H-89 2HCl

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抑制剂描述：

产品名称：H-89 2HCl

产品别名：见爱必信官网

英文别名：H-89 2HCl

靶点：PKA

CAS：130964-39-5

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：

H892HCl是一种有效的PKA抑制剂，无细胞试验中Ki为48nM，作用于PKA比作用于PKG选择性高10倍，比作用于PKC，MLCK，钙调蛋白激酶II和酪蛋白激I/II选择性高500倍。

溶解性：DMSO：104 mg/mL (200.27 mM) Water：6 mg/mL (11.55 mM)

体外研究：

H89 2HCl is a potent PKA (cAMP-dependent) protein kinase A inhibitor with Ki of 48 nM, exhibits 10-fold selectivity over PKG, exhibits >500-fold selectivity over PKC, MLCK, calmodulin kinase II and casein kinase I/II. Pretreatment of the cells with H-89 (30 μM) 1 h before the addition of forskolin markedly inhibits the forskolin-induced protein phosphorylation in a dose-dependent manner. H89 also inhibits several other kinases with IC50 of 80, 120, 135, 270, 2600 and 2800 nM for S6K1, MSK1, PKA, ROCKII, PKBα and MAPKAP-K1b, respectively. H89 also has activity at some cellular receptors and ion channels, including Kv1.3 K+ channels,β1AR and β2AR.

体内研究：H89 causes distinct modifications of protein phosphorylation, with the most robust changes in phosphorylation are fructose-1,6-biphosphatase, heterogeneous nuclear ribonucleoprotein (hnRNP), NSFL1 cofactor p47, all which have potentially regulatory connections to cAMP/PKA. H-89 (0.5, 1, 5 mg/kg) significantly attenuates prominent behavioral signs of morphine withdrawal in morphine-dependent mice.

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