H-89 Dihydrochloride

• 产品编号：CST-9844S      品牌：CST       原厂货号：9844S
• 产品分类：生化试剂 > 生物试剂 > 生物活性小分子 > 抑制剂
• 应用分类：

描述：

H-89以5.19mg粉剂提供。储存在-20℃。使用前将粉末溶解于0.5ml DMSO中成为20mM H-89。对于工作浓度为10uM-20uM，将原液按1:2000到1:1000稀释。使用需要的浓度处理细胞30分钟。H-89在粉剂状态比溶液中更稳定；因此推荐在使用前再将其溶解。储存在-20℃或更低温度。H-89是cAMP依赖的蛋白激酶（PKA）的强有力的选择性抑制剂。H-89在体外对PKA的IC50大约是50nM，体内对PKA底物磷酸化的抑制及其相关功能的范围为10uM-30uM（1,2）。除了PKA，H-89也显示出对PKG和PKCμ的中等强度的抑制，IC50在500nM范围内（1,3）。H-89的抑制作用因为竞争性的结合到激酶催化亚基的ATP结合口袋而产生（4）。

1. Chijiwa, T. et al. (1990) J Biol Chem 265, 5267-72.
2. Meja, K.K. et al. (2004) J Pharmacol Exp Ther 309, 833-44.
3. Johannes, F.J. et al. (1995) Eur J Biochem 227, 303-7.
4. Engh, R.A. et al. (1996) J Biol Chem 271, 26157-64.

原厂资料：

Directions for Use

H-89 is supplied as 5.19 mg powder. Store at or below -20ºC. Before usage, dissolve powder in 0.5 ml DMSO to make 20 mM H-89. For working concentrations of 10 μM-20 μM, dilute DMSO stock 1:2000 to 1:1000. Treat cells with the desired concentration for 30 minutes. The H-89 is more stable as a powder than in solution; it is therefore recommended to dissolve as close as possible prior to use. Store solution at or below -20ºC.

Background

H-89 is a potent selective inhibitor of cAMP dependent protein kinase (PKA). The in vitro IC50 of H-89 for PKA is approximately 50 nM and in vivo the inhibitiory effect on PKA substrate phosphorylation and related cellular functions range from 10 μM to 30 μM (1,2). In addition to PKA, H-89 also exhibits a moderate inhibitory effect on PKG and PKCμ, with IC50 in the 500 nM range (1,3). The inhibitory effect of H-89 is due to its competitive binding to the ATP pocket on the kinase catalytic subunit (4).

1. Chijiwa, T. et al. (1990) J Biol Chem 265, 5267-72.
2. Meja, K.K. et al. (2004) J Pharmacol Exp Ther 309, 833-44.
3. Johannes, F.J. et al. (1995) Eur J Biochem 227, 303-7.
4. Engh, R.A. et al. (1996) J Biol Chem 271, 26157-64.

注意事项：

Storage: Store lyophilized or in solution at -20°C, desiccated.
Protect from light. In lyophilized form, the chemical is stable for
24 months. Once in solution, use within 3 months to prevent loss
of potency. Aliquot to avoid multiple freeze/thaw cycles.