871543-07-6
| 中文名称 | 871543-07-6 |
|---|---|
| 中文同义词 | RHO激酶抑制剂(H-1152 DIHYDROCHLORIDE);H-1152双盐酸盐;H 1152二盐酸盐 |
| 英文名称 | H1152, DIHYDROCHLORIDE |
| 英文同义词 | 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;4-methyl-5-[[(2S)-2-methyl-1,4-diazepan-1-yl]sulfonyl]isoquinoline;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 |
| 结构式 |  |
871543-07-6 性质
| 熔点 | 182-184°C |
|---|---|
| 储存条件 | Hygroscopic, -20°C Freezer, Under Inert Atmosphere |
| 溶解度 | 溶于甲醇、水 |
| 形态 | 固体 |
| 颜色 | 白色至类白色 |
| 稳定性 | 吸湿性 |
|
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 ) |
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.
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-15720A | 871543-07-6 H-1152 dihydrochloride | 871543-07-6 | 2mg | 1240元 |
| 2024/01/25 | HY-15720A | 871543-07-6 H-1152 dihydrochloride | 871543-07-6 | 10mM * 1mLin DMSO | 1605元 |