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CE3F4 is an uncompetitive inhibitor of Epac1 activity toward its effector Rap1 in vitro (IC50 = 23 µM) and in cells.1,2. It has no effect on PKA activity. CE3F4 blocks Epac1-induced autophagy in cardiomyocytes stimulated with isoprenaline and blocks the activation of transient receptor potential canonical (TRPC) channels by the Epac activator 8-pCPT.3,4
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1. Identification of a tetrahydroquinoline analog as a pharmacological inhibitor of the cAMP-
2. Identification and validation of modulators of exchange protein activated by cAMP (Epac) activity: Structure-
3. Exchange protein directly activated by cAMP 1 promotes autophagy during cardiomyocyte hypertrophy. Cardiovasc. Res. 105(1), 55-64 (2015).
4. Proarrhythmic effect of sustained EPAC activation on TRPC3/4 in rat ventricular cardiomyocytes. J. Mol. Cell. Cardiol. 87, 74-78 (2015).