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Y-27632 . dihydrochloride

ROCK inhibitor
 
ALX-270-333-M001 1 mg 85.00 USD
 
ALX-270-333-M005 5 mg 174.00 USD
 
ALX-270-333-M025 25 mg 543.00 USD
Do you need bulk/larger quantities?
 
Replaces Prod. #: BML-EI299

  • High potency inhibitor of smooth muscle contractions
  • Applications in nephrology, stem cell studies, cardiovascular, cancer, and neurology
  • Highly cited
Y-27632 is a highly potent, cell permeable, selective and ATP competitive inhibitor of ROCK1 and ROCK2 (IC50=800nM). It acts as a potent inhibitor of agonist-induced Ca2+sensitization of myosin phosphorylation and smooth muscle contractions, blocking cell spreading and suppresses RhoA-induced formation of stress fibers in hepatic stellate cells. Y-27632 significantly reduces the increase of inflammatory cytokines after reperfusion, preventing the development of acute renal failure. There are numerous application for this compound including: cardioprotective effects, suppression of tumor cell invasion, inhibition of superoxide production, mimicking effect of β-agonists on human cells, and an antinociceptive effect.
 
There has been a growing interest in Y-27632 for use in stem cell self-renewal and reprogramming. It is known to increase the survival rate of human embryonic stem cells undergoing cryopreservation.

Product Specification

Alternative Name:(R)-(+)-trans-N-(4-Pyridyl)-4-(1-aminoethyl)-cyclohexanecarboxamide . 2HCl
 
Formula:C14H21N3O . 2HCl
 
MW:247.3 . 73.0
 
CAS:129830-38-2
 
Purity:≥98% (HPLC (UV))
 
Purity Detail:Enantiomeric excess ≥96%
 
Identity:Determined by MS, 1H- and 13C-NMR.
 
Appearance:White to pale yellow powder.
 
Solubility:Soluble in DMSO (25mg/ml), methanol (25mg/ml), acetonitrile (<1mg/ml), dioxan (<1mg/ml), water (very soluble).
 
Shipping:Ambient
 
Long Term Storage:-20°C
 
Use/Stability:Stock solutions are stable for up to 1 month when stored at -20°C.
 
Handling:Protect from light. Packaged under inert gas. After reconstitution, prepare aliquots and store at -20°C.
 
270-333
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Product Literature References

