1. Metabolic Enzyme/Protease
  2. Acyltransferase
  3. ESI-05

ESI-05  (Synonyms: NSC 116966)

Cat. No.: HY-117656 Purity: 99.94%
COA Handling Instructions

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.

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

ESI-05 Chemical Structure

ESI-05 Chemical Structure

CAS No. : 5184-64-5

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 73 In-stock
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10 mM * 1 mL in DMSO USD 73 In-stock
Solid
5 mg USD 66 In-stock
10 mg USD 116 In-stock
50 mg USD 352 In-stock
100 mg USD 605 In-stock
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Customer Review

Based on 4 publication(s) in Google Scholar

Top Publications Citing Use of Products

    ESI-05 purchased from MedChemExpress. Usage Cited in: Cell Metab. 2022 Nov 11;S1550-4131(22)00490-9.  [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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    Description

    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[1][2].

    IC50 & Target

    IC50: 0.43 μM (EPAC2)[1]

    In Vitro

    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].
    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.

    Western Blot Analysis[1]

    Cell Line: HEK293 cells
    Concentration: 1, 5, 10, and 25 μM
    Incubation Time: 5 min
    Result: Led to a dose-dependent reduction of the EPAC-selective cAMP analog (007-AM) induced Rap1 activation.
    In Vivo

    ESI-05 (2, 4, and 8 mg/kg) decreases neuronal apoptosis by inhibiting the p38/BIM pathway in vivo[2].

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

    Animal Model: Intracranial hemorrhage (ICH) model[2]
    Dosage: 2, 4, and 8 mg/kg
    Administration:
    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.
    Molecular Weight

    274.38

    Formula

    C16H18O2S

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=S(C1=C(C)C=C(C)C=C1C)(C2=CC=C(C)C=C2)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

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

    DMSO : 50 mg/mL (182.23 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.6446 mL 18.2229 mL 36.4458 mL
    5 mM 0.7289 mL 3.6446 mL 7.2892 mL
    10 mM 0.3645 mL 1.8223 mL 3.6446 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

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

      Solubility: ≥ 2.5 mg/mL (9.11 mM); Clear solution

    *All of the co-solvents are available by MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.94%

    References
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    ESI-05 Related Classifications

    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.

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    This equation is commonly abbreviated as: C1V1 = C2V2

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    × = ×
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    Product Name:
    ESI-05
    Cat. No.:
    HY-117656
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