产品信息
抗原名称
C-Raf
商品描述
GW 5074是可渗透入细胞的c-Raf1激酶选择性抑制剂，IC50为9nM，有超过100倍的选择性对CDK1，CDK2，c-src，ERK2，MEK，p38，Tie2，VEGFR2和c-fms。
分子量
520.94
纯度
98%
可溶性
DMSO : 96 mg/mL (184.3 mM)
外观
yellow to orange-brown solid
In vitro(体外研究)
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(体内研究)
GW5074 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.
背景
分子式
C15H8Br2INO2
CAS号
220904-83-6
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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