Y0503

Y-27632 dihydrochloride

≥98% (HPLC)

• Synonym(s): Rock inhibitor y-27632, Y-27632 2HCl, (R)-(+)-trans-4-(1-Aminoethyl)-N-(4-Pyridyl)cyclohexanecarboxamide dihydrochloride
• Empirical Formula (Hill Notation): C₁₄H₂₁N₃O · 2HCl
• CAS Number: 129830-38-2
• Molecular Weight: 320.26
• MDL number: MFCD03490488
• UNSPSC Code: 12352200
• PubChem Substance ID: 24277699
• NACRES: NA.77

Properties

• biological source: synthetic (organic)
• Quality Level: 100
• Assay: ≥98% (HPLC)
• form: powder
• optical activity: [α]/D +3.0 to +5.0°, c = 1.0 in methanol
• color: white to beige
• solubility: H₂O: 14 mg/mL
• storage temp.: 2-8°C
• SMILES string: Cl.Cl.C[C@@H](N)[C@H]1CC[C@@H](CC1)C(=O)Nc2ccncc2
• 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
• InChI key: IDDDVXIUIXWAGJ-LJDSMOQUSA-N
• Gene Information: human ... ROCK1(6093) , ROCK2(9475)

Description

General description

Y-27632 dihydrochloride is an effective bronchodilator and improves lung resistance (RL) induced by antigen and acetylcholine.[1] Y-27632 controls neutrophil migration and lung edema and may be a potential agent against acute lung injury.[2]The utilization of Y-27632 dihydrochloride, in conjunction with Accutase or other enzyme solutions, during the passaging of human embryonic stem (hES) cells has been demonstrated to enhance cell survival and significantly improve cloning efficiency[3]

Y-27632, a Rho-kinase inhibitor, counteracts noradrenergic contractions in the penile corpus cavernosum of rabbits and humans. It helps to relax vascular and non-vascular smooth muscle in various preparations and lower blood pressure in hypertensive rats.[4] Additionally, this inhibitor induces reversible changes in cell shape and decreases in actin stress fibers, focal adhesions, and protein phosphotyrosine staining in human trabecular meshwork (TM) cells and Schlemm′s canal cells.[5] Y-27632 inhibits the kinase activity of both ROCK-I and ROCK-II in vitro, and this inhibition is competitively reversed by ATP, indicating that these compounds bind to the catalytic site to inhibit the kinases.[6] Ki = 140 nM for p160ROCK.

Application

Y-27632 dihydrochloride has been used:

• as a medium supplement in pancreatic ductal adenocarcinoma organoid culture[7]
• in the inhibition of Ras homolog gene family (Rho) kinase in mouse embryonic stem cells[8]
• in the inhibition of Rho-associated protein kinase (ROCK) in human embryonic stem cells[9] and human induced pluripotent stem cells (iPSCs)[10]
• Y-27632 dihydrochloride has been used as a supplement in the E8 medium to promote in vitro differentiation of human pluripotent stem cells[11]

Biochem/physiol Actions

Y-27632 is highly potent, cell-permeable, selective ROCK (Rho-associated coiled coil forming protein serine/threonine kinase) inhibitor. K_i = 140 nM for p160^ROCK. Y-27632 also inhibits ROCK-II with equal potency. The inhibition is competitive with respect to ATP.

Features and Benefits

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Legal Information

Sold under license from Mitsubishi Pharma Corporation

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable
• Personal Protective Equipment: dust mask type N95 (US), Eyeshields, Gloves