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CE3F4 

Cat. No.: HY-108539
Handling Instructions

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.

For research use only. We do not sell to patients.

CE3F4 Chemical Structure

CE3F4 Chemical Structure

CAS No. : 143703-25-7

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10 mg USD 240 Get quote
25 mg USD 540 Get quote

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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 IC50s of 10.7 μM and 66 μM for Epac1 and Epac2(B), respectively. CE3F4 is more active on Epac1 than (S)-stereoisomer ((S)-CE3F4, IC50, 56 μM), but less active than (R)-CE3F4 (IC50, 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 IC50 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].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8489 mL 14.2446 mL 28.4892 mL
5 mM 0.5698 mL 2.8489 mL 5.6978 mL
10 mM 0.2849 mL 1.4245 mL 2.8489 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[2]

To determine Epac1 exchange activity, 200 nM of purified GST-Rap1A preloaded with bGDP are incubated at 22°C in exchange buffer (50 mM Tris-HCl (pH 7.5), 50 mM NaCl, 5 mM MgCl2, 5 mM 1,4-dithioerythritol, 5% glycerol, 0.01% Nonidet P-40) in the presence of 100 nM purified GST-Epac1 or GST-Epac1-Cat; 20 μM unlabeled GDP; and defined concentrations of cAMP, cyclic nucleotide analogs, and test compounds (CE3F4). Experiments are performed in black 384-well plates in a final volume of 30 μL. bGDP fluorescence (excitation, 480 nm and emission, 535 nm) is measured using a multilabel plate reader[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[3]

Cells are cultured overnight in 96-well black-walled plates at 37°C and 5% CO2, then washed twice in phosphate buffered saline. Cells are pre-incubated for two hours in glucose-free, modified KRBH supplemented with 0.05% fatty acid-free BSA at 37°C and 5% CO2. The pre-incubation buffer is decanted, and cells are stimulated with 18 mM glucose in KRBH. Cells are incubated with or without inhibitors (CE3F4) in modified KRBH for 30 min at 37°C and 5 % CO2 before glucose stimulation. The reactions are terminated at the indicated time points by decanting the treatments and fixing the cells with 4% formaldehyde. In experiments using pharmacological inhibitors, reactions are terminated 10 min after glucose stimulation is initiated. Total ERK and pERK is measured using the Phospho-ERK1 (T202/Y204) / ERK2 (T185/Y187) Cell-Based ELISA. Total ERK1/ERK2 is measured at 450 nm with excitation at 360 nm, and phosphorylated ERK1/ERK2 is measured at 600 nm with excitation at 540 nm, using a Synergy 4 Microplate Reader. The data are expressed as the ratio of pERK to total ERK then normalized and expressed as either fold over basal or % glucose response[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

351.01

Formula

C₁₁H₁₀Br₂FNO

CAS No.

143703-25-7

SMILES

O=CN1C(C)CCC2=C1C=C(Br)C(F)=C2Br

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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CE3F4
Cat. No.:
HY-108539
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CE3F4

Cat. No.: HY-108539