Biochem/physiol Actions

Reversible: yes

Product does not compete with ATP.

Primary TargetPKA 1

Cell permeable: yes

General description

A potent, cell-permeable, and reversible metabolically-stable cAMP antagonist that inhibits cAMP-dependent protein kinase and shows preference for PKA type I. More lipophilic than cAMP antagonist Rp-cAMPS (Cat. No. 116814).

Cell-permeable, potent, reversible, and metabolically stable antagonist of cAMP that is resistant to the action of mammalian cyclic nucleotide phosphodiesterases. Rp-8-Br-cAMPS is more lipophilic as compared to 8-Br-cAMP and Rp-cAMPS. In contrast to other common ATP-site inhibitors or to its parent compound Rp-cAMPS, Rp-8-Br-cAMPS discriminates between both isozymes of protein kinase A, preferring type I, thus providing additional selectivity. By occupying cAMP binding sites, prevents dissociation and activation of the kinase holoenzyme. λ _{= 264 nm (H2O, pH 7.0); εmax 17,000 M^-1cm^-1.}

Note: 5 µmol = 2.23 mg.

Legal Information

Sold under license of Patent DE 3,802,865.4 issued to BIOLOG LSI.

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

Other Notes

Calaghan, S.C., et al. 1999. Pflugers Arch. 437, 780.Gjertsen, B.T., et al. 1995. J. Biol. Chem. 270, 20599.Yokozaki, H., et al. 1992. Cancer Res.52, 2504.Dostmann, W.R. et al. 1990. J. Biol. Chem.265, 10484.

Packaging

5 µmol in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Warning

Toxicity: Standard Handling (A)