H-1152

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

H-1152 是一种有效、特异性、ATP 竞争性且细胞可渗透的 ROCK 抑制剂 (Ki = 1.6 nM)。

H-1152 is a potent specific ATP-competitive and cell permeable ROCK inhibitor (Ki = 1.6 nM).

H-1152 is an inhibitor of Rho-kinase, with an IC50 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 IC50s 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 Ki of 1.6 nM, and slightly suppresses PKA, PKC and MLCK, with Kis of?0.63, 9.27, and 10.1 μM, respectively. H-1152 (0.1-10 μM) highly inhibits MARCKS phosphorylation, with an IC50 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.

——

——

Cell Cycle/DNA Damage

ROCK

ROCK

——

——

451462-58-1

319.42

C16H21N3O2S

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (313.07 mM)

Cc1cncc2cccc(S(=O)(=O)N3CCCNC[C@@H]3C)c12

4-Methyl-5-[[(2S)-2-methyl-14-diazepan-1-yl]sulfonyl]isoquinoline

(-20℃)

With Ice Pack

≥ 2 years