688000 Y-27632 - CAS 146986-50-7 - Calbiochem

688000
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₄H₂₁N₃O · 2HCl · H₂O 146986-50-7

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      688000-100MG
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          Plastic ampoule 100 mg
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          688000-10MG
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              Glass bottle 10 mg
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              688000-1MG
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                  688000-5MG
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                      Description
                      OverviewA highly potent, cell-permeable, reversible, and selective inhibitor of Rho-associated protein kinases (Ki = 140 nM for p160ROCK). Also inhibits ROCK-II with equal potency. The inhibition is competitive with respect to ATP. Exhibits 10- to 50-fold lower affinity for PKCε than p160ROCK. Does not affect the activity of p21-activated protein kinase (PAK) even at higher concentrations (~100 µM). Also acts as a potent inhibitor of agonist-induced Ca2+ sensitization of myosin phosphorylation and smooth muscle contraction. Prevents apoptosis and enhances the survival and cloning efficiency of dissociated hES cells without affecting their pluripotency. Pretreatment with Y-27632 reduces the risk of lung injury in rat models of sepsis. A 5 mM (500 µg/296 µl) solution of Y-27632 (Cat. No. 688001) in H2O and a 10 mM solution in DMSO (Cat. No. 688002) are also available.
                      Catalogue Number688000
                      Brand Family Calbiochem®
                      SynonymsROCK Inhibitor, (R)-(+)-trans-N-(4-Pyridyl)-4-(1-aminoethyl)-cyclohexanecarboxamide, 2HCl, Rho Kinase Inhibitor VI
                      References
                      ReferencesCinel, I., et al. 2012. J. Thorac . Dis. 4, 30.
                      Watanabe, K., et al. 2007. Nature Biotech. 25, 681.
                      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. 1998. J. Cell Biol. 141, 1625.
                      Maekawa, M., et al. 1999. Science 285, 895.
                      Uehata, M., et al. 1997. Nature 389, 990.
                      Product Information
                      CAS number146986-50-7
                      ATP CompetitiveY
                      DeclarationSold under license of PCT Application W098/06,433A1 and under license from Mitsubishi Pharma Tanabe Corporation.
                      FormWhite solid
                      Hill FormulaC₁₄H₂₁N₃O · 2HCl · H₂O
                      Chemical formulaC₁₄H₂₁N₃O · 2HCl · H₂O
                      Hygroscopic Hygroscopic
                      ReversibleY
                      Structure formula ImageStructure formula Image
                      Applications
                      ApplicationY-27632, CAS 146986-50-7, is a cell-permeable, reversible, inhibitor of Rho kinases (Ki = 140 nM for p160ROCK). Enhances survival & cloning efficiency of ESC without affecting their pluripotency.
                      Biological Information
                      Primary Targetp160 Rho-associated protein kinases (ROCK)
                      Primary Target K<sub>i</sub>140 nM for p160 Rho-associated protein kinases (ROCK)
                      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 Ambient Temperature Only
                      Toxicity Harmful
                      Storage -20°C
                      Protect from Light Protect from light
                      Hygroscopic Hygroscopic
                      Do not freeze Ok to freeze
                      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for 6 months at -20°C.
                      Packaging Information
                      Packaged under inert gas Packaged under inert gas
                      Transport Information
                      Supplemental Information
                      Specifications

                      Documentation

                      Y-27632 - CAS 146986-50-7 - Calbiochem SDS

                      Title

                      Safety Data Sheet (SDS) 

                      Y-27632 - CAS 146986-50-7 - Calbiochem Certificates of Analysis

                      TitleLot Number
                      688000

                      References

                      Reference overview
                      Cinel, I., et al. 2012. J. Thorac . Dis. 4, 30.
                      Watanabe, K., et al. 2007. Nature Biotech. 25, 681.
                      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. 1998. J. Cell Biol. 141, 1625.
                      Maekawa, M., et al. 1999. Science 285, 895.
                      Uehata, M., et al. 1997. Nature 389, 990.

                      Brochure

                      Title
                      Biologics 33.2

                      Citations

                      Title
                    • Cinel, I., et al. 2012. J. Thorac . Dis. 4, 30.
                    • Jennifer L. Farmer, et al. (2008) Galectin 15 (LGALS15) functions in trophectoderm migration and attachment. Federation of American Societies for Experimental Biology Journal 22, 548-560.
                    • 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.

                      Revision27-February-2012 RFH
                      SynonymsROCK Inhibitor, (R)-(+)-trans-N-(4-Pyridyl)-4-(1-aminoethyl)-cyclohexanecarboxamide, 2HCl, Rho Kinase Inhibitor VI
                      DescriptionA highly potent, cell-permeable, reversible, and 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 µM). 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). Prevents apoptosis and enhances the survival and cloning efficiency of dissociated hES cells without affecting their pluripotency. Pretreatment with Y-27632 reduces the risk of lung injury in rat models of sepsis.
                      FormWhite solid
                      Intert gas (Yes/No) Packaged under inert gas
                      CAS number146986-50-7
                      Chemical formulaC₁₄H₂₁N₃O · 2HCl · H₂O
                      Structure formulaStructure formula
                      Purity≥95% by HPLC
                      SolubilityH₂O (100 mg/ml)
                      Storage -20°C
                      Hygroscopic
                      Protect from light
                      Do Not Freeze Ok to freeze
                      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for 6 months at -20°C.
                      Toxicity Harmful
                      ReferencesCinel, I., et al. 2012. J. Thorac . Dis. 4, 30.
                      Watanabe, K., et al. 2007. Nature Biotech. 25, 681.
                      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. 1998. J. Cell Biol. 141, 1625.
                      Maekawa, M., et al. 1999. Science 285, 895.
                      Uehata, M., et al. 1997. Nature 389, 990.
                      Citation
                    • Cinel, I., et al. 2012. J. Thorac . Dis. 4, 30.
                    • Jennifer L. Farmer, et al. (2008) Galectin 15 (LGALS15) functions in trophectoderm migration and attachment. Federation of American Societies for Experimental Biology Journal 22, 548-560.
                    • 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.