| Identification | Back Directory | [Name]
CE3F4 | [CAS]
143703-25-7 | [Synonyms]
CE3F4
CE3F4 >=98% (HPLC)
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- | [Molecular Formula]
C11H10Br2FNO | [MOL File]
143703-25-7.mol | [Molecular Weight]
351.01 |
| Hazard Information | Back Directory | [Uses]
CE3F4 has been used as a selective exchange protein directly activated by cAMP isoform 1 (Epac1) inhibitor in cell proliferation assay to study the influence of Epac type I on cell proliferation of C6 cells (a model of glioma). | [Biological Activity]
CE3F4 is a tetrahydroquinoline derivative th at blocks agonist-stimulated Epac1 (exchange protein directly activated by cAMP isoform 1) guanine nucleotide exchange activity toward its effector Rap1 (IC50 = 23 μM; Epac agonist = 2 μM 8-CPT-2μ-O-Me-cAMP) by targeting agonist-bound Epac1 in an agonist-uncompetitive manner without affecting the GDP exchange on Rap1Rap1-Epac1 interactionor PKA type I/II activity (CβRIβ & CαRIIβ). CE3F4 (20 μM) effectively inhbits cellular Rap1 activation upon 10 μM Sp-8-pCPT-2μ-O-Me-cAMPS (Epac1-transfected HEK293 and r at neonatal cardiac myocytes) or 10 μM β-adrenergic receptor agonist isoprenaline stimulation (β1AR & Epac1 dually transfected HEK293). The isolated CE3F4 R enantiomer is reported to display 10-fold Epac1 selectivity over Epac2and is 10-times more potent than the CE3F S enantiomer against Epac1.''Epac1 is a downstream effector of the cyclic adenosine monophosp | [storage]
Store at -20°C |
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