell-permeable inhibitor of protein kinase C (IC₅₀ = 660 nM) that binds to the catalytic domain of PKC. Chelerythrine is at least 100-fold more selective for PKCs than for other kinases.^1,2

In platelets, Chelerythrine inhibits thromboxane formation and phosphoinositide metabolism.^3,4 It has an inhibitory effect on ACh-induced current in PC12 cells.⁵

Chelerythrine induces apoptotic cell death in polymorphonuclear leukocyte through activation of caspase-3.⁶ 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.⁷

Chelerythrine inhibits SERCA pumps with an IC₅₀ of 1.5 µM⁸. It also antagonizes P2X7 receptors; it inhibits ATP-induced ⁸⁶Rb⁺ efflux with an IC₅₀ of 5.6 µM⁹.