ESI-05
Based on 4 publication(s) in Google Scholar
ESI-05 is a specific exchange proteins directly activated by cAMP 2 (EPAC2) inhibitor. ESI-05 inhibits cAMP-mediated EPAC2 GEF activity with an IC50 of 0.43 μM. ESI-05 can be used for the research of diabetes, insulin secretion and neurological disorders.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.78%
- No. CAS: 5184-64-5
- Fòrmula: C16H18O2S
- Peso molecular:274.38
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
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Publications Citing Use of MedChemExpress (MCE) ESI-05
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Actividad biológica
IC50: 0.43 μM (EPAC2)[1]
ESI-05 (0.01 μM -1 nM) inhibits cAMP-mediated EPAC2 GEF activity with IC50 of 0.43 μM, but completely ineffective in suppressing EPAC1 GEF activity[1].
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ESI-05 (1, 5, 10, and 25 μM; 5 min) selectively modulates EPAC2 activation in living cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293 cells
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Concentration:1, 5, 10, and 25 μM
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Incubation Time:5 min
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Result:Led to a dose-dependent reduction of the EPAC-selective cAMP analog (007-AM) induced Rap1 activation.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Intracranial hemorrhage (ICH) model[2]
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Dosage:2, 4, and 8 mg/kg
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Administration:
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Result:Decreased the apoptosis rate of nerve cells in the cortex accompanied by a corresponding decrease in the protein expression of phosphorylated p38, Bcl-2like protein 11 (BIM), and caspase-3.
Chemical Information
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No. CAS 5184-64-5
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Appearance Solid
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Peso molecular 274.38
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Fòrmula C16H18O2S
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Color White to off-white
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SMILES
O=S(C1=C(C)C=C(C)C=C1C)(C2=CC=C(C)C=C2)=O
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Synonyms
NSC 116966
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Cell Metab
Cancer cells co-opt nociceptive nerves to thrive in nutrient-poor environments and upon nutrient-starvation therapies. [Abstract]2022 Dec 6;34(12):1999-2017.e10. PMID: 36395769
ESI-05 purchased from MedChemExpress. Usage Cited in: Cell Metab. 2022 Dec 6;34(12):1999-2017.e10. [Abstract]
CGRP-mediated enhanced interaction between Rap1 and Raptor is antagonized by blocking the activation of Rap1 into Rap1-GTP using ESI-05 (10 µM; 1 h), in Cal27 cells.
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Cell Rep Med
2025 Aug 19;6(8):102254. PMID: 40713970 -
Stem Cells
β-Arrestin 2 and Epac2 Cooperatively Mediate DRD1-Stimulated Proliferation of Human Neural Stem Cells and Growth of Human Cerebral Organoids. [Abstract]2022 Sep 26;40(9):857-869. PMID: 35772103 -
Neurosci Lett
Overexpression of miR-338-5p in exosomes derived from mesenchymal stromal cells provides neuroprotective effects by the Cnr1/Rap1/Akt pathway after spinal cord injury in rats. [Abstract]2021 Sep 14:761:136124. PMID: 34302891
Solvente y solubilidad
DMSO : 50 mg/mL (182.23 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Tsalkova T, et al. Isoform-specific antagonists of exchange proteins directly activated by cAMP. Proc Natl Acad Sci U S A. 2012 Nov 6;109(45):18613-8. [Content Brief]
[2]. Yan Zhuang, et al. Inhibition of EPAC2 Attenuates Intracerebral Hemorrhage-Induced Secondary Brain Injury via the p38/BIM/Caspase-3 Pathway. J Mol Neurosci. 2019 Mar;67(3):353-363. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.6446 mL | 18.2229 mL | 36.4458 mL | 91.1145 mL |
| 5 mM | 0.7289 mL | 3.6446 mL | 7.2892 mL | 18.2229 mL | |
| 10 mM | 0.3645 mL | 1.8223 mL | 3.6446 mL | 9.1115 mL | |
| 15 mM | 0.2430 mL | 1.2149 mL | 2.4297 mL | 6.0743 mL | |
| 20 mM | 0.1822 mL | 0.9111 mL | 1.8223 mL | 4.5557 mL | |
| 25 mM | 0.1458 mL | 0.7289 mL | 1.4578 mL | 3.6446 mL | |
| 30 mM | 0.1215 mL | 0.6074 mL | 1.2149 mL | 3.0372 mL | |
| 40 mM | 0.0911 mL | 0.4556 mL | 0.9111 mL | 2.2779 mL | |
| 50 mM | 0.0729 mL | 0.3645 mL | 0.7289 mL | 1.8223 mL | |
| 60 mM | 0.0607 mL | 0.3037 mL | 0.6074 mL | 1.5186 mL | |
| 80 mM | 0.0456 mL | 0.2278 mL | 0.4556 mL | 1.1389 mL | |
| 100 mM | 0.0364 mL | 0.1822 mL | 0.3645 mL | 0.9111 mL |
ESI-05 Related Classifications
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