C-Raf inhibitor,potent and selective
CAS：220904-83-6
分子式：C15H8Br2INO2
分子量：520.95
纯度：98%
存储：Store at -20°C

Background:

GW5074 is a synthetic inhibitor of c-Raf with IC50 value of 9nM [1].

GW5074 is found to be a potent inhibitor of c-Raf and has no effect on cdk1, cdk2, c-src, p38 MAP kinase, VEGFR2 and c-fms. GW5074 also shows no direct effect on JNK proteins and p38 MAP kinase. In neurons, GW5074 reduces the phosphorylation level of c-Raf at Ser259, results in an induction of c-Raf activity. It is further proved that GW5074 shows neuroprotective efficacy when its dose is below 1μM. In addition, GW5074 suppresses cell apoptosis through delaying the down-regulation of Akt phosphorylation and preventing the activation of GSK3β. In the in vivo model of Huntington’s disease, GW5074 protects neurons via resisting 3-NP-induced striatal neurodegeneration [1].

参考文献:
[1] Burgess S, Echeverria V. Raf inhibitors as therapeutic agents against neurodegenerative diseases. CNS & Neurological Disorders-Drug Targets (Formerly Current Drug Targets-CNS & Neurological Disorders), 2010, 9(1): 120-127.