ESI-09
Based on 10 publication(s) in Google Scholar
ESI-09 is a novel noncyclic nucleotide EPAC antagonist with IC50 values of 3.2 and 1.4 μM for EPAC1 and EPAC2, respectively.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.15%
- CAS. Nr.: 263707-16-0
- Formel: C16H15ClN4O2
- Molecular Weight:330.77
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Publications Citing Use of MedChemExpress (MCE) ESI-09
More- Signal Transduct Target Ther. 2022 Aug 31;7(1):290. [Abstract]
- Small Methods. 2025 Mar;9(3):e2401144. [Abstract]
- Acta Pharmacol Sin. 2025 May;46(5):1289-1302. [Abstract]
- Oncogene. 2025 Sep;44(34):3142-3148. [Abstract]
- J Agric Food Chem. 2026 Apr 22;74(15):12132-12144. [Abstract]
- iScience. 2025 Jan 21;28(2):111856. [Abstract]
- J Neurosci. 2016 Oct 12;36(41):10560-10573. [Abstract]
- Cell Signal. 2025 Jan 22:111615. [Abstract]
- Acta Biochim Biophys Sin (Shanghai). 2017 Jul 1;49(7):573-580. [Abstract]
- bioRxiv. 2026 Mar 31:2026.03.29.715116. [Abstract]
Customer Validation & Images
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WB
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Cell Proliferation/Viability Assay
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Cell Imaging/Staining
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Histological Imaging/Staining
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IF
Biologische Aktivität
IC50: 3.2 μM (EPAC1), 1.4 μM (EPAC2)[1]
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Cell Line
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Type | Value | Description | References |
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| HeLa S3 | IC50 |
10.8 μM
Compound: ESI-09
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Inhibition of recombinant C-terminal FLAG/HA-tagged EPAC1 (unknown origin) expressed in retrovirus infected human HeLaS3 cells assessed as reduction in cAMP-mediated guanine nucleotide exchange factor activity in presence of C-terminal truncated Rap1B (1
Inhibition of recombinant C-terminal FLAG/HA-tagged EPAC1 (unknown origin) expressed in retrovirus infected human HeLaS3 cells assessed as reduction in cAMP-mediated guanine nucleotide exchange factor activity in presence of C-terminal truncated Rap1B (1
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[PMID: 27190593] |
| HeLa S3 | IC50 |
4.4 μM
Compound: ESI-09
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Inhibition of recombinant C-terminal FLAG/HA-tagged EPAC2 (unknown origin) expressed in retrovirus infected human HeLaS3 cells assessed as reduction in cAMP-mediated guanine nucleotide exchange factor activity in presence of C-terminal truncated Rap1B (1
Inhibition of recombinant C-terminal FLAG/HA-tagged EPAC2 (unknown origin) expressed in retrovirus infected human HeLaS3 cells assessed as reduction in cAMP-mediated guanine nucleotide exchange factor activity in presence of C-terminal truncated Rap1B (1
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[PMID: 27190593] |
While cAMP competes with 8-NBD-cAMP binding with an IC50 of 39 μM, ESI-09 shows an increased potency with an apparent IC50 of 10 μM. ESI-09 inhibis cAMP-mediated EPAC2 and EPAC1 GEF activity with an IC50 of 1.4 and 3.2μM, respectively. ESI-09 could fit well into the functional cAMP-binding pocket of EPAC1, establishing favorable hydrophobic and hydrogen bonding interactions with the protein’s active-site residues. ESI-09 inhibits 007-AM-stimulated Akt phosphorylation at T308 and S473 in a dose-dependent manner. ESI-09 inhibits pancreatic cancer cells AsPC-1 and PANC-1 migration. ESI-09 inhibits EPAC1-mediated adhesion of PDA cells on collagen I[1]. Exposure to ESI-09 significantly reduces intracellular and total bacterial counts in HUVECs at 30 min postinfection with 10 multiplicities of infection (MOI) of R. australis compared with similarly infected controls[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 263707-16-0
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Appearance Solid
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Molecular Weight 330.77
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Formel C16H15ClN4O2
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Color Yellow to orange
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SMILES
O=C(C1=NOC(C(C)(C)C)=C1)/C(C#N)=N/NC2=CC(Cl)=CC=C2
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (10)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
p53 positively regulates the proliferation of hepatic progenitor cells promoted by laminin-521. [Abstract]2022 Aug 31;7(1):290. PMID: 36042225 -
Small Methods
An Integrated Microcurrent Delivery System Facilitates Human Parathyroid Hormone Delivery for Enhancing Osteoanabolic Effect. [Abstract]2025 Mar;9(3):e2401144. PMID: 39420694
ESI-09 purchased from MedChemExpress. Usage Cited in: Small Methods. 2025 Mar;9(3):e2401144. [Abstract]
ESI‐09 (EPAC1 inhibitor) (10 µM; 0.5 h) blocked linearization of VE-cadherin and the transformation of intracellular SFs to CBs in HUVEC monolayers after MDS stimulation.
