Y-27632 DIHYDROCHLORIDE Inhibitor CAS No. 146986-50-7

Product Name	Y-27632 DIHYDROCHLORIDE
CAS No.	146986-50-7
Molecular Weight	247.26
Formula	C₁₄H₂₁N₃O.₂HCl
Chemical Name	(R)-(+)-TRANS-N-(4-PYRIDYL)-4-(1-AMINOETHYL)-CYCLOHEXANECARBOXAMIDE 2HCL
Smiles	[C@@H]1(CCC(CC1)[C@@H](C)N)C(=O)Nc1ccncc1
Chemical Structure
Documents	HPLC COA

Biological activities

Y-27632 is a potent, highly specific, cell-permeable inhibitor of Rho kinase (ROCK) with K_{i of 140 nM. ^[1] Y-27632 inhibits both Rho kinase 1 and Rho kinase 2 with K_{i of 0.14 and 1.0 µM, respectively. Treatment of human trabecular meshwork (HTM) and schlemm?? canal (SC) cells with Y-27632 triggers the dephosphorylation of myosin light chain. Y-27632 modulates monolayer permeability/barrier function in SC cells. Treatment of HTM and SC cells with Y-27632 induces changes in cell morphology and leads to decreases in actin stress fibers and focal adhesions and in levels of protein phosphotyrosine, compared with untreated controls. Aqueous humor out flow facility increases (40%??0%) in enucleated porcine eyes perfused with Y-27632 (10-100 mM). ^[2] Y-27632 prevents the migration of rat MM1 hepatoma cells. ^[1] Y-27632 significantly attenuates constrictions induced by either KCl physiological salt solution (KPSS) or PGF^2α in a concentration-dependent manner. Y-27632 inhibits phase 2 of hypoxic pulmonary vasoconstriction (HPV) in concentration-dependent manner with an IC50 of 300 nM. Y-27632 inhibits HPV in perfused rat lungs, phase 1 and phase 2 of HPV in rat intrapulmonary arteries (IPA), and also inhibits PGF2a-induced and KPSS-induced constriction of rat IPA. ^[3] Y-27632 inhibits the contractions induced not only by receptor agonists but also by high K⁺ with the similar IC50 (0.8-4.9 µM). Y-27632 disrupts the actin filament network and decreases the filamentous actin. ^[4]Y-27632 is a potential therapeutic to treat elevated ocular pressure in glaucoma patients. ^[2]}}

Protocols

Y-27632 is dissolved in DMSO. ^[4]

References

[1] Breitenlechner C, et al. Protein kinase A in complex with Rho-kinase inhibitors Y-27632, Fasudil, and H-1152P: structural basis of selectivity. Structure. 2003, 11(12): 1595-1607. [2] Rao PV, et al. Modulation of aqueous humor outflow facility by the Rho kinase-specific inhibitor Y-27632. Invest Ophthalmol Vis Sci. 2001, 42(5): 1029-1037. [3] Robertson TP, et al. Inhibition of sustained hypoxic vasoconstriction by Y-27632 in isolated intrapulmonary arteries and perfused lung of the rat. Br J Pharmacol. 2000, 131(1): 5-9. [4] Sakamoto K, et al. Inhibition of high K+-induced contraction by the ROCKs inhibitor Y-27632 in vascular smooth muscle: possible involvement of ROCKs in a signal transduction pathway. J Pharmacol Sci. 2003, 92(1): 56-69.

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