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

H-89, Dihydrochloride, CAS 127243-85-0, is a cell-permeable, potent, selective, reversible, ATP-competitive inhibitor of protein kinase A (Ki = 48 nM).

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: N-[2-((p-Bromocinnamyl)amino)ethyl]-5-isoquinolinesulfonamide, 2HCl, PKA Inhibitor III

Primary Target: PKA
371963
Purchase on Sigma-Aldrich

Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
127243-85-0C₂₀H₂₀BrN₃O₂S · 2HCl

Products

Catalogue NumberPackaging Qty/Pack
371963-1MG Plastic ampoule 1 mg
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
Global Trade Item Number
Catalogue Number GTIN
371963-1MG 04055977213522

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.
    		•