2. Anti-infection
  3. Virus Protease
  4. ESI-09

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

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CAS 番号 : 263707-16-0

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10 mM * 1 mL in DMSO
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10 mg $116 在庫あり
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カスタマーレビュー

Based on 9 publication(s) in Google Scholar

ESI-09 関連抗体

Top Publications Citing Use of Products

    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.

    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.

    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.

    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.

    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.

    • 生物活性

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    製品説明

    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]
    Cellular Effect
    Cell Line Type Value Description References
    HeLa S3 IC50
    10.8 μM
    Compound: ESI-09
    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 to 167 residues)-Mant-GDP by spectrofluorometric analysis
    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 to 167 residues)-Mant-GDP by spectrofluorometric analysis
    		[PMID: 27190593]
    HeLa S3 IC50
    4.4 μM
    Compound: ESI-09
    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 to 167 residues)-Mant-GDP by spectrofluorometric analysis
    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 to 167 residues)-Mant-GDP by spectrofluorometric analysis
    		[PMID: 27190593]
    体外実験

    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.

    ESI-09 関連抗体
    体内実験

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

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    分子量

    330.77

    分子式

    C16H15ClN4O2
    CAS 番号
    Appearance

    Solid

    Color

    Yellow to orange

    SMILES

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

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    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.

    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
    View the 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.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

    C1

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    体積 （開始）

    V1

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    濃度 （終了）

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    体内:

    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.

    • Protocol 1

      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.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (7.56 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
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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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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    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.
    純度とドキュメンテーション

    純度: 99.65%

    COA (246 KB) LCMS (93 KB)

    取扱説明書 (2659 KB)
    参考文献
    細胞実験
    [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].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    動物実験
    [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].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    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 3.0232 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
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    ESI-09 Related Classifications

    • Molarity Calculator

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    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    ESI-09263707-16-0ESI09ESI 09Virus ProteaseInhibitorinhibitorinhibit

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    製品名:
    ESI-09
    製品番号:
    HY-16704
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