688001
Y-27632
≥95% (HPLC), liquid, Rho kinase inhibitor, Calbiochem®
Synonyme(s) :
InSolution Y-27632, Rho Kinase Inhibitor VI
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A propos de cet article
Formule empirique (notation de Hill) :
C14H21N3O · 2HCl · xH2O
Poids moléculaire :
320.26 (anhydrous basis)
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥95% (HPLC)
Form:
liquid
Storage condition:
OK to freeze, protect from light
Service technique
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Laissez-nous vous aiderNom du produit
Y-27632, InSolution
Quality Segment
assay
≥95% (HPLC)
form
liquid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
shipped in
wet ice
storage temp.
−20°C
General description
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).
Biochem/physiol Actions
Cell permeable: yes
Primary Target
p160ROCK
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)
Packaging
Packaged under inert gas
Physical form
A 5 mM (500 µg/296 µl) solution of Y-27632 (Cat. No. 688000) in H₂O.
Preparation Note
Following initial thaw, aliquot and freeze (-20°C).
Other Notes
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.
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.
Legal Information
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
Disclaimer
Toxicity: Harmful (C)
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