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Acta Pharmacol Sin
Endothelial Gsα deficiency promotes ferroptosis and exacerbates atherosclerosis in apolipoprotein E-deficient mice via the inhibition of NRF2 signaling. [Abstract]2025 May;46(5):1289-1302. PMID: 39806063
ESI-09 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2025 May;46(5):1289-1302. [Abstract]
ESI-09 (20 μM) ounteracted the increase in NRF2 expression and interfered with the increase in CTCF expression in HAECs promoted by Gsα overexpression.
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Oncogene
Identification of RAPGEF3 as the therapeutic vulnerability of basal-subtype lung squamous cell carcinoma. [Abstract]2025 Sep;44(34):3142-3148. PMID: 40781157
ESI-09 purchased from MedChemExpress. Usage Cited in: Oncogene. 2025 Sep;44(34):3142-3148. [Abstract]
ESI-09 (5-10 µM) treatment significantly inhibited L78 and H520 cell growth.
ESI-09 purchased from MedChemExpress. Usage Cited in: Oncogene. 2025 Sep;44(34):3142-3148. [Abstract]
Treatment with ESI-09 (10 µM; 72 h) also caused notable morphological changes in L78 cells, e.g., cell shrinkage and loss of cell adhesion.
ESI-09 purchased from MedChemExpress. Usage Cited in: Oncogene. 2025 Sep;44(34):3142-3148. [Abstract]
ESI-09 (10 mg/kg; i.g.; twice a week for 3 weeks) reduced Ki67 levels and increased CC3 levels of tumors in PDX 1059 mice.
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J Agric Food Chem
Preventive Effect of Caffeic Acid Phenethyl Ester, an Active Component of Propolis, against TNF-α-Induced Endothelial Dysfunction through the β2-Adrenoceptor-Mediated eNOS/NO Signal Pathway. [Abstract]2026 Apr 22;74(15):12132-12144. PMID: 41957988 -
iScience
The matricellular protein Fibulin-5 regulates β-cell proliferation in an autocrine/paracrine manner. [Abstract]2025 Jan 21;28(2):111856. PMID: 39995864 -
J Neurosci
Olig2-Targeted G-Protein-Coupled Receptor Gpr17 Regulates Oligodendrocyte Survival in Response to Lysolecithin-Induced Demyelination. [Abstract]2016 Oct 12;36(41):10560-10573. PMID: 27733608
ESI-09 purchased from MedChemExpress. Usage Cited in: J Neurosci. 2016 Oct 12;36(41):10560-10573. [Abstract]
The inhibition of Epac1 activity by ESI-09 reduces oligodendrocyte maturation.
