555550
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).
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)
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所有图片(1)
About This Item
经验公式（希尔记法）:
C16H21N3O2S · 2HCl
CAS号:
分子量:
392.34
MDL编号:
UNSPSC代码:
12352200
NACRES:
NA.54
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质量水平
方案
≥95% (HPLC)
表单
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
SMILES字符串
[S](=O)(=O)(N3[C@H](CNCCC3)C)c1c2c(cncc2C)ccc1.Cl.Cl
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
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.
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
储存分类代码
11 - Combustible Solids
WGK
WGK 1
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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