Potent, brain-permeable inhibitor of c-Raf (IC50 value 9 nM) when tested in vitro with no effect on the activities of CDK1/2/5/6, JNK1/2/3, c-Src, MEK1, p38 MAP kinase, VEGFR2, and c-fms. In contrast to its effect in vitro, treatment of neurons with GW 5074 causes c-Raf activation (when measured in vitro inthe absence of the drug) and stimulates the Raf-MEK-ERK pathway. GW 5074 protects neurons from death in culture and in an in vivo paradigm of neurodegeneration.

KEYWORDS: GW 5074 | supplier | C-Raf inhibitor | GW5074 | CAS [220904-83-6] | MEK | RAF | Inhibitor | Raf-1 | cell-permeable | activation | Raf-MEK-ERK | pathway | CNS | neurodegeneration | neuroprotection