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HJC0350 is a selective inhibitor of exchange protein directly activated by cAMP 2 (Epac2) with an IC50 value of 300 nM for competition with 8-NBD-cAMP binding.1 It inhibits Epac2 guanine nucleotide exchange activity but does not inhibit Epac1-mediated Rap1-GDP exchange or cAMP-mediated protein kinase A (PKA) activation in vitro, indicating it is selective for Epac2 at a concentration of 25 μM. HJC0350 also blocks stimulation of Epac2, but not Epac1, by 007-AM in HEK293 cells.
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1. Identification and characterization of small molecules as potent and specific EPAC2 antagonists. J. Med. Chem. 56(3), 952-962 (2013).