The acetoxymethyl group of 8-pCPT-2’-O-Me-cAMP-AM masks the charged polar phosphate and thus makes the molecule highly membrane-permeant. Inside the cell esterases release the more polar 8-pCPT-2’-O-Me-cAMP (Prod. No. BLG-C041), which is a potent and specific agonist of exchange factors directly activated by cAMP (Epac or cAMP-GEF), a newly discovered receptor for cyclic AMP.
Since a free 2’-ribose hydroxyl group in cyclic AMP is essential for stimulation of cAMP-dependent protein kinase (PKA), the methylated structure of 8-pCPT-2’-O-Me-cAMP is an extremely poor PKA activator and allows for specific discrimination between both signalling pathways.
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