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

371963
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Key Specifications Table

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

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371963-1MG
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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
      Quality LevelMQ100
      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

      H-89, Dihydrochloride - CAS 127243-85-0 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      H-89, Dihydrochloride - CAS 127243-85-0 - Calbiochem 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.

      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.