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

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

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Sinónimo: ROCK Inhibitor
Solicitud: A cell permeable inhibitor of ROCK-1 and ROCK-2
Número de CAS: 129830-38-2
Pureza: ≥98%
Peso Molecular: 320.26
Fórmula Molecular: C14H21N3O•2HCl
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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


Estado de Materia :
Solid
Solubilidad :
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).
ALMACENAMIENTO :
Store at -20° C
Indice de Refracción :
n20D 1.58
Actividad Óptica :
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
Datos Ki :
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
Valores de pK :
pKa: 13.53 (Predicted), pKb: 10.74 (Predicted)
Para Uso Exclusivo en Investigación. No está diseñado para uso en diagnosis o terapia.
WGK Alemania :
3
PubChem CID :
9901617
Número MDL :
MFCD03490488
SMILES :
C[C@H](C1CCC(CC1)C(=O)NC2=CC=NC=C2)N.Cl.Cl

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Y-27632 dihydrochloride  Menciones del Producto

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Citaciones 1 a 10 de un total de 10

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.

Citaciones 1 a 10 de un total de 10
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