| 货号 | 9844S |
| 供应商 | CST |
| 背景 | 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). |
| 存放说明 | |
| 参考文献 | Chijiwa, T. et al. (1990) J Biol Chem 265, 5267-72. Meja, K.K. et al. (2004) J Pharmacol Exp Ther 309, 833-44. Johannes, F.J. et al. (1995) Eur J Biochem 227, 303-7. Engh, R.A. et al. (1996) J Biol Chem 271, 26157-64. |
Western blot analysis of extracts from SKNMC cells, untreated or treated with indicated concentrations of H-89 for 30 minutes, followed by stimulation with 30 µM Forskolin for 10 minutes. The phosphorylation of CREB was detected using Phospho-CREB (Ser133) (87G3) Rabbit mAb #9198 (upper), CREB (48H2) Rabbit mAb #9197 was used as a loading control (lower). H-89 inhibition of Forskolin induced PKA phosphorylation on CREB at Ser133 is shown. 对SKNMC细胞，未处理或所示浓度的H-89处理30分钟，接下来用30 nM Forskolin刺激10分钟。CREB磷酸化使用Phospho-CREB (Ser133) (87G3)兔单抗 #9198检测，CREB（48H2）兔单抗#9197作为装载抗体（下图）。H-89对Forskolin诱导PKA磷酸化CREB Ser133的抑制如图所示。 | |
Structure of H-89. H89的结构 |
