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GW 5074

CAS No. : 220904-83-6

MCE 站：GW 5074

产品活性：GW 5074 是一种有效的，选择性的 c-Raf 抑制剂，IC₅₀ 值为 9 nM；对 JNK1/2/3，MEK1，MKK6/7，CDK1/2，c-Src，p38 MAP，VEGFR2 或 c-Fms 等没有作用。

研究领域：MAPK/ERK Pathway  |  Apoptosis

作用靶点：Raf  |  Apoptosis

In Vitro: GW5074 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 Vivo: GW5074 (5 mg/Kg) completely prevents extensive bilateral striatal lesions induced by 3-NP in mice. GW5074 suppresses sidestream smoke-induced airway hyperresponsiveness in mice.

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