ROCK Inhibitor

Y 27632 is a cell-permeable and selective inhibitor of Rho-associated, coiled-coil-containing protein kinase (ROCK) and 1 is its dihydrochloride. Y 27632 inhibits ROCK1 (K_i = 220 nM) and ROCK2 (K_i = 300 nM). The inhibition manner of the enzymes by Y 27632 is competitive with ATP for binding to the catalytic site.^1,2) Y 27632 also prevents dissociation-induced apoptosis (anoikis) of human embryonic stem (ES) cells, when they are dissociated to single cells. Therefore, cloning efficiency of human ES cells is increased by the use of Y 27632.³⁾

References

• 1) Specificity and mechanism of action of some commonly used protein kinase inhibitors
• S. P. Davies, H. Reddy, M. Caivano, P. Cohen, Biochem. J. 2000, 351, 95.
• 2) Pharmacological properties of Y-27632, a specific inhibitor of rho-associated kinases.
• T. Ishizaki, M. Uehata, I. Tamechika, J. Keel, K. Nonomura, M. Maekawa S. Narumiya, Mol. Pharmacol. 2000, 57, 976.
• 3) A ROCK inhibitor permits survival of dissociated human embryonic stem cells
• K. Watanabe, M. Ueno, D. Kamiya, A. Nishiyama, M. Matsumura, T. Wataya, J. B. Takahashi, S. Nishikawa, S. Nishikawa, K. Muguruma, Y. Sasai, Nat. Biotechnol. 2007, 25, 681.

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