Y-27632 dihydrochloride CAS: 129830-38-2
MF: C14H21N3O•2HCl
MW: 320.26

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

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Noms alternatifs: Y-27632 dihydrochloride is also known as ROCK Inhibitor
Application: Y-27632 dihydrochloride is a cell permeable inhibitor of ROCK-1 and ROCK-2 which plays an important role in Rho-mediated cell adhesion and smooth muscle contraction.
Numéro CAS: 129830-38-2
Pureté: ≥98%
Masse Moléculaire: 320.26
Formule Moléculaire: C14H21N3O•2HCl
Pour la Recherche Uniquement. Non conforme pour le Diagnostic ou pour une Utilisation Thérapeutique.
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Y-27632 dihydrochloride is a selective Rho-kinase inhibitor. Y-27632 dihydrochloride 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.


Références

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


État Physique :
Solid
Solubilité :
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).
STOCKAGE :
Store at -20° C
Indice de Réfraction :
n20D 1.58
Activité Optique :
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
Valeurs pK :
pKa: 13.53 (Predicted), pKb: 10.74 (Predicted)
Pour la Recherche Uniquement. Non conforme pour le Diagnostic ou pour une Utilisation Thérapeutique.
WGK Allemagne :
3
PubChem CID :
Numéro MDL :
MFCD03490488
SMILES :
C[[email protected]](C1CCC(CC1)C(=O)NC2=CC=NC=C2)N.Cl.Cl

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

Consultez les publications faisant référence à l' utilisation de Y-27632 dihydrochloride (CAS 129830-38-2). Cliquez sur le lien pour afficher lentrée PubMed .

Citations 1 à 10 sur un total de 35

PMID: # 33529599  Shah, PP.|Lv, W.|Rhoades, JH.|Poleshko, A.|Abbey, D.|Caporizzo, MA.|Linares-Saldana, R.|Heffler, JG.|Sayed, N.|Thomas, D.|Wang, Q.|Stanton, LJ.|Bedi, K.|Morley, MP.|Cappola, TP.|Owens, AT.|Margulies, KB.|Frank, DB.|Wu, JC.|Rader, DJ.|Yang, W.|Prosser, BL.|Musunuru, K.|Jain, R.| et al. 2021. Cell Stem Cell. 28: 938-954.e9.

PMID: # 33898197  Wang, H.|Gong, P.|Chen, T.|Gao, S.|Wu, Z.|Wang, X.|Li, J.|Marjani, SL.|Costa, J.|Weissman, SM.|Qi, F.|Pan, X.|Liu, L.| et al. 2021. Adv Sci (Weinh). 8: 2004320.

PMID: # 33794364  Vaidyanathan, S.|Baik, R.|Chen, L.|Bravo, DT.|Suarez, CJ.|Abazari, SM.|Salahudeen, AA.|Dudek, AM.|Teran, CA.|Davis, TH.|Lee, CM.|Bao, G.|Randell, SH.|Artandi, SE.|Wine, JJ.|Kuo, CJ.|Desai, TJ.|Nayak, JV.|Sellers, ZM.|Porteus, MH.| et al. 2021. Mol Ther.

PMID: # 32845994  Das, D.|Li, J.|Cheng, L.|Franco, S.|Mahairaki, V.| et al. 2020. Radiat Res. 194: 191-198.

PMID: # 31978363  Kathiriya, JJ.|Brumwell, AN.|Jackson, JR.|Tang, X.|Chapman, HA.| et al. 2020. Cell Stem Cell. 26: 346-358.e4.

PMID: # 32619513  Toyohara, T.|Roudnicky, F.|Florido, MHC.|Nakano, T.|Yu, H.|Katsuki, S.|Lee, M.|Meissner, T.|Friesen, M.|Davidow, LS.|Ptaszek, L.|Abe, T.|Rubin, LL.|Pereira, AC.|Aikawa, M.|Cowan, CA.| et al. 2020. Cell Stem Cell. 27: 178-180.

PMID: # 33373890  Siehler, J.|Blöchinger, AK.|Akgün, M.|Wang, X.|Shahryari, A.|Geerlof, A.|Lickert, H.|Burtscher, I.| et al. 2020. Stem Cell Res. 50: 102126.

PMID: # 30776675  Kahounová, Z.|Slabáková, E.|Binó, L.|Remšík, J.|Fedr, R.|Bouchal, J.|Vrtěl, R.|Jurečková, L.|Porokh, V.|Páralová, D.|Hampl, A.|Souček, K.| et al. 2019. Stem Cell Res. 35: 101405.

PMID: # 30481741  Kahounová, Z.|Slabáková, E.|Binó, L.|Remšík, J.|Fedr, R.|Bouchal, J.|Kurfűrstová, D.|Vrtěl, R.|Študent, V.|Jurečková, L.|Porokh, V.|Hampl, A.|Souček, K.| et al. 2018. Stem Cell Res. 33: 255-259.

PMID: # 29462126  Remšík, J.|Fedr, R.|Navrátil, J.|Binó, L.|Slabáková, E.|Fabian, P.|Svoboda, M.|Souček, K.| et al. 2018. Br J Cancer. 118: 813-819.

Citations 1 à 10 sur un total de 35
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