8-(4-Chlorophenylthio)-2′-O-methyladenosine 3′,5′-cyclic Monophosphate . sodium salt

Specific, potent and membrane permeant activator of the Epac cAMP receptor. Activates Epac1 and Epac2, the guanine nucleotide-exchange factors (GEFs) for the small GTPases Rap1 and Rap2. Does not activate protein kinase A (PKA), neither in vitro nor in vivo and is therefore a valuable tool to specifically discriminate between PKA- and Epac-mediated effects. Since a free 2′-ribose hydroxyl group in cyclic AMP is essential for stimulation of PKA, the methylated structure of 8-CPT-2′-O-Me-cAMP is an extremely poor PKA activator. Its high lipophilicity allows for good membrane permeability in most biosystems and its increased resistance towards phosphodiesterases prevents rapid hydrolysis.