中文名称:

871543-07-6

中文同义词:

RHO激酶抑制剂(H-1152 DIHYDROCHLORIDE)

英文名称:

H1152, DIHYDROCHLORIDE

英文同义词:

4-methyl-5-[[(2S)-2-methyl-1,4-diazepan-1-yl]sulfonyl]isoquinoline;5-[[(2S)-Hexahydro-2-Methyl-1H-1,4-diazepin-1-yl]sulfonyl]-4-Methylisoquinoline;H1152, DIHYDROCHLORIDE;H1152P2HCl,(S)-(+)-2-Methyl-1-[(4-methyl-5-isoquinolynyl)sulfonyl]homopiperazineDihydrochloride;H1152P Dihydrochloride, (S)-(+)-2-Methyl-1-[(4-methyl-5-isoquinolynyl)sulfonyl]homopiperazine Dihydrochloride;H-1152 2HCl;H 1152 DIHYDROCHLORIDE; H1152 DIHYDROCHLORIDE

CAS号:

871543-07-6

分子式:

C16H21N3O2S

分子量:

319.42184

EINECS号:

相关类别:

细胞生物学试剂;Protein Kinase Inhibitors and Activators;Inhibitors;All Inhibitors;Intermediates Fine Chemicals;Pharmaceuticals

Mol文件:

871543-07-6.mol

熔点 

182-184°C

储存条件 

Hygroscopic, -20°C Freezer, Under Inert Atmosphere

生物活性

H-1152 dihydrochloride 是一种膜通透的，选择性的 ROCK 抑制剂，Ki 值为 1.6 nM，对 ROCK2 的 IC50 值为 12 nM。

靶点

ROCKII 12 nM (IC 50 ) CaMKII 0.18 μM (IC 50 ) PKG 0.36 μM (IC 50 ) AuroraA 0.745 μM (IC 50 ) PKA 3.03 μM (IC 50 ) Src 3.06 μM (IC 50 ) PKC 5.68 μM (IC 50 ) Abl 7.77 μM (IC 50 ) MKK4 16.9 μM (IC 50 ) MLCK 28.3 μM (IC 50 ) EGFR 50 μM (IC 50 ) GSK3α 60.7 μM (IC 50 ) AMPK 100 μM (IC 50 ) P38α 100 μM (IC 50 )

ROCKII 12 nM (IC 50 )

CaMKII 0.18 μM (IC 50 )

体外研究

H-1152 dihydrochloride is an inhibitor of Rho-kinase, with an IC 50 of 12 nM for ROCK2. H-1152 (H-1152P) also shows less inhibitory activities against CaMKII, PKG, AuroraA, PKA, Src, PKC, MLCK, Abl, EGFR, MKK4, GSK3α, AMPK, and P38α, with IC 50 s of 0.180, 0.360, 0.745, 3.03, 3.06, 5.68, 28.3, 7.77, 50.0, 16.9, 60.7, 100, and 100 μM, respectively. H-1152 potently inhibits Rho kinase, with a K i of 1.6 nM, and slightly suppresses PKA, PKC and MLCK, with K i s of 0.63, 9.27, and 10.1 μM, respectively. H-1152 (0.1-10 µM) highly inhibits MARCKS phosphorylation, with an IC 50 value of 2.5 µM in LPA-treated cells, but shows no such obvious effects in PDBu-treated cells. H-1152 (0.5-10 μM) cuases no decreased neuronal survival. H-1152 (1, 5 or 10 μM) also exerts no alterations in the ratios of different neuronal morphologies. Furthermore, H-1152 (10 μM) increases neurite length in both BMP4 and LIF cultures.