688001 InSolution™ Y-27632 - Calbiochem

Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₄H₂₁N₃O · 2HCl · H₂O

Pricing & Availability

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688001-500UG
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      Plastic ampoule 500 μg
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      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

      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.

      Brochure

      Title
      In Solution!" Product Flyer

      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 -20°C
      Protect from light
      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.