CE3F4产品描述: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 IC
50s of 10.7 μM and 66 μM for Epac1 and Epac2(B), respectively. CE3F4 is more active on Epac1 than (S)-stereoisomer ((S)-CE3F4, IC
50, 56 μM), but less active than (R)-CE3F4 (IC
50, 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 IC
50 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].
产品链接:
www.medchemexpress.com/CE3F4.html研究领域:
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更新时间:2024/1/2 10:10:55
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