Merck, 371963-1MG, H-89, Dihydrochloride

General description
A 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.
Biochem/physiol Actions
Primary Target
PKA
Target Ki: 48 nM for protein kinase A
Preparation Note
Following reconstitution, store in the refrigerator (4°C). Stock solutions are stable for at up to 4 months at 4°C.
Other Notes
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)