| Bioactivity | HJC0350 is a potent and specific EPAC2 antagonist with an IC50 of 0.3 µM. | ||||||||||||
| Target | IC50: 0.3 µM (EPAC2) | ||||||||||||
| Invitro | 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]. | ||||||||||||
| Name | HJC0350 | ||||||||||||
| CAS | 885434-70-8 | ||||||||||||
| Formula | C15H19NO2S | ||||||||||||
| Molar Mass | 277.38 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
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| Reference | [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. |