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688001 InSolution™ Y-27632 - Calbiochem

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Empirical Formula
C₁₄H₂₁N₃O · 2HCl · H₂O

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688001-500UG
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      Ampoule plast. 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
      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
      Référence GTIN
      688001-500UG 07790788052386