Conditionally reprogrammed normal and primary tumor prostate epithelial cells: a novel patient-derived cell model for studies of human prostate cancer: O.A. Timofeeva, et al.; Oncotarget 8, 22741 (2017), Application(s): Cell culture, Abstract; Full Text
Epithelial tension in the second heart field promotes mouse heart tube elongation: A. Francou, et al.; Nat. Commun. 8, 14770 (2017), Abstract; Full Text
Potential antitumor activity and apoptosis induction of Glossostemon bruguieri root extract against hepatocellular carcinoma cells: M.S. Alwhibi, et al.; Evid. Based Complement Alternat. Med. 2017, 7218562 (2017), Application(s): Cell culture, Abstract; Full Text
A comparison of strategies for immortalizing mouse embryonic fibroblasts: M.M. St. Amad, et al.; J. Biol. Methods 3, e41 (2016), Application(s): Immortalization via Rock inhibitor supplementation, Full Text
Caffeine Suppresses the Progression of Human Glioblastoma via Cathepsin B and MAPK Signaling Pathway: Y.C. Cheng, et al.; J. Nutr. Biochem. 33, 63 (2016), Application(s): Cell culture, Abstract;
Down-regulation of 14-3-3 Zeta Inhibits TGF-β1-Induced Actomyosin Contraction in Human Trabecular Meshwork Cells Through RhoA Signaling Pathway: Y. Ye, et al.; Invest. Ophthalmol. Vis. Sci. 57, 719 (2016), Application(s): Cell culture, Abstract; Full Text
Endothelin A receptor drives invadopodia function and cell motility through the β-arrestin/PDZ-RhoGEF pathway in ovarian carcinoma: E. Semprucci, et al.; Oncogene 35, 3432 (2016), Application(s): Cell culture , Abstract;
Generation and characterization of rat liver stem cell lines and their engraftment in a rat model of liver failure: E.W. Kuijk, et al.; Sci. Rep. 6, 22154 (2016), Application(s): Rat liver stem cell isolation and culture, Abstract; Full Text
Single-cell functional analysis of parathyroid adenomas reveals distinct classes of calcium sensing behaviour in primary hyperparathyroidism: J. Koh, et al. ; J. Cell Mol. Med. 20, 351 (2016), Application(s): Cell culture, Abstract; Full Text
The impact of low-frequency, low-force cyclic stretching of human bronchi on airway responsiveness: M. Le Guen, et al.; Respir. Res. 17, 151 (2016), Abstract; Full Text
Generation of iPSCs as a Pooled Culture Using Magnetic Activated Cell Sorting of Newly Reprogrammed Cells: W. Yang, et al.; PLoS One 10, e0134995 (2015), Application(s): Cell culture, Abstract; Full Text
High-efficiency reprogramming of fibroblasts into cardiomyocytes requires suppression of pro-fibrotic signalling: Y. Zhao, et al.; Nat. Commun. 6, 8243 (2015), Application(s): Cell Culture, Abstract; Full Text
The effect of ROCK on TNF-α-induced CXCL8 secretion by intestinal epithelial cell lines is mediated through MKK4 and JNK signaling: A.C. Perey, et al.; Cell Immunol. 293, 80 (2015), Application(s): Cell Culture, Abstract;
Vaginal innate immune mediators are modulated by a water extract of Houttuynia cordata Thunb: S. Satthakarn, et al.; BMC Complement. Altern. Med. 15, 183 (2015), Application(s): Cell Culture, Abstract; Full Text
Strigolactone analogues induce apoptosis through activation of p38 and the stress response pathway in cancer cell lines and in conditionally reprogrammed primary prostate cancer cells: C.B. Pollock, et al.; Oncotarget 5, 1683 (2014), Application(s): Cell Culture, Abstract; Full Text
Dissecting the roles of ROCK isoforms in stress-induced cell detachment : J. Shi, et al. ; Cell Cycle 12, 1492 (2013), Abstract;
Distinct roles for ROCK1 and ROCK2 in the regulation of cell detachment: J. Shi, et al.; Cell Death Dis. 4, e483 (2013), Abstract; Full Text
Conditionally reprogrammed cells represent a stem-like state of adult epithelial cells: F.A. Suprynowicz, et al. ; PNAS 109, 20035 (2012), Abstract;
ROCK Inhibitor and Feeder Cells Induce the Conditional Reprogramming of Epithelial Cells : X. Liu, et al.; Am. J. Pathol. 180, 599,607 (2012), Abstract;
Use of reprogrammed cells to identify therapy for respiratory papillomatosis: H. Yuan, et al. ; N. Engl. J. Med. 367, 1220 (2012), Abstract;
Small molecule inhibition of cytoskeletal dynamics in melanoma tumors results in altered transcriptional expression patterns of key genes involved in tumor initiation and progression: C. Spencer, et al.; Cancer Genom. Proteom. 8, 77 (2011), Abstract;
Effects of rho-kinase inhibition on pulmonary hypertension, lung growth, and structure in neonatal rats chronically exposed to hypoxia: AJ. Ziino, et al.; Pediatr. Res. 67, 177 (2010), Abstract;
The proline-rich region of HIV-1 Nef affects CXCR4-mediated chemotaxis in Jurkat T cells: C.M. Lee, et al.; Viral Immunol. 21, 347 (2008), Abstract;
Molecular characterization of the effects of Y-27632: H. Darenfed, et al.; Cell Motil. Cytoskeleton 64, 97 (2007), Abstract;
A Rho-kinase inhibitor, Y-27632, reduces cholinergic contraction but not neurotransmitter release: L. Fernandes, et al.; Eur. J. Pharmacol. 550, 155 (2006), Abstract;
Rho-kinase inhibitor, Y-27632, has an antinociceptive effect in mice: K. Buyukafsar, et al.; Eur. J. Pharmacol. 541, 49 (2006), Abstract;
Structural basis for induced-fit binding of Rho-kinase to the inhibitor Y-27632: H. Yamaguchi, et al.; J. Biochem. 140, 305 (2006), Abstract;
Preventive effect of Y-27632, a selective Rho-kinase inhibitor, on ischemia/reperfusion-induced acute renal failure in rats: K. Teraishi, et al.; Eur. J. Pharmacol. 505, 205 (2004), Abstract;
Comparison of effects of Y-27632 and Isoproterenol on release of cytokines from human peripheral T cells: M. Aihara, et al.; Int. Immunopharmacol. 3, 1619 (2003), Abstract;
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: K. Sakamoto, et al.; J. Pharmacol. Sci. 92, 56 (2003), Abstract;
Protein kinase A in complex with Rho-kinase inhibitors Y-27632, Fasudil, and H-1152P: structural basis of selectivity: C. Breitenlechner, et al.; Structure 11, 1595 (2003), Abstract;
Y-27632, a Rho-kinase inhibitor, inhibits proliferation and adrenergic contraction of prostatic smooth muscle cells: R.W. Rees, et al.; J. Urol. 170, 2517 (2003), Abstract;
Antagonism of Rho-kinase stimulates rat penile erection via a nitric oxide-independent pathway: K. Chitaley, et al.; Nat. Med. 7, 119 (2001), Abstract;
Inhibition of intrahepatic metastasis of human hepatocellular carcinoma by Rho-associated protein kinase inhibitor Y-27632: M. Takamura, et al.; Hepatology 33, 577 (2001), Abstract;
A p160ROCK-specific inhibitor, Y-27632, attenuates rat hepatic stellate cell growth: H. Iwamoto, et al.; J. Hepatol. 32, 762 (2000), Abstract;
Pharmacological properties of Y-27632, a specific inhibitor of rho-associated kinases: T. Ishizaki, et al.; Mol. Pharmacol. 57, 976 (2000), Abstract;
Specificity and mechanism of action of some commonly used protein kinase inhibitors: S.P. Davies, et al.; Biochem. J. 351, 95 (2000), Abstract; Full Text
The effect of a Rho kinase inhibitor Y-27632 on superoxide production, aggregation and adhesion in human polymorphonuclear leukocytes: A. Kawaguchi, et al.; Eur. J. Pharmacol. 403, 203 (2000), Abstract;
Use and properties of ROCK-specific inhibitor Y-27632: S. Narumiya, et al.; Meth. Enzymol. 325, 273 (2000), Abstract;
Y-27632, an inhibitor of rho-associated protein kinase, suppresses tumor cell invasion via regulation of focal adhesion and focal adhesion kinase: F. Imamura, et al.; Jpn. J. Cancer Res. 91, 811 (2000), Abstract;
Signaling from Rho to the actin cytoskeleton through protein kinases ROCK and LIM-kinase: M. Maekawa, et al.; Science 285, 895 (1999), Abstract;
Molecular dissection of the Rho-associated protein kinase (p160ROCK)-regulated neurite remodeling in neuroblastoma N1E-115 cells: M. Hirose, et al.; J. Cell Biol. 141, 1625 (1998), Abstract;
Calcium sensitization of smooth muscle mediated by a Rho-associated protein kinase in hypertension: M. Uehata, et al.; Nature 389, 990 (1997), Abstract;

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