中文名 | CE3F4 |
英文名 | CE3F4 |
别名 | 化合物CE3F4 |
英文别名 | CE3F4 5,7-Dibromo-6-fluoro-3,4-dihydro-2-methyl-1(2H)-quinolinecarboxaldehyde 1(2H)-Quinolinecarboxaldehyde, 5,7-dibromo-6-fluoro-3,4-dihydro-2-methyl- |
CAS | 143703-25-7 |
化学式 | C11H10Br2FNO |
分子量 | 351.01 |
存储条件 | Room Temprature |
体外研究 | CE3F4 is a selective antagonist of Epac1, with IC 50 s 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). 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. CE3F4 (20 μM) significantly inhibits the late phase of ERK activation stimulated by glucose in INS-1 cells. |
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