Biochem/physiol Actions

Cell permeable: no

Reversible: no

Target K_i: 48 nM against protein kinase A

Product does not compete with ATP.

Primary TargetPKA

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 (K_i = 48 nM). Inhibits other kinases at several fold higher concentrations: myosin light chain kinase (K_i = 28.3 µM), Ca²⁺/calmodulin-dependent protein kinase II (K_i = 29.7 µM), protein kinase C (K_i = 31.7 µM), casein kinase I (K_i = 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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

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.

Packaging

1 mg in Plastic ampoule

Packaged under inert gas

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).

Warning

Toxicity: Irritant (B)