688001 InSolution™ Y-27632 - Calbiochem

688001
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₄H₂₁N₃O · 2HCl · H₂O

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      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
          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.