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688001

Sigma-Aldrich

Y-27632

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

Synonyme(s) :

InSolution Y-27632, Rho Kinase Inhibitor VI

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About This Item

Formule empirique (notation de Hill):
C14H21N3O · 2HCl · xH2O
Poids moléculaire :
320.26 (anhydrous basis)
Code UNSPSC :
12352200
Nomenclature NACRES :
NA.77

product name

Y-27632, InSolution, ≥95%, reversible, inhibitor of Rho kinases

Niveau de qualité

Pureté

≥95% (HPLC)

Forme

liquid

Fabricant/nom de marque

Calbiochem®

Conditions de stockage

OK to freeze
protect from light

Conditions d'expédition

wet ice

Température de stockage

−20°C

Description générale

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 (Ki = 140 nM for p160ROCK (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 PKCε than p160ROCK. 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 (Ki = 140 nM for p160ROCK (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 PKCε than p160ROCK. 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).

Actions biochimiques/physiologiques

Cell permeable: yes
Primary Target
p160ROCK
Product competes with ATP.
Reversible: no
Target IC50: 700 nM against phenylephrine-induced contractions in aortic strips
Target Ki: 140 nM for p160ROCK (ROCK-I)

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Harmful (C)

Forme physique

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

Reconstitution

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

Autres remarques

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.

Informations légales

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

Code de la classe de stockage

12 - Non Combustible Liquids

Classe de danger pour l'eau (WGK)

WGK 2

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable


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