EPAC 5376753 |
| Catalog No.GC31579 |
EPAC 5376753은 Swiss 3T3 세포에서 4μM의 IC50으로 Epac1을 억제하는 Epac의 알로스테릭 억제제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 302826-61-5
Sample solution is provided at 25 µL, 10mM.
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EPAC 5376753 is an allosterically inhibitor of Epac which inhibits Epac1 with an IC50 of 4 µM in Swiss 3T3 cells.
Epac is a key mediator of cAMP signaling. EPAC 5376753, the thiobarbituric acid modification of 5225554, has a greater ability to decrease the conformational changes of Epac necessary for its activation and to inhibit Epac signaling in cells. 5376753 selectively inhibits Epac-mediated migration in fibroblasts[1].
[1]. Brown LM, et al. Allosteric inhibition of Epac: computational modeling and experimental validation to identify allosteric sites and inhibitors. J Biol Chem. 2014 Oct 17;289(42):29148-57.
Cell experiment: | Swiss 3T3 cells are treated with EPAC 5376753 (1, 10, 25, 50, 75, 100 μM) or 1% dimethyl sulfoxide for 48 h. Cell viability is assessed using the CellTiter-Glo assay[1]. |
References: [1]. Brown LM, et al. Allosteric inhibition of Epac: computational modeling and experimental validation to identify allosteric sites and inhibitors. J Biol Chem. 2014 Oct 17;289(42):29148-57. | |
| Cas No. | 302826-61-5 | SDF | |
| Canonical SMILES | O=C(/C(C(N1)=O)=C/C2=CC=C(C3=CC=C(Cl)C=C3Cl)O2)NC1=S | ||
| Formula | C15H8Cl2N2O3S | M.Wt | 367.21 |
| Solubility | DMSO : 10 mg/mL (27.23 mM; ultrasonic and warming and heat to 60°C) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.7232 mL | 13.6162 mL | 27.2324 mL |
| 5 mM | 0.5446 mL | 2.7232 mL | 5.4465 mL |
| 10 mM | 0.2723 mL | 1.3616 mL | 2.7232 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 28 reference(s) in Google Scholar.)
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