688001

Y-27632

≥95% (HPLC), liquid, Rho kinase inhibitor, Calbiochem^®

• 別名: InSolution Y-27632, Rho Kinase Inhibitor VI
• 実験式（ヒル表記法）: C₁₄H₂₁N₃O · 2HCl · xH₂O
• 分子量: 320.26 (anhydrous basis)
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• 製品名: Y-27632, InSolution, ≥95%, reversible, inhibitor of Rho kinases
• 品質水準: 100
• アッセイ: ≥95% (HPLC)
• フォーム: liquid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 輸送温度: wet ice
• 保管温度: −20°C

詳細

詳細

A 5 mM (500 µg/296 µl) aqueous solution of Y-27632 (Cat. No. 688000). A highly potent, cell-permeable, selective inhibitor of Rho-associated protein kinase (K_i = 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 mM). 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).

A highly potent, cell-permeable, selective inhibitor of Rho-associated protein kinase (K_i = 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 mM). 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).

生物化学的／生理学的作用

Cell permeable: yes

Primary Target
p160ROCK

Product competes with ATP.

Reversible: no

Target IC₅₀: 700 nM against phenylephrine-induced contractions in aortic strips

Target K_i: 140 nM for p160ROCK (ROCK-I)

包装

Packaged under inert gas

警告

Toxicity: Harmful (C)

物理的形状

A 5 mM (500 µg/296 µl) solution of Y-27632 (Cat. No. 688000) in H₂O.

再構成

Following initial thaw, aliquot and freeze (-20°C).

その他情報

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. 1999. 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: 12 - Non Combustible Liquids
• WGK: WGK 2
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable