Rho Kinase Inhibitor-Calbiochem

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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; K_i= 1.6 nM). Exhibits a much weaker affinity for other serine/threonine kinases (K_i= 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 ?g/128 ?l) 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; K_i= 1.6 nM). Inhibits other serine/threonine kinases only at higher concentrations (K_i= 630 nM for PKA, 9.27 ?M for PKC, and 10.1 ?M 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 ?M). 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).

包装

5 mg in Glass bottle
1 mg in Plastic ampoule
Packaged under inert gas

生化/生理作用

Primary Target
ROCK
Target K_i: 1.6 nM against G-protein Rho-associated kinase
Reversible: yes
Cell permeable: yes
Product competes with ATP.

警告

Toxicity: Harmful (C)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

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

基本信息

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安全信息