CE3F4 是选择性的Epac1拮抗剂，能够作用于 Epac1 (IC50:10.7 μM)和 Epac2(B) (IC50:66 μM)。

CE3F4 is a selective antagonist of exchange protein directly activated by cAMP (Epac1; IC50s of 10.7 μM and 66 μM for Epac1 and Epac2(B), respectively).

CE3F4 is a selective antagonist of Epac1, with IC50s of 10.7 μM and 66 μM for Epac1 and Epac2(B), respectively. CE3F4 is more active on Epac1 than (S)-stereoisomer ((S)-CE3F4, IC50, 56 μM), but less active than (R)-CE3F4 (IC50, 5.8 μM). CE3F4 (20 μM) inhibits Epac-induced Rap1 activation in living cultured HEK293 cells[2] and CE3F4 (20 μM) significantly inhibits the late phase of ERK activation stimulated by glucose in INS-1 cells[3]. CE3F4 (40 μM) specifically inhibits Epac1 guanine nucleotide exchange activity without interference with Rap1 activity or Epac1-Rap1 interaction. CE3F4 (50 μM) shows more inhibitory activities against GEF activity of Epac1, than that of Epac2(AB) or Epac2(B)[1]. CE3F4 reduces the exchange activity of Epac1 induced by 007, with IC50 of 23 ± 3 μM. CE3F4 has no influence on PKA activity.

143703-25-7

C11H10Br2FNO

351.01

DMSO:50 mg/mL (142.45 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years