中文名 | H1152 Dihydrochloride |
英文名 | H-1152 Dihydrochloride |
别名 | RHO激酶抑制剂(H-1152 DIHYDROCHLORIDE) |
英文别名 | 871543-07-6 H-1152 2HCl H1152 Dihydrochloride H 1152 DIHYDROCHLORIDE H1152, DIHYDROCHLORIDE H-1152 Dihydrochloride H1152 DIHYDROCHLORIDE 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 H1152P2HCl,(S)-(+)-2-Methyl-1-[(4-methyl-5-isoquinolynyl)sulfonyl]homopiperazineDihydrochloride H1152P Dihydrochloride, (S)-(+)-2-Methyl-1-[(4-methyl-5-isoquinolynyl)sulfonyl]homopiperazine Dihydrochloride |
CAS | 871543-07-6 |
化学式 | C16H21N3O2S |
分子量 | 319.42184 |
熔点 | 182-184°C |
溶解度 | 甲醇、水 |
存储条件 | Hygroscopic, -20°C Freezer, Under Inert Atmosphere |
稳定性 | 吸湿性 |
外观 | 固体 |
颜色 | White to Off-White |
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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.549 ml | 12.744 ml | 25.488 ml |
5 mM | 0.51 ml | 2.549 ml | 5.098 ml |
10 mM | 0.255 ml | 1.274 ml | 2.549 ml |
5 mM | 0.051 ml | 0.255 ml | 0.51 ml |
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