371963 | H-89, Dihydrochloride - CAS 127243-85-0 - Calbiochem

371963
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₀H₂₀BrN₃O₂S · 2HCl 127243-85-0

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      371963-1MG
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          Plastic ampoule 1 mg
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          Description
          OverviewA cell-permeable, selective, reversible, ATP-competitive and potent inhibitor of protein kinase A (Ki = 48 nM). Inhibits other kinases only at much higher concentrations: CaM kinase II (Ki = 29.7 µM), casein kinase I (Ki = 38.3 µM), myosin light chain kinase (Ki = 28.3 µM), protein kinase C (Ki = 31.7 µM), and ROCK-II (IC50 = 270 nM). May be used to discriminate between the effects of PKA and cAMP-regulated guanine-nucleotide-exchange factors (GEFs) such as GEFI, GEFII, or Epac (exchange protein directly activated by cAMP). Enhances radiation-induced apoptosis in the human cell line BM 13674. A 10 mM (1 mg/193 µl) solution of H-89, 2HCl (Cat. No. 371962) in DMSO is also available.
          Catalogue Number371963
          Brand Family Calbiochem®
          SynonymsN-[2-((p-Bromocinnamyl)amino)ethyl]-5-isoquinolinesulfonamide, 2HCl, PKA Inhibitor III
          References
          ReferencesLeemhuis, J., et al. 2002. J. Pharmacol. Exp. Ther. 300, 1000.
          Davies, S.P., et al. 2000. Biochem. J. 351, 95.
          Kawasaki, H., et al. 1998. Science 282, 2275.
          de Rooij, J., et al. 1998. Nature 396, 474.
          Findik, D., et al. 1995. J. Cell. Biochem. 57, 12.
          Geilen, C.C. 1992. FEBS Lett. 309, 381.
          Chijiwa, T., et al. 1990. J. Biol. Chem. 265, 5267.
          Combest, W.L., et al. 1988. J. Neurochem. 51, 1581.
          Product Information
          CAS number127243-85-0
          ATP CompetitiveY
          FormClear to off-white crystalline film
          Hill FormulaC₂₀H₂₀BrN₃O₂S · 2HCl
          Chemical formulaC₂₀H₂₀BrN₃O₂S · 2HCl
          ReversibleY
          Structure formula ImageStructure formula Image
          Applications
          ApplicationH-89, Dihydrochloride, CAS 127243-85-0, is a cell-permeable, potent, selective, reversible, ATP-competitive inhibitor of protein kinase A (Ki = 48 nM).
          Biological Information
          Primary TargetPKA
          Primary Target K<sub>i</sub>48 nM for protein kinase A
          Purity≥99% by HPLC
          Physicochemical Information
          Cell permeableY
          Dimensions
          Materials Information
          Toxicological Information
          Safety Information according to GHS
          Safety Information
          Product Usage Statements
          Storage and Shipping Information
          Ship Code Ambient Temperature Only
          Toxicity Standard Handling
          Storage +2°C to +8°C
          Do not freeze Ok to freeze
          Special InstructionsFollowing reconstitution, store in the refrigerator (4°C). Stock solutions are stable for at up to 4 months at 4°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          Certificates of Analysis

          TitleLot Number
          371963

          References

          Reference overview
          Leemhuis, J., et al. 2002. J. Pharmacol. Exp. Ther. 300, 1000.
          Davies, S.P., et al. 2000. Biochem. J. 351, 95.
          Kawasaki, H., et al. 1998. Science 282, 2275.
          de Rooij, J., et al. 1998. Nature 396, 474.
          Findik, D., et al. 1995. J. Cell. Biochem. 57, 12.
          Geilen, C.C. 1992. FEBS Lett. 309, 381.
          Chijiwa, T., et al. 1990. J. Biol. Chem. 265, 5267.
          Combest, W.L., et al. 1988. J. Neurochem. 51, 1581.

          Brochure

          Title
          Calmodulin and Related Products Technical Bulletin
          Nitric Oxide and Oxidative Stress Brochure

          Citations

          Title
        • Ying Zhang, Mingjuan Liao and Maria L. Dufau. (2006) Phosphatidylinositol 3-kinase/protein kinase Cγ-induced phosphorylation of Sp1 and p107 repressor release have a critical role in histone deacetylase inhibitor-mediated depression of transcription of the luteinizing hormone receptor gene. Molecular and Cellular Biology 26, 6748-6761.
        • 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.

          Revision08-April-2011 JSW
          SynonymsN-[2-((p-Bromocinnamyl)amino)ethyl]-5-isoquinolinesulfonamide, 2HCl, PKA Inhibitor III
          DescriptionA cell-permeable, selective, reversible, ATP-competitive and potent inhibitor of protein kinase A (Ki = 48 nM). Inhibits other kinases at several fold higher concentrations: myosin light chain kinase (Ki = 28.3 µM), Ca2+/calmodulin-dependent protein kinase II (Ki = 29.7 µM), protein kinase C (Ki = 31.7 µM), casein kinase I (Ki = 38.3 µM), and Rho Kinase II (IC50 = 270 nM). May be used to discriminate between the effects of PKA and cAMP-regulated guanine-nucleotide-exchange factors (GEFs), such as GEFI or Epac (exchange protein directly activated by cAMP) and GEFII. Reported to induce neurite formation in NG 108-15 cells (~1 mM) by blocking the action of Rho kinase II.
          FormClear to off-white crystalline film
          Intert gas (Yes/No) Packaged under inert gas
          CAS number127243-85-0
          Chemical formulaC₂₀H₂₀BrN₃O₂S · 2HCl
          Structure formulaStructure formula
          Purity≥99% by HPLC
          SolubilityDMSO (200 mg/ml) or H₂O (25 mg/ml)
          Storage +2°C to +8°C
          Do Not Freeze Ok to freeze
          Special InstructionsFollowing reconstitution, store in the refrigerator (4°C). Stock solutions are stable for at up to 4 months at 4°C.
          Toxicity Standard Handling
          ReferencesLeemhuis, J., et al. 2002. J. Pharmacol. Exp. Ther. 300, 1000.
          Davies, S.P., et al. 2000. Biochem. J. 351, 95.
          Kawasaki, H., et al. 1998. Science 282, 2275.
          de Rooij, J., et al. 1998. Nature 396, 474.
          Findik, D., et al. 1995. J. Cell. Biochem. 57, 12.
          Geilen, C.C. 1992. FEBS Lett. 309, 381.
          Chijiwa, T., et al. 1990. J. Biol. Chem. 265, 5267.
          Combest, W.L., et al. 1988. J. Neurochem. 51, 1581.
          Citation
        • Ying Zhang, Mingjuan Liao and Maria L. Dufau. (2006) Phosphatidylinositol 3-kinase/protein kinase Cγ-induced phosphorylation of Sp1 and p107 repressor release have a critical role in histone deacetylase inhibitor-mediated depression of transcription of the luteinizing hormone receptor gene. Molecular and Cellular Biology 26, 6748-6761.