Y27632, 1.61mg

Y27632 is a highly potent, cell-permeable, reversible, and selective inhibitor of Rho-associated protein kinase (Ki = 140 nM for p160ROCK (ROCK-I)(1). It also inhibits ROCK-II with almost equal potency. Inhibition is achieved by competing with ATP for binding to the catalytic site. It exhibits 10- to 50-fold lower affinity for PKCε than p160ROCK but does not affect the activity of p21-activated protein kinase (PAK) even at high concentrations (~100 µM)(2). It also acts as a potent inhibitor of agonist-induced Ca2+ sensitization of myosin phosphorylation and smooth muscle contractions (IC50 = 700 nM for phenylephrine-induced contractions in aortic strips)(3,4). Prevents apoptosis and enhances the survival and cloning efficiency of dissociated human ES cells without affecting their pluripotency(5).

CAS Number
146986-50-7

Chemical Formula
C₁₄H₂₃Cl₂N₃O

Chemical Name
(1R,4r)-4-((R)-1-aminoethyl)-N-(pyridine-4-yl)cyclohexanecarboxamide dihydrochloride

Molecular Weight
320.3

QC Specifications
Mass Spectrometry
Mouse ESC culture for toxicity

Shipping Information
on blue ice

Storage
-20°C, protected from light

Stability
Stable for up to 6 months from date of receipt when stored as directed.

Reference
1.Narumiya, S., et al. Use and properties of ROCK-specific inhibitor Y-27632 (2000) Methods in Enzymology 325:273-284

2.Hirose, M., et al. Molecular dissection of the Rho-associated protein kinase (p160ROCK)-regulated neurite remodeling in neuroblastoma N1E-115 cells (1998) J Cell Biol. 141: 1625-1636

3.Uehata, M., et al. Calcium sensitization of smooth muscle mediated by a Rho-associated protein kinase in hypertension (1997) Nature 389:990-994.

4.Chitaley, K., et al. Antagonism of Rho-kinase stimulates rat penile erection via a nitric oxide-independent pathway (2001) Nat Medicine 7:119-122

5.Watanabe, K., et al. A ROCK inhibitor permits survival of dissociated human embryonic stem cells (2007) Nat Biotech 25: 681-686