tcsc0029107 CE3F4

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

IC50 & Target: IC50: 10.7 μM (Epac1), 66 μM (Epac2(B))^[1]

In Vitro: 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 (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 (40 μM) specifically inhibits Epac1 guanine nucleotide exchange activity without interference with Rap1 activity or Epac1-Rap1 interaction. CE3F4 has no influence on PKA activity. CE3F4 (20 μM) inhibits Epac-induced Rap1 activation in living cultured HEK293 cells^[2]. CE3F4 (20 μM) significantly inhibits the late phase of ERK activation stimulated by glucose in INS-1 cells^[3].