[CAS NO. 263707-16-0] ESI-09
PRODUCTS SPECIFICATIONS [263707-16-0]
DESCRIPTION [263707-16-0]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 330.77 |
| Molecular Formula | C16H15ClN4O2 |
| SMILES | O=C(C1=NOC(C(C)(C)C)=C1)/C(C#N)=N/NC2=CC(Cl)=CC=C2 |
3 Publications Citing Use of MCE
Summary
ESI-09 is a novel noncyclic nucleotide EPAC antagonist with IC 50 values of 3.2 and 1.4 μM for EPAC1 and EPAC2, respectively.
IC50 & Target
IC50: 3.2 μM (EPAC1), 1.4 μM (EPAC2) [1]
In Vitro
While cAMP competes with 8-NBD-cAMP binding with an IC 50 of 39 µM, ESI-09 shows an increased potency with an apparent IC 50 of 10 µM. ESI-09 inhibis cAMP-mediated EPAC2 and EPAC1 GEF activity with an IC 50 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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Treatment with ESI-09 dramatically protects WT mice against R. australis infection with much milder disease manifestations and significantly improves survival [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 47 mg/mL ( 142.09 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.0232 mL | 15.1162 mL | 30.2325 mL |
| 5 mM | 0.6046 mL | 3.0232 mL | 6.0465 mL |
| 10 mM | 0.3023 mL | 1.5116 mL | 3.0232 mL |
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Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (7.56 mM); Clear solution
References
- [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.
- [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.