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Cell Signal
D-Ala2-GIP (1-30) promotes angiogenesis by facilitating endothelial cell migration via the Epac/Rap1/Cdc42 signaling pathway. [Abstract]2025 Jan 22:111615. PMID: 39855534 -
Acta Biochim Biophys Sin (Shanghai)
Lithium and an EPAC-specific inhibitor ESI-09 synergistically suppress pancreatic cancer cell proliferation and survival. [Abstract]2017 Jul 1;49(7):573-580. PMID: 28475672
ESI-09 purchased from MedChemExpress. Usage Cited in: Acta Biochim Biophys Sin (Shanghai). 2017 Jul 1;49(7):573-580. [Abstract]
PANC-1 cells treated with different concentrations of combination of CHIR99021 and ESI-09 (0, 1 μM+1 μM, 3 μM+3 μM, 5 μM+5 μM, and 10 μM+10 μM) for 48 h.
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bioRxiv
2026 Mar 31:2026.03.29.715116. PMID: 41959225
Lösungsmittel & Löslichkeit
DMSO : ≥ 47 mg/mL (142.09 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.56 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Protokoll
INS-1 cells are plated in 96-well plates precoated with polylysine. After overnight incubation, the medium is replaced with Krebs-Ringer bicarbonate (KRB) containing 2.9 mM glucose. After an additional 2-hour incubation, the cells are treated with ESI-09 or DMSO vehicle as a control in fresh KRB containing 11.8 mM glucose for 10 minutes, followed by a 30-minute stimulation with 10 µM 007-AM. The supernatant is collected, and insulin is quantified using an Ultra Sensitive Rat Insulin ELISA kit from Crystal Chem Inc[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice: ESI-09 is dissolved in buffered saline containing 10% (vol/vol) ethanol and 10% (vol/vol) Tween-80. Thirty-three WT C57BL/6 mice are divided into four groups [11 mice (group A), 10 mice (group B), 6 mice each (groups C and D)]. Groups A and C are treated with the Epac-specific inhibitor ESI-09 [10 mg/kg ] via i.p. injection for 5 d before infection, whereas groups B and D are treated with vehicle, followed by i.v. inoculation of R. australis for groups A and B or mock inoculation for groups C and D. ESI-09 or vehicle treatment is continued for another 7 d until mice are killed on day 8. During the course of the experiments, animals are monitored daily for signs of illness and mortality[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (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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Handling Instructions (2659 KB)
Verweise
[1]. Almahariq M, et al. A novel EPAC-specific inhibitor suppresses pancreatic cancer cell migration and invasion. Mol Pharmacol. 2013 Jan;83(1):122-8. [Content Brief]
[2]. Gong B, et al. Exchange protein directly activated by cAMP plays a critical role in bacterial invasion during fatal rickettsioses. Proc Natl Acad Sci U S A. 2013 Nov 26;110(48):19615-20. [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 |
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| DMSO | 1 mM | 3.0232 mL | 15.1162 mL | 30.2325 mL | 75.5812 mL |
| 5 mM | 0.6046 mL | 3.0232 mL | 6.0465 mL | 15.1162 mL | |
| 10 mM | 0.3023 mL | 1.5116 mL | 3.0232 mL | 7.5581 mL | |
| 15 mM | 0.2015 mL | 1.0077 mL | 2.0155 mL | 5.0387 mL | |
| 20 mM | 0.1512 mL | 0.7558 mL | 1.5116 mL | 3.7791 mL | |
| 25 mM | 0.1209 mL | 0.6046 mL | 1.2093 mL | 3.0232 mL | |
| 30 mM | 0.1008 mL | 0.5039 mL | 1.0077 mL | 2.5194 mL | |
| 40 mM | 0.0756 mL | 0.3779 mL | 0.7558 mL | 1.8895 mL | |
| 50 mM | 0.0605 mL | 0.3023 mL | 0.6046 mL | 1.5116 mL | |
| 60 mM | 0.0504 mL | 0.2519 mL | 0.5039 mL | 1.2597 mL | |
| 80 mM | 0.0378 mL | 0.1890 mL | 0.3779 mL | 0.9448 mL | |
| 100 mM | 0.0302 mL | 0.1512 mL | 0.3023 mL | 0.7558 mL |
ESI-09 Related Classifications
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