Y-27632 2HCl - CAS 129830-38-2
Catalog number: B0084-457869
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C14H21N3O.2HCl
Molecular Weight:
320.26
COA:
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Targets:
ROCK
Description:
Y-27632 2HCl inhibits ROCK-II while displaying little activity against PKC, cAMP-dependent protein kinase and myosin light-chain kinase (MLCK) with Ki of 26 μM, 25 μM and > 250 μM, respectively.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-457869 50 mg $228 In stock
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Purity:
>98%
Related CAS:
129830-38-2 ( Y27632 2HCl); 3146986-50-7 ( Y27632 free base)
Appearance:
white to off-white solid powder
Synonyms:
(1R,4r)-4-((R)-1-aminoethyl)-N-(pyridin-4-yl)cyclohexanecarboxamide dihydrochloride; Y27632; Y-27632; Y 27632; Y27632 HCl; Y27632 dihydrochloride
MSDS:
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InChIKey:
IDDDVXIUIXWAGJ-LJDSMOQUSA-N
InChI:
1S/C14H21N3O.2ClH/c1-10(15)11-2-4-12(5-3-11)14(18)17-13-6-8-16-9-7-13;;/h6-12H,2-5,15H2,1H3,(H,16,17,18);2*1H/t10-,11-,12-;;/m1../s1
Canonical SMILES:
O=C([C@H]1CC[C@H]([C@H](N)C)CC1)NC2=CC=NC=C2.[H]Cl.[H]Cl
1.Sertoli-germ cell adherens junction dynamics in the testis are regulated by RhoB GTPase via the ROCK/LIMK signaling pathway.
Lui WY1, Lee WM, Cheng CY. Biol Reprod. 2003 Jun;68(6):2189-206. Epub 2003 Jan 22.
During spermatogenesis, cell-cell actin-based adherens junctions (AJs), such as ectoplasmic specializations (ESs), between Sertoli and germ cells undergo extensive restructuring in the seminiferous epithelium to facilitate germ cell movement across the epithelium. Although the mechanism(s) that regulates AJ dynamics in the testis is virtually unknown, Rho GTPases have been implicated in the regulation of these events in other epithelia. Studies have shown that the in vitro assembly of the Sertoli-germ cell AJs but not of the Sertoli cell tight junctions (TJs) is associated with a transient but significant induction of RhoB. Immunohistochemistry has shown that the localization of RhoB in the seminiferous epithelium is stage specific, being lowest in stages VII-VIII prior to spermiation, and displays cell-specific association during the epithelial cycle. Throughout the cycle, RhoB was localized near the site of basal and apical ESs but was restricted to the periphery of the nuclei in elongating (but not elongated) spermatids, spermatocytes, and Sertoli cells.
2.Cerivastatin, a hydroxymethylglutaryl coenzyme A reductase inhibitor, inhibits cardiac myocyte hypertrophy induced by endothelin.
Nishikimi T1, Tadokoro K, Wang X, Mori Y, Asakawa H, Akimoto K, Yoshihara F, Horio T, Minamino N, Matsuoka H. Eur J Pharmacol. 2002 Oct 25;453(2-3):175-81.
We investigated the direct effects of cerivastatin on hypertrophy of cultured rat neonatal myocytes induced by endothelin and the mechanism by which cerivastatin exerts its effects. Endothelin significantly increased [14C]phenylalanine ([14C]Phe) incorporation, atrial natriuretic peptide (ANP) release, ANP mRNA expression and cell size. Cerivastatin significantly reduced the increase in [14C]phenylalanine incorporation, ANP peptide release, ANP mRNA expression and cell size induced by endothelin, but pravastatin did not. Exogenous mevalonate completely prevented the inhibitory effect of cerivastatin on [14C]phenylalanine incorporation, ANP release and cell size. Cotreatment with geranylgeranyl pyrophosphate also attenuated the effect of cerivastatin on [14C]phenylalanine incorporation, but cotreatment with farnesyl pyrophosphate or squalene did not. Furthermore, both Rho inhibitor C3 exoenzyme and Rho-dependent kinase inhibitor, (R)-(+)-trans-N-(4-pyridyl)-4-(1-aminoethyl)-cyclohexanecarboxamide.
3.Rho-kinase inhibitor upregulates migration by altering focal adhesion formation via the Akt pathway in colon cancer cells.
Adachi S1, Yasuda I, Nakashima M, Yamauchi T, Yoshioka T, Okano Y, Moriwaki H, Kozawa O. Eur J Pharmacol. 2011 Jan 10;650(1):145-50. doi: 10.1016/j.ejphar.2010.10.014. Epub 2010 Oct 16.
Although Rho-kinase is reportedly implicated in carcinogenesis and the progression of human cancers, its precise mechanism has not been fully elucidated. We recently reported that Rho-kinase negatively regulates epidermal growth factor (EGF)-stimulated cancer progression in SW480 colon cancer cells. In the present study, we investigated the effect of Rho-kinase on the migration of SW480 colon cancer cells and the mechanism underlying the involvement of Rho-kinase. Interestingly, (R)-(+)-trans-N-(4-pyridyl)-4-(1-aminoethyl)-cyclohexanecarboxamide, 2HCl (Y27632), a specific inhibitor of Rho-kinase, dose-dependently enhanced cell migration. SW480 cells spontaneously release vascular endothelial growth factor (VEGF), however, Y27632 had little effect on its release. While Rho-kinase, which is generally phosphorylated in unstimulated cells, was clearly suppressed by Y27632, exogenous VEGF did not affect its phosphorylation. Immunofluorescence microscopy revealed that Y27632 caused a dramatic change in the localization of focal adhesion components, vinculin, phosphorylated caveolin-1 and tyrosine-phosphorylated proteins in SW480 cells.
4.M2 and M3 muscarinic receptor activation of urinary bladder contractile signal transduction. II. Denervated rat bladder.
Braverman AS1, Doumanian LR, Ruggieri MR Sr. J Pharmacol Exp Ther. 2006 Feb;316(2):875-80. Epub 2005 Oct 21.
Normal rat bladder contractions are mediated by the M(3) muscarinic receptor subtype. The M(2) receptor subtype mediates contractions of the denervated, hypertrophied bladder. This study determined signal transduction mechanisms mediating contraction of the denervated rat bladder. Denervated bladder muscle strips were exposed to inhibitors of enzymes thought to be involved in signal transduction in vitro followed by a cumulative carbachol concentration-response curve. Outcome measures were the maximal contraction, the potency of carbachol, and the affinity of darifenacin for inhibition of contraction. Inhibition of phosphoinositide-specific phospholipase C (PI-PLC) with 1-O-octadecyl-2-O-methyl-sn-glycero-3-phosphorylcholine (ET-18-OCH(3)) has no effect on denervated bladder contractions, whereas inhibition of phosphatidyl choline-specific phospholipase C (PC-PLC) with O-tricyclo[5.2.1.02,6]dec-9-yl dithiocarbonate potassium salt (D609) attenuates the carbachol maximum and potency.
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CAS 129830-38-2 Y-27632 2HCl

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