HJC0350 has an apparent IC50 value of 0.3 µM for competing with 8-NBD-cAMP binding of EPAC2, and is about 133-fold more potent than cAMP. HJC0350 is found not to inhibit EPAC1-mediated Rap1-GDP exchange activity at 25 µM in the presence of equal concentration of cAMP, indicating that it is EPAC2-specific antagonists. Pretreatment of HEK293/EPAC2-FL cells with 10 µM HJC0350 fully blocks the 007-AM induced decrease of FRET[1].
Kinase Assay
Cell Assay
Animal Administration
References
[1]. Chen H, et al. Identification and characterization of small molecules as potent and specific EPAC2 antagonists. J Med Chem. 2013 Feb 14;56(3):952-62.
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