Synonyms: 5,7-Dibromo-6-fluoro-3,4-dihydro-2-methyl-1(2H)-quinolinecarboxaldehyde
Molecular Formula: C11H10Br2FNO
Molecular Weight: 351.01
Linear Structural Formula: C11H10Br2FNO
MDL Number: MFCD30182244
Purity: >=98% (HPLC)
Storage: -20C
Biochem Physiol Actions: CE3F4 is a tetrahydroquinoline derivative that blocks agonist-stimulated Epac1 (exchange protein directly activated by cAMP isoform 1) guanine nucleotide exchange activity toward its effector Rap1 (IC50 = 23 muM; Epac agonist = 2 muM 8-CPT-2'-O-Me-cAMP) by targeting agonist-bound Epac1 in an agonist-uncompetitive manner without affecting the GDP exchange on Rap1, Rap1-Epac1 interaction, or PKA type I/II activity (CbetaRIbeta & CalphaRIIbeta). CE3F4 (20 muM) effectively inhbits cellular Rap1 activation upon 10 muM Sp-8-pCPT-2'-O-Me-cAMPS (Epac1-transfected HEK293 and rat neonatal cardiac myocytes) or 10 muM beta-adrenergic receptor agonist isoprenaline stimulation (beta1AR & Epac1 dually transfected HEK293). The isolated CE3F4 R enantiomer is reported to display 10-fold Epac1 selectivity over Epac2, and is 10-times more potent than the CE3F S enantiomer against Epac1.