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Rho Kinase Inhibitor-Calbiochem

产品编号:4085839
规格: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).
CAS NO:871543-07-6
包装规格:1 MG,5 MG
产品类别:进口试剂
品牌:Sigma-Aldrich
优惠价:立即咨询
产品价格
产品编号包装单位单价(元)国内现货国外库存询价单
40858391 MG4000
40858395 MG8420
产品别名

871543-07-6

Rho Kinase Inhibitor-Calbiochem

H-1152, H-1152P, (S)-(+)-2-Methyl-1-[(4-methyl-5-isoquinolinyl)sulfonyl]homopiperazine, 2HCl, ROCK Inhibitor, Dimethylfasudil (diMF, H-1152P)

基本信息
Empirical Formula【经验(实验)分子式】
C16H21N3O2S · 2HCl
Molecular weight
392.34
General description【一般描述】
A cell-permeable isoquinolinesulfonamide compound that acts as a highly specific, reversible, potent, and ATP-competitive inhibitor of G-protein Rho-associated kinase (ROCK; Ki = 1.6 nM). Exhibits a much weaker affinity for other serine/threonine kinases (Ki = 630 nM for PKA, 9.27 μM for PKC, and 10.1 μM for MLCK). Shown to selectively block lysophosphatidic acid-induced, but not PDBu-induced, phosphorylation of myristoylated alanine-rich C kinase substrate MARCKS (IC50 = 2.5 μM) in NT-2 cells. Reported to be more potent and selective than Y-27632 (Cat. Nos. 688000 and 688001). Mainly targets Aurora Kinase A, and induces polyploidization of acute megakaryocytic leukemia cells (AMKL). At 10 mM (500 µg/128 µl) solution of Rho Kinase Inhibitor (Cat. No. 555552) in H2O is also available.
A cell-permeable isoquinolinesulfonamide compound that acts as a highly specific, reversible, potent, and ATP-competitive inhibitor of G-protein Rho-associated kinase (ROCK; Ki = 1.6 nM). Inhibits other serine/threonine kinases only at higher concentrations (Ki = 630 nM for PKA, 9.27 µM for PKC, and 10.1 µM for MLCK). Shown to selectively block lysophosphatidic acid-induced, but not PDBu-induced, phosphorylation of myristoylated alanine-rich C kinase substrate (MARCKS) in NT-2 cells (IC50 = 2.5 µM). Reported to be a more potent and selective inhibitor than Y-27632 (Cat. No. 688000 & 688001). Mainly targets Aurora Kinase A, and induces polyploidization of acute megakaryocytic leukemia cells (AMKL).
Biochem/physiol Actions【生化/生理作用】
Primary Target
ROCK
Target Ki: 1.6 nM against G-protein Rho-associated kinase
Reversible: yes
Cell permeable: yes
Product competes with ATP.
Warning【警告】
Toxicity: Harmful (C)
Reconstitution【重悬】
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes【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.
Legal Information【法律信息】
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
产品性质
Quality Level【质量水平】
100
Assay【测定】
≥95% (HPLC)
form【形式】
solid
manufacturer/tradename
Calbiochem®
storage condition【储存条件】
OK to freeze
desiccated (hygroscopic)
protect from light
color【颜色】
white
solubility【溶解性】
methanol: 5 mg/mL
water: 5 mg/mL
shipped in【运输】
ambient
storage temp.【储存温度】
2-8℃
packaging【包装】
5 mg in Glass bottle
1 mg in Plastic ampoule
Packaged under inert gas
安全信息
Storage Class Code【储存分类代码】
11 - Combustible Solids
WGK
WGK 1
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