Description
General description
A highly potent, cell-permeable, reversible, and selective inhibitor of Rho-associated protein kinases (Ki = 140 nM for p160ROCK). Also inhibits ROCK-II with equal potency. The inhibition is competitive with respect to ATP. Exhibits 10- to 50-fold lower affinity for PKCε than p160ROCK. Does not affect the activity of p21-activated protein kinase (PAK) even at higher concentrations (~100 µM). Also acts as a potent inhibitor of agonist-induced Ca²⁺ sensitization of myosin phosphorylation and smooth muscle contraction. Prevents apoptosis and enhances the survival and cloning efficiency of dissociated hES cells without affecting their pluripotency. Pretreatment with Y-27632 reduces the risk of lung injury in rat models of sepsis. A 5 mM (500 µg/296 µl) solution of Y-27632 (Cat. No. 688001) in H₂O and a 10 mM solution in DMSO (Cat. No. 688002) are also available.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
p160 Rho-associated protein kinases (ROCK)
Product competes with ATP.
Reversible: yes
Target Ki: 140 nM for p160 Rho-associated protein kinases (ROCK)
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for 6 months at -20°C.
Other Notes
Cinel, I., et al. 2012. J. Thorac . Dis.4, 30.
Watanabe, K., et al. 2007. Nature Biotech.25, 681.
Chitaley, K., et al. 2001. Nat. Med.7, 119.
Davies, S.P., et al. 2000. Biochem. J. 351, 95.
Narumiya, S., et al. 2000. Methods Enzymol.325, 273.
Hirose, M., et al. 1998. J. Cell Biol.141, 1625.
Maekawa, M., et al. 1999. Science285, 895.
Uehata, M., et al. 1997. Nature389, 990.
Legal Information
Sold under license of PCT Application W098/06,433A1 and under license from Mitsubishi Pharma Tanabe Corporation.
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Harmful (C)
