CE3F4

CE3F4

Application

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).

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 µM; Epac agonist = 2 µM 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 (CβRIβ & CαRIIβ). CE3F4 (20 µM) effectively inhbits cellular Rap1 activation upon 10 µM Sp-8-pCPT-2′-O-Me-cAMPS (Epac1-transfected HEK293 and rat 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 Epac2, and is 10-times more potent than the CE3F S enantiomer against Epac1.

Epac1 is a downstream effector of the cyclic adenosine monophosphate (cAMP) pathway.

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Code Description Colour Manufacturer Storage Temp. Solubility Form Assay Price Quantity
3575736 CE3F4 white to beige SIGMA-ALDRICH −20°C DMSO: 2 mg/mL, clear (warmed) powder ≥98% (HPLC)
£402.54 (exc VAT) per 25MG
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3575737 CE3F4 white to beige SIGMA-ALDRICH −20°C DMSO: 2 mg/mL, clear (warmed) powder ≥98% (HPLC)
£124.10 (exc VAT) per 5MG
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