H 1152二盐酸盐H-1152 dihydrochloride ROCK抑制剂|CAS 871543-07-6（53084ES）

H-1152 dihydrochloride (H1152 dihydrochloride, H-1152 2HCl)，又称H1152二盐酸盐，是异喹啉磺酰胺化合物，是一种膜渗透性、ATP竞争性、选择性ROCK的抑制剂(K_i: 1.6 nM)，对ROCK2的IC₅₀值为12 nM。H-1152对其他丝氨酸/苏氨酸激酶的作用弱得多，如PKA、PKC、Aurora A的IC₅₀值分别为3.03 μM、5.68 μM、0.745 μM。

参考文献

1. Tamura M, et al. Development of specific Rho-kinase inhibitors and their clinical application. Biochim Biophys Acta. 2005 Dec 30;1754(1-2):245-52.
2. Ikenoya M, et al. Inhibition of rho-kinase-induced myristoylated alanine-rich C kinase substrate (MARCKS) phosphorylation in human neuronal cells by H-1152, a novel and specific Rho-kinase inhibitor. J Neurochem. 2002 Apr;81(1):9-16.
3. Lie M, et al. Accelerated neurite growth from spiral ganglion neurons exposed to the Rho kinase inhibitor H-1152. Neuroscience. 2010 Aug 25;169(2):855-62.

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