688000

Y-27632

≥95% (HPLC), solid, Rho kinase inhibitor, Calbiochem

• 別名: Y-27632, (R)-(+)-trans-N-(4-Pyridyl)-4-(1-aminoethyl)-cyclohexanecarboxamide, 2HCl, ROCK Inhibitor, Rho Kinase Inhibitor VI, ROCK Inhibitor, (R)-(+)-trans-N-(4-Pyridyl)-4-(1-aminoethyl)-cyclohexanecarboxamide, 2HCl, Rho Kinase Inhibitor VI
• 実験式（ヒル表記法）: C₁₄H₂₁N₃O · 2HCl · xH₂O
• CAS番号: 331752-47-7
• 分子量: 320.26 (anhydrous basis)
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• product name: Y-27632-CAS 331752-47-7-Calbiochem, Y-27632A, CAS 331752-47-7, is a cell-permeable, reversible, inhibitor of Rho kinases (K_i = 140 nM for p160ROCK). Enhances survival & cloning efficiency of ESC without affecting their pluripotency.
• 品質水準: 100
• アッセイ: ≥95% (HPLC)
• 形状: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; desiccated (hygroscopic); protect from light
• 色: white
• 溶解性: water: 100 mg/mL
• 輸送温度: ambient
• 保管温度: −20°C
• InChI: 1S/C14H21N3O/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)/t10-,11?,12?/m1/s1
• InChI Key: IYOZTVGMEWJPKR-VOMCLLRMSA-N

詳細

詳細

A highly potent, cell-permeable, reversible, and selective inhibitor of Rho-associated protein kinase (Ki = 140 nM for p160^ROCK (ROCK-I). Also inhibits ROCK-II with almost equal potency. Inhibition is achieved by competing with ATP for binding to the catalytic site. Exhibits 10- to 50-fold lower affinity for PKC_ε than p160^ROCK. Does not affect the activity of p21-activated protein kinase (PAK) even at high concentrations (~100 µM). Also acts as a potent inhibitor of agonist-induced Ca²⁺ sensitization of myosin phosphorylation and smooth muscle contractions (IC₅₀ = 700 nM for phenylephrine-induced contractions in aortic strips). Prevents apoptosis and enhances the survival and cloning efficiency of dissociated hES cells without affecting their pluripotency. Pretreatment with Y-27632 reduces the risk of lung injury in rat models of sepsis.

A highly potent, cell-permeable, reversible, and selective inhibitor of Rho-associated protein kinases (K_i = 140 nM for p160^ROCK). Also inhibits ROCK-II with equal potency. The inhibition is competitive with respect to ATP. Exhibits 10- to 50-fold lower affinity for PKC_ε than p160^ROCK. Does not affect the activity of p21-activated protein kinase (PAK) even at higher concentrations (~100 µM). Also acts as a potent inhibitor of agonist-induced Ca²⁺ sensitization of myosin phosphorylation and smooth muscle contraction. Prevents apoptosis and enhances the survival and cloning efficiency of dissociated hES cells without affecting their pluripotency. Pretreatment with Y-27632 reduces the risk of lung injury in rat models of sepsis. A 5 mM (500 µg/296 µl) solution of Y-27632 (Cat. No. 688001) in H₂O and a 10 mM solution in DMSO (Cat. No. 688002) are also available.

生物化学的／生理学的作用

Cell permeable: yes

Primary Target
p160 Rho-associated protein kinases (ROCK)

Product competes with ATP.

Reversible: yes

Target K_i: 140 nM for p160 Rho-associated protein kinases (ROCK)

包装

Packaged under inert gas

警告

Toxicity: Harmful (C)

再構成

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for 6 months at -20°C.

その他情報

Cinel, I., et al. 2012. J. Thorac . Dis.4, 30.
Watanabe, K., et al. 2007. Nature Biotech.25, 681.
Chitaley, K., et al. 2001. Nat. Med.7, 119.
Davies, S.P., et al. 2000. Biochem. J. 351, 95.
Narumiya, S., et al. 2000. Methods Enzymol.325, 273.
Hirose, M., et al. 1998. J. Cell Biol.141, 1625.
Maekawa, M., et al. 1999. Science285, 895.
Uehata, M., et al. 1997. Nature389, 990.

法的情報

Sold under license of PCT Application W098/06,433A1 and under license from Mitsubishi Pharma Tanabe Corporation.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable