871543-07-6

中文名称 871543-07-6

英文名称 H1152, DIHYDROCHLORIDE

CAS 871543-07-6

分子式 C16H21N3O2S

分子量 319.422

MOL 文件 871543-07-6.mol

871543-07-6 结构式

基本信息物理化学性质图谱信息 871543-07-6价格(试剂级) 常见问题列表

基本信息

中文别名

H-1152双盐酸盐
RHO激酶抑制剂(H-1152 DIHYDROCHLORIDE)

英文别名

H-1152 2HCl
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

所属类别

生物化工：激动剂抑制剂

物理化学性质

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

颜色白色至灰白色

稳定性吸湿性

图谱信息

871543-07-6(871543-07-6)核磁图(¹HNMR)

871543-07-6价格(试剂级)

报价日期	产品编号	产品名称	CAS号	包装	价格
2024/04/30	HY-15720A	871543-07-6 H-1152 dihydrochloride	871543-07-6	2mg	1240元
2024/04/30	HY-15720A	871543-07-6 H-1152 dihydrochloride	871543-07-6	10mM * 1mLin DMSO	1605元
2024/01/25	HY-15720A	871543-07-6 H-1152 dihydrochloride	871543-07-6	5mg	1860元

常见问题列表

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 )

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.