(R)-(+)-trans-N-(4-Pyridyl)-4-(1-aminoethyl)-cyclohexanecarboxamide, 2HCl ROCK Inhibitor White solid. PROTECT FROM LIGHT. HYGROSCOPIC. PACKAGED UNDER INERT GAS. A highly potent, cell-permeable 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 PKCe 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. Purity: ≥95% by HPLC. CAS 146986-50-7. Ref.: 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. Science 285, 895. Uehata, M., et al. 1997. Nature 389, 990. R: 20/21/22; S: 36 Sold under license of U.S. Patent 4,997,834 and PCT Application W098/06,433A1 and under license from Mitsubishi Pharma Tanabe Corporation. |