PKA抑制剂H-89的生物活性数据?

1个回答

  • 产品描述:x09H 89 2HCl是一种有效的PKA抑制剂,Ki为48 nM,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.

    体外研究:x09H89 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.

    体内研究:x09H89 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.

    更多信息:www.***.cn/products/H-89-dihydrochloride.html