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CE3F4 is a selective antagonist of exchange protein directly activated by cAMP (Epac1; IC50s of 10.7 μM and 66 μM for Epac1 and Epac2(B), respectively).

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 5 mg | $47 | In Stock | In Stock | |
| 10 mg | $80 | In Stock | In Stock | |
| 25 mg | $156 | In Stock | In Stock | |
| 50 mg | $288 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $52 | In Stock | In Stock |
| Description | CE3F4 is a selective antagonist of exchange protein directly activated by cAMP (Epac1; IC50s of 10.7 μM and 66 μM for Epac1 and Epac2(B), respectively). |
| Targets&IC50 | EPAC2B:66 μM, EPAC1:10.7 μM |
| In vitro | CE3F4 acts as a selective antagonist of the Epac1, demonstrating inhibitory concentrations (IC50) of 10.7 μM for Epac1 and 66 μM for Epac2(B), illustrating greater potency against Epac1 as compared to its (S)-stereoisomer ((S)-CE3F4, IC50, 56 μM), yet showing lesser activity than its (R)-stereoisomer ((R)-CE3F4, IC50, 5.8 μM). At a concentration of 20 μM, CE3F4 effectively inhibits Epac-induced Rap1 activation in HEK293 cells and significantly reduces the late-phase ERK activation prompted by glucose in INS-1 cells. Moreover, at 40 μM, it specifically targets Epac1's guanine nucleotide exchange activity without disturbing Rap1's function or the Epac1-Rap1 interaction. CE3F4 at a 50 μM concentration exhibits stronger inhibitory effects on the guanine nucleotide exchange factor (GEF) activity of Epac1 compared to both forms of Epac2. It also inhibits the Epac1 exchange activity induced by compound 007, with an IC50 of 23 ± 3 μM, while not affecting PKA activity. |
| Molecular Weight | 351.01 |
| Formula | C11H10Br2FNO |
| Cas No. | 143703-25-7 |
| Smiles | CC1CCc2c(Br)c(F)c(Br)cc2N1C=O |
| Relative Density. | no data available |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 50 mg/mL (142.45 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.7 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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