Description
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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
PKA 1
Product does not compete with ATP.
Reversible: yes
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
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.
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
Disclaimer
Toxicity: Standard Handling (A)
