Y-27632 dihydrochloride A cell permeable inhibitor of ROCK-1 and ROCK-2

Y-27632 dihydrochloride (CAS 129830-38-2)

Y-27632 dihydrochloride | CAS 129830-38-2 is rated 5.0 out of 5 by 1.
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Synonym: ROCK Inhibitor
Application: A cell permeable inhibitor of ROCK-1 and ROCK-2
CAS Number: 129830-38-2
Purity: ≥98%
Molecular Weight: 320.26
Molecular Formula: C14H21N3O•2HCl
* Refer to Certificate of Analysis for lot specific data (including water content).
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Y-27632 dihydrochloride is a selective Rho-kinase inhibitor, which suppresses cholinergic nerve-mediated contractions. In addition, studies show that Y-27632 dihydrochloride increases the release of neurotransmitters from cholinergic nerves. Studies conducted on smooth muscle preparations suggest that Y-27632 dihydrochloride suppresses nerve-mediated contractile responses stimulated by acetylcholine and noradrenaline. Furthermore, studies on lung tissue damage in rats suggest that Y-27632 dihydrochloride can restore the damage caused by oleic acid by inhibition of ROCK-1 and ROCK-2. Y-27632 dihydrochloride also inhibits protein kinase C related kinase, PRK2.


References

1. Uehata, M., et al., 1997. Calcium sensitization of smooth muscle mediated by a Rho-associated protein kinase in hypertension. Nature. 389(6654): 990-4. PMID: 9353125
2. Itoh, K., et al., 1999. An essential part for Rho-associated kinase in the transcellular invasion of tumor cells. Nature medicine. 5(2): 221-5. PMID: 9930872
3. Davies, S P., et al., 2000. Specificity and mechanism of action of some commonly used protein kinase inhibitors. The Biochemical journal. 351(Pt 1): 95-105. PMID: 10998351
4. Narumiya, S., et al., 2000. Use and properties of ROCK-specific inhibitor Y-27632. Methods in enzymology. 325(): 273-84. PMID: 11036610
5. Köksel, Oğuz., et al., 2005. Rho-kinase (ROCK-1 and ROCK-2) upregulation in oleic acid-induced lung injury and its restoration by Y-27632. European journal of pharmacology. 510(1-2): 135-42. PMID: 15740734
6. Fernandes, Lynette., et al., 2006. A Rho-kinase inhibitor, Y-27632, reduces cholinergic contraction but not neurotransmitter release. European journal of pharmacology. 550(1-3): 155-61. PMID: 17010334

Physical State :
Solid
Solubility :
Soluble in water (14 mg/mL), ethanol (~5 mg/mL), DMSO (~20 mg/mL), DMF (~30 mg/mL), PBS, pH 7.2 (~10 mg/mL), and methanol (25 mg/mL).
Storage :
Store at -20° C
Refractive Index :
n20D 1.58
Optical Activity :
α20/D +7°, c = 0.4 in methanol
IC50 :
ROCK-II: IC50 = 800 nM; PRK2: IC50 = 600 nM; Smooth-muscle contraction induces by various agonists including phenylephrine, histamine, acetylcholine, serotonin, endothelin, and thromboxane : IC50 = 0.3-1 µM
Ki Data :
p160ROCK: Ki= 140 nM; cAMP-dependent protein kinase: Ki= 25 µM; PKC: Ki= 26 µM; Myosin light-chain kinase: Ki= >250 µM; ROCKI: Ki= 0.22 µM; ROCKII: Ki= 0.3 µM; PKCα: Ki= 73 µM
pK Values :
pKa: 13.53 (Predicted), pKb: 10.74 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
9901617
MDL Number :
MFCD03490488
SMILES :
C[C@H](C1CCC(CC1)C(=O)NC2=CC=NC=C2)N.Cl.Cl

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Certificate of Analysis

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Y-27632 dihydrochloride  Product Citations

See how others have used Y-27632 dihydrochloride. Click on the entry to view the PubMed entry .

Citations 1 to 10 of 10 total

PMID: # 28104444  Ghasemi, A. et al. 2017. Cell. Signal. 32: 104-114.

PMID: # 27596957  2016. Stem Cell Res. 17: 296-305.

PMID: # 26391686  Al-Shboul, O. et al. 2016. J Physiol Sci. 66: 85-92.

PMID: # 26225425  Namachivayam, K. et al. 2015. PloS one. 10: e0134003.

PMID: # 26168083  Tivari, S. et al. 2015. J Vis Exp. e52672.

PMID: # 25752964  Al-Shboul, O. et al. 2015. Can. J. Physiol. Pharmacol. 93: 405-11.

PMID: # 25956403  Cernecka, H. et al. 2015. Naunyn Schmiedebergs Arch. Pharmacol. 388: 749-59.

PMID: # 23785737  2013. SourceStemBook.

PMID: # 23450810  Fedr, R. et al. 2013. Cytometry A. 83: 472-82.

Citations 1 to 10 of 10 total

What is the storage temperature for solution of Y-27632 dihydrochloride?

Asked by: two2igm05
It is recommended to store aliquots of sc-281642 in solution for up to 6 months at -20º C. Before usage, the aliquots should be thawed at room temperature for an hour.
Answered by: Chemical Support 4
Date published: 2017-02-25
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Rated 5 out of 5 by from Pigati Pigati, PA. et al. (PubMed 26264367) evaluated the effects of Y-27632 dihydrochloride, a selective Rho-kinase inhibitor, with or without concurrent dexamethasone treatment, on airway and lung tissue mechanical responses, inflammation, extracellular matrix remodeling, and oxidative stress in guinea pigs with chronic allergic inflammation. This therapeutic strategy reduced the levels of collagen and IFN- in the airway walls, as well as IL-2, IFN- , 8-iso-PGF2 and NF- B in the distal parenchyma, when compared to isolated treatment with corticosteroid or Rho-kinase inhibitor (P < 0.05) and reduced the number of TIMP-1-positive cells and eosinophils in the alveolar septa compared to corticosteroid-treated animals (P < 0.05). -SCBT Publication Review
Date published: 2015-06-10
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