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Inhibitor Resource

Inhibitor Database

Inhibitor Libraries
  H-89, Dihydrochloride
Cat. No. 371963  
All Categories » Calbiochem » Inhibitors » Kinase and Phosphatase » Protein Kinase A (PKA)

N-[2-((p-Bromocinnamyl)amino)ethyl]-5-isoquinolinesulfonamide, 2HCl

Off-white solid. PACKAGED UNDER INERT GAS. A cell-permeable, selective, 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. Purity: ≥99% by HPLC. CAS 127243-85-0.

Ref.: 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.
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SolubilityMolecular FormulaMol. Wt.
DMSO or EtOH:H2O (1:1) C20H20BrN3O2S · 2HCl 519.3 


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Material Safety Data Sheets:
371963: H-89, Dihydrochloride - English
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Related Categories:
All Categories » Calbiochem » Inhibitors » Kinase and Phosphatase » Protein Kinase A (PKA)

Selected Citations:
  1. 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.