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Merck
CN
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文件

555550

Sigma-Aldrich

Rho激酶抑制剂

The Rho kinase inhibitor, CAS 872543-07-6, is a cell-permeable, highly specific, reversible, potent, and ATP-competitive inhibitor of Rho-associated kinase (ROCK; Ki = 1.6 nM).

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别名:
Rho激酶抑制剂, H-1152，H-1152P，(S)-(+)-2-甲基-1-[(4-甲基-5-异喹啉)磺酰基]高哌嗪，2HCl，ROCK抑制剂，二甲基法舒地尔(diMF，H-1152P)
经验公式（希尔记法）:
C16H21N3O2S · 2HCl
CAS号:
871543-07-6
分子量:
392.34
UNSPSC代码:
12352200
NACRES:
NA.54

质量水平

100

检测方案

≥95% (HPLC)

形式

solid

制造商/商品名称

Calbiochem®

储存条件

OK to freeze
desiccated (hygroscopic)
protect from light

颜色

white

溶解性

methanol: 5 mg/mL
water: 5 mg/mL

运输

ambient

储存温度

2-8°C

InChI

1S/C16H21N3O2S.2ClH/c1-12-9-18-11-14-5-3-6-15(16(12)14)22(20,21)19-8-4-7-17-10-13(19)2;;/h3,5-6,9,11,13,17H,4,7-8,10H2,1-2H3;2*1H/t13-;;/m0../s1

InChI key

BFOPDSJOLUQULZ-GXKRWWSZSA-N

一般描述

一种细胞可渗透性氯硝基苯甲酰胺化合物，可作为G蛋白Rho相关激酶（ROCK；Ki =1.6 nM）的高度特异性、可逆、有效和ATP竞争性抑制剂。仅在较高浓度下抑制其他丝氨酸/苏氨酸激酶（PKA的Ki=630nm，PKC的Ki=9.27µM，MLCK的Ki=10.1µM）。在NT-2细胞（IC50=2.5 µM）中，显示出选择性阻断溶血磷脂酸诱导的、但不是PDBu诱导的豆蔻酰化富含丙氨酸的C激酶底物（MARKS）的磷酸化。据报道，是一种比Y-27632（目录号688000&688001）更有效、更具选择性的抑制剂。主靶极光激酶A，诱导急性巨核细胞白血病细胞（AMKL）多倍体化。
一种细胞可渗透性氯硝基苯甲酰胺化合物，可作为G蛋白Rho相关激酶（ROCK；Ki =1.6 nM）的高度特异性、可逆、有效和ATP竞争性抑制剂。对其他丝氨酸/苏氨酸激酶的亲和力要弱得多（PKA的Ki=630nm，PKC的Ki=9.27μM，MLCK的Ki=10.1μM）。在NT-2细胞（IC50 = 2.5 μM)）中，显示出选择性阻断溶血磷脂酸诱导的、但不是PDBu诱导的豆蔻酰化富含丙氨酸的C激酶底物的磷酸化。据报道比Y-27632（目录号688000和688001）更具效力和选择性。主靶极光激酶A，诱导急性巨核细胞白血病细胞（AMKL）多倍体化。 也可提供10 mM (500 µg/128 µlRho激酶抑制剂（目录号555552）的H2O溶液。

生化/生理作用

主要靶标
ROCK
产物与ATP竞争。
可逆性：是
细胞可渗透性：是
靶标Ki：对G蛋白Rho相关激酶为1.6 nM

包装

用惰性气体包装

警告

毒性：有害（C）

重悬

复溶后，等分并冷冻保存（-20°C）。贮备溶液在-20°C下可稳定保存至多6个月。

其他说明

Wen, Qiang, et al. 2012.Cell150, 575.
Ikenoya, M., et al. 2002.J. Neurochem.81, 9.
Sasaki, Y., et al. 2002.Pharmacol.Ther.93, 225.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

WGK

WGK 1

闪点(°F)

Not applicable

闪点(°C)

Not applicable

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