Rho Kinase Inhibitor-Calbiochem

C₁₆H₂₁N₃O₂S · 2HCl

392.34

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 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; K_i = 1.6 nM). Inhibits other serine/threonine kinases only at higher concentrations (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) 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).

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

Toxicity: Harmful (C)

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

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.

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

100

≥95% (HPLC)

solid

Calbiochem^®

OK to freeze
desiccated (hygroscopic)
protect from light

white

methanol: 5 mg/mL
water: 5 mg/mL

ambient

2-8℃

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

11 - Combustible Solids

WGK 1