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ESI-09 

Cat. No.: HY-16704 Purity: 98.07%
Handling Instructions

ESI-09 is a novel noncyclic nucleotide EPAC antagonist with IC50 values of 3.2 and 1.4 μM for EPAC1 and EPAC2, respectively.

For research use only. We do not sell to patients.

ESI-09 Chemical Structure

ESI-09 Chemical Structure

CAS No. : 263707-16-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 106 In-stock
Estimated Time of Arrival: December 31
5 mg USD 96 In-stock
Estimated Time of Arrival: December 31
10 mg USD 178 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Customer Review

Based on 4 publication(s) in Google Scholar

Top Publications Citing Use of Products

    ESI-09 purchased from MCE. Usage Cited in: J Neurosci. 2016 Oct 12;36(41):10560-10573.

    The inhibition of Epac1 activity by ESI-09 reduces oligodendrocyte maturation.

    ESI-09 purchased from MCE. Usage Cited in: Acta Biochim Biophys Sin (Shanghai). 2017 Jul 1;49(7):573-580.

    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.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    ESI-09 is a novel noncyclic nucleotide EPAC antagonist with IC50 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 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].

    In Vivo

    Treatment with ESI-09 dramatically protects WT mice against R. australis infection with much milder disease manifestations and significantly improves survival[2].

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 47 mg/mL (142.09 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    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
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Cell Assay
    [1]

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [2]

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    330.77

    Formula

    C₁₆H₁₅ClN₄O₂

    CAS No.

    263707-16-0

    SMILES

    O=C(C1=NOC(C(C)(C)C)=C1)/C(C#N)=N/NC2=CC(Cl)=CC=C2

    Shipping

    Room temperature in continental US; may vary elsewhere

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    Product Name:
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    Cat. No.:
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    Cat. No.: HY-16704