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抑制剂描述:

产品名称:GF109203X

产品别名:见爱必信官网

英文别名:GF109203X

靶点:PKC

CAS:133052-90-1

纯度:>98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

GF 109203X是一种有效的PKC抑制剂,抑制PKCα,PKCβI,PKCβII和PKCγ,IC50分别为20 nM,17 nM,16nM和20 nM,作用于PKC比作用于EGFR,PDGFR和胰岛素受体选择性高3000倍以上。

溶解性:DMSO : ≥ 32 mg/mL (77.58 mM)

体外研究:

GF109203X, as an ATP-competitive PKC inhibitor, prevents platelet aggregation induced by stimuli that activate PKC, and has the potential as a tool for studying the involvement of PKC in signal transduction pathways. GF 109203X produces reversal activity on P-glycoprotein and MRP -mediated multidrug resistance. PKC inhibition by GF109203X significantly reduces carbachol-stimulated ERK1/2 activation and the subsequent proliferation of SNU-407 colon cancer cells.

体内研究:GF109203X (10 μg/mouse, i.pl.) dose-dependently inhibits BK-induced mechanical allodynia in Wistar rats.

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