Potent Inhibitor of Protein Kinase A, Protein Kinase C and Protein Kinase G.
K252a is an alkaloid isolated from Nocardiopisis sp. soil fungi. This ATP analog is a highly potent cell permeable inhibitor of CaM kinase and phosphorylase kinase (IC50= 1.8 and 1.7 nM respectively). At higher concentrations it is also an efficient inhibitor of serine/threonine protein kinases (IC50�of 10 to 30 nM).
It is reported to promote myogenic differentiation in C2 mouse myoblasts and has been shown to block the neuronal differentiation of rat pheochromocytoma PC12 cells by inhibition of trk tyrosine kinase activity. Paradoxically K252a exerts neurotrophic effects on primary sensory neurons, neuroblastoma cells, PC12 cells, and central neuron.
Protein Kinase Inhibitors and Activatiors; Protein Kinase Inhibitors (non specific)