371962
H-89, Dihydrochloride
InSolution 10 mM, ≥99%, reversible ATP-competitive inhibitor of protein kinase A
Synonym(s):
InSolution H-89, Dihydrochloride, N-[2-(( p-Bromocinnamyl)amino)ethyl]-5-isoquinolinesulfonamide, 2HCl, PKA Inhibitor III, N-[2-((p-Bromocinnamyl)amino)ethyl]-5-isoquinolinesulfonamide, 2HCl, PKA Inhibitor III
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About This Item
Empirical Formula (Hill Notation):
C20H20BrN3O2S
Molecular Weight:
446.36
UNSPSC Code:
12352200
NACRES:
NA.77
Recommended Products
Quality Level
assay
≥99% (HPLC)
form
liquid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
shipped in
wet ice
storage temp.
−20°C
General description
A solution of H-89, Dihydrochloride (Cat. No. 371963) in anhydrous DMSO. H-89 is a cell-permeable selective 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 µM) by blocking the action of Rho kinase II.
Biochem/physiol Actions
Cell permeable: no
Primary Target
PKA
PKA
Product does not compete with ATP.
Reversible: no
Target Ki: 48 nM against protein kinase A
Packaging
Packaged under inert gas
Warning
Toxicity: Irritant (B)
Physical form
A 10 mM (1 mg/193 µl) solution of H-89, 2HCl (Cat. No. 371963) in DMSO.
Reconstitution
Following initial thaw, aliquot and freeze (-20°C).
Other Notes
Leemhuis, J., et al. 2002. J. Pharmacol. Exp. Ther.300, 1000.
Davies, S.P. et al. 2000. Biochem. J.351, 95.
de Rooij, J., et al. 1998. Nature.396, 474.
Kawasaki, H., et al. 1998. Science.282, 2275.
Findik, D., et al. 1995. J. Cell. Biochem.57, 12.
Hidaka, H., and Kobayashi, R. 1992. Annu. Rev. Pharmacol. Toxicol.32, 377.
Geilen, C.C., et al. 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.
Davies, S.P. et al. 2000. Biochem. J.351, 95.
de Rooij, J., et al. 1998. Nature.396, 474.
Kawasaki, H., et al. 1998. Science.282, 2275.
Findik, D., et al. 1995. J. Cell. Biochem.57, 12.
Hidaka, H., and Kobayashi, R. 1992. Annu. Rev. Pharmacol. Toxicol.32, 377.
Geilen, C.C., et al. 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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class
10 - Combustible liquids
wgk_germany
WGK 1
flash_point_f
188.6 °F - closed cup - (Dimethylsulfoxide)
flash_point_c
87 °C - closed cup - (Dimethylsulfoxide)
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