Rp-8-bromo-Cyclic AMPS (sodium salt)

Description

Rp-8-bromo-Cyclic AMPS (Rp-8-bromo-cAMPS) is a cell-permeable cAMP analog that combines an exocyclic sulfur substitution in the equatorial position of the cyclophosphate ring with a bromine substitution in the adenine base of cAMP.^1,2 It acts as an antagonist of cAMP-dependent protein kinases (PKAs) and is resistant to hydrolysis by cyclic nucleotide phosphodiesterases. Rp-8-bromo-cAMPS more effectively antagonizes cAMP-dependent activation of purified PKA type I from rabbit muscle than PKA type II from bovine heart.²

Uses

Rp-8-Br-cAMPS sodium is an analog of cAMP and an inhibitor of PKA. Rp-8-Br-cAMPS sodium occupies cAMP binding sites on PKA type I regulatory subunits, thereby preventing PKA dissociation and activation. Rp-8-Br-cAMPS sodium can be used in the study of tumors and retrovirus-induced immune deficiency. Rp-8-Br-cAMPS sodium also inhibits insulin secretion[1][2][3].

in vivo

References

1. Dostmann, W.R., Taylor, S.S., Genieser, H.G., et al. Probing the cyclic nucleotide binding sites of cAMP-dependent protein kinases I and II with analogs of adenosine 3',5'-cyclic phosphorothioates J. Biol. Chem. 265(18),10484-10491(1990).
2. Gjertsen, B.T., Mellgran, G., Otten, A., et al. Novel (Rp)-cAMPS analogs as tools for inhibition of cAMP-kinase in cell culture. Basal cAMP-kinase activity modulates interleukin-1β action J. Biol. Chem. 270(35),20599-20607(1995).