ZM 336372

개요The Ras/Raf-1 signalling pathway is a well-characterized system that links receptor tyrosine kinase (RTK) activation with changes in gene expression and cell behavior. Raf-1 is a serine/threonine protein kinase that phosphorylates and activates MAPK-kinase (MEK) in response to activation by Ras. ZM 336372 is a potent ATP-competitive inhibitor of Raf-1 in vitro (IC50 = 70 nM) with the paradoxical effect of inducing >100-fold activation of Raf-1 in whole cells. Activation of the Raf-1 signalling pathway using ZM 336372 in human carcinoid tumor cells results in induction of cell cycle inhibitors and suppression of cellular proliferation.