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688001 InSolution™ Y-27632 - Calbiochem

Overview

Replacement Information

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
Applications
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
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
R PhraseR: 20/21/22

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

Wear suitable protective clothing.
Product Usage Statements
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
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
688001-500UG 07790788052386

Documentation

InSolution™ Y-27632 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

InSolution™ Y-27632 - Calbiochem Certificates of Analysis

TitleLot Number
688001

References

Reference overview
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. Science 285, 895.
Uehata, M., et al. 1997. Nature 389, 990.

Citations

Title
  • James J. Fiordalisi, Patricia J. Keller and Adrienne D. Cox. (2006) PRL Tyrosine Phosphatases Regulate Rho Family GTPases to Promote Invasion and Motility. Cancer Research 66, 3153-3161.
  • Karen E. Porter, et al. (2004) Simvastatin reduces human atrial myofibroblast proliferation independently of cholesterol lowering via inhibition of RhoA. Cardiovascular Research 61, 745-755.
  • Rick B. Vega, et al. (2004) Protein Kinases C and D Mediate Agonist-Dependent Cardiac Hypertrophy through Nuclear Export of Histone Deacetylase 5. Molecular and Cellular Biology 24, 8374-8385.
  • Data Sheet

    Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

    Revision16-September-2008 RFH
    SynonymsRho Kinase Inhibitor VI
    DescriptionA 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).
    FormLiquid
    FormulationA 5 mM (500 µg/296 µl) solution of Y-27632 (Cat. No. 688000) in H₂O.
    Intert gas (Yes/No) Packaged under inert gas
    Chemical formulaC₁₄H₂₁N₃O · 2HCl · H₂O
    Structure formulaStructure formula
    Purity≥95% by HPLC
    Storage Protect from light
    -20°C
    Do Not Freeze Ok to freeze
    Special InstructionsFollowing initial thaw, aliquot and freeze (-20°C).
    Toxicity Harmful
    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.
    Citation
  • James J. Fiordalisi, Patricia J. Keller and Adrienne D. Cox. (2006) PRL Tyrosine Phosphatases Regulate Rho Family GTPases to Promote Invasion and Motility. Cancer Research 66, 3153-3161.
  • Karen E. Porter, et al. (2004) Simvastatin reduces human atrial myofibroblast proliferation independently of cholesterol lowering via inhibition of RhoA. Cardiovascular Research 61, 745-755.
  • Rick B. Vega, et al. (2004) Protein Kinases C and D Mediate Agonist-Dependent Cardiac Hypertrophy through Nuclear Export of Histone Deacetylase 5. Molecular and Cellular Biology 24, 8374-8385.