EPAC 5376753 is an allosterically inhibitor of Epac which inhibits Epac1 with an IC50 of 4 µM in Swiss 3T3 cells.
Epac is a key mediator of cAMP signaling. EPAC 5376753, the thiobarbituric acid modification of 5225554, has a greater ability to decrease the conformational changes of Epac necessary for its activation and to inhibit Epac signaling in cells. 5376753 selectively inhibits Epac-mediated migration in fibroblasts[1].
[1]. Brown LM, et al. Allosteric inhibition of Epac: computational modeling and experimental validation to identify allosteric sites and inhibitors. J Biol Chem. 2014 Oct 17;289(42):29148-57.
















