GW5074 (C09-0901-634)

InformationGW5074 is a potent and selectivec-Rafinhibitor withIC50of 9 nM, no effect on the activities of JNK1/2/3, MEK1, MKK6/7, CDK1/2, c-Src, p38 MAP, VEGFR2 or c-Fms is noted. GW5074 inhibits LK-inducedapoptosis.In vitroGW5074 is a potent and specific inhibitor of c-Raf with IC50 of 9 nM and has no effect of MKK6, MKK7, p38 MAP kinase and cdks in vitro. However, treatment of neuronal cultures with GW5074 permits accumulation of activating modifications on c-Raf and also B-Raf. The inhibition of LK-induced apoptosis by GW5074 in cerebellar granule neurons is not MEK-ERK-dependent. GW5074 delays down-regulation of Akt activity but inhibits apoptosis by an Akt-independent mechanism. GW5074 affects Ras, nuclear factor-kappa B and c-jun. GW5074 inhibits cell death caused by neurotoxins in granule cells and other neuronal types.In vivoGW5074 is protective in an in vivo experimental model of Huntington’s disease. GW5074 (5 mg/Kg) completely prevented extensive bilateral striatal lesions induced by 3-NP in mice. GW5074 completely abolishes chronic morphine-mediated AC superactivation I in CHO cells stably expressing the humanμ-opioid receptor. GW5074 suppresses sidestream smoke-induced airway hyperresponsiveness in mice.Cell Datacell lines：Concentrations：~5 μMIncubation Time：24 hoursPowder Purity:≥99%. Specification: 10mM in DMSO Molecular Formula: C15H8Br2INO2 Molecular Weight: 520.94