302826-61-5

EPAC 5376753 (302826-61-5) is an allosteric inhibitor of Epac1, IC50= 4 μM.1 Does not inhibit PKA or adenylyl cyclase. Inhibits biological functions mediated by Epac including cAMP-induced increase in migration of cardiac fibroblasts. A useful tool for probing the role of Epac in cellular physiology and pathophysiology.2

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1) Brown et al. (2014), Allosteric inhibition of Epac: computational modeling and experimental validation to identify allosteric sites and inhibitors; J. Biol. Chem., 289 29148 2) Parnell et al. (2015), The future of EPAC-targeted therapies: agonism versus antagonism; Trends Pharmacol. Sci., 36 203