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688001 InSolution™ Y-27632 - Calbiochem

688001
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Overview

Key Spec Table

Empirical Formula
C₁₄H₂₁N₃O · 2HCl · H₂O

Products

Catalogue NumberPackaging Qty/Pack
688001-500UG Plastic ampoule 500 μg
Description
OverviewA 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).
Catalogue Number688001
Brand Family Calbiochem®
SynonymsRho Kinase Inhibitor VI
References
ReferencesChitaley, 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. Science 285, 895.
Uehata, M., et al. 1997. Nature 389, 990.
Product Information
ATP CompetitiveY
DeclarationSold under license of PCT Application W098/06,433A1 and under license from Mitsubishi Pharma Tanabe Corporation.
FormLiquid
FormulationA 5 mM (500 µg/296 µl) solution of Y-27632 (Cat. No. 688000) in H₂O.
Hill FormulaC₁₄H₂₁N₃O · 2HCl · H₂O
Chemical formulaC₁₄H₂₁N₃O · 2HCl · H₂O
ReversibleN
Structure formula ImageStructure formula Image
Quality LevelMQ100
Biological Information
Primary Targetp160ROCK
Primary Target IC<sub>50</sub>700 nM against phenylephrine-induced contractions in aortic strips
Primary Target K<sub>i</sub>140 nM for p160ROCK (ROCK-I)
Purity≥95% by HPLC
Physicochemical Information
Cell permeableY
Safety Information
R PhraseR: 20/21/22

Harmful by inhalation, in contact with skin and if swallowed.
S PhraseS: 36

Wear suitable protective clothing.
Storage and Shipping Information
Ship Code Blue Ice Only
Toxicity Harmful
Storage -20°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing initial thaw, aliquot and freeze (-20°C).
Packaging Information
Packaged under inert gas Packaged under inert gas
Global Trade Item Number
Catalogue Number GTIN
688001-500UG 07790788052386