688001

Y-27632

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

• Sinônimo(s): InSolution Y-27632, Rho Kinase Inhibitor VI
• Fórmula empírica (Notação de Hill): C₁₄H₂₁N₃O · 2HCl · xH₂O
• Peso molecular: 320.26 (anhydrous basis)
• Código UNSPSC: 12352200
• NACRES: NA.77

Propriedades

• Nome do produto: Y-27632, InSolution, ≥95%, reversible, inhibitor of Rho kinases
• Nível de qualidade: 100
• Ensaio: ≥95% (HPLC)
• Formulário: liquid
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• Condições de expedição: wet ice
• temperatura de armazenamento: −20°C

Descrição

Descrição geral

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).

Ações bioquímicas/fisiológicas

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)

Embalagem

Packaged under inert gas

Advertência

Toxicity: Harmful (C)

forma física

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

Reconstituição

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

Outras notas

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.

Informações legais

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

Informações de segurança

• Código de classe de armazenamento: 12 - Non Combustible Liquids
• Classe de risco de água (WGK): WGK 2
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable