GF109203X,133052-90-1

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YZ剂描述：

产品名称：GF109203X

产品别名：3-[1-[3-(二甲氨基)丙基]1H-吲哚-3-基]-4-(吲哚-3-基)1H--2,5二酮

英文别名：Bisindolylmaleimide I;Go 6850

靶点：PKCβ2 ,PKCβ1 ,PKCα ,PKCγ

CAS：133052-90-1

纯度：＞98%

外观：red to orange

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：

GF 109203X是一种有效的PKCYZ剂，YZPKCα，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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