2. Cell Cycle/DNA Damage Autophagy Apoptosis
  3. Eukaryotic Initiation Factor (eIF) Autophagy Apoptosis
  4. 4EGI-1

4EGI-1 is an inhibitor of eIF4E/eIF4G interaction, with a Kd of 25 μM against eIF4E binding.

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

4EGI-1 Chemical Structure

4EGI-1 Chemical Structure

CAS No. : 315706-13-9

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 131 In-stock
Solid
5 mg USD 119 In-stock
10 mg USD 158 In-stock
25 mg USD 290 In-stock
50 mg USD 462 In-stock
100 mg USD 739 In-stock
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Customer Review

Based on 14 publication(s) in Google Scholar

Other Forms of 4EGI-1:

4EGI-1 Related Antibodies

Top Publications Citing Use of Products

    4EGI-1 purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2018 Dec;17(12):2676-2688.  [Abstract]

    Immunoblot assessing protein synthesis, using puromycin labeling, and CHK1 levels of cell lines treated with the protein translation inhibitor 4EGI-1.

    4EGI-1 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2017 Jun 8;8:15617.  [Abstract]

    Immunoblot analysis of KRAS protein levels in parental (P) and resistant derivatives (R1 and R2) following 4 h treatment with the corresponding inhibitors Rapamycin, AZD2014, MLN0128, BEZ235 and 4EGI-1. Images are cropped for clarity from the same exposure of the same membrane.

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    4EGI-1 is an inhibitor of eIF4E/eIF4G interaction, with a Kd of 25 μM against eIF4E binding.

    IC50 & Target

    eIF4

     

    In Vitro

    4EGI-1 is an inhibitor of eIF4E/eIF4G interaction, with a Kd of 25 μM against eIF4E binding. 4EGI-1 disrupts the eIF4F complex and inhibits expression of oncogenic proteins in mammalian cells. 4EGI-1 (0-40 μM) also exhibits proapoptotic activity and inhibits the growth of multiple cancer cell lines[1]. 4EGI-1 is cytotoxic to breast cancer cells, such as SKBR-3, MCF-7 and MDA-MB-231 cells, with the IC50 of appr 30 μM, and to the non-CSCs (Cancer stem cells), the IC50 is about 22 μM. 4EGI-1 enhances breast CSC differentiation (40 μM), and suppresses breast CSC induced HUVEC tube-like structure formation (8 μM). Moreover, 4EGI-1 selectively inhibits translation that persists in CSC maintenance and dissemination[2]. 4EGI-1 (50 μM) impairs the formation of eIF4F complex in U87 cells. 4EGI-1 (10, 50 and 100 μM) inhibits cell proliferation via inducing apoptosis in U87 cells, and the apoptosis is via Bax activation. 4EGI-1 causes mitochondrial dysfunction, and induces ER stress via GRP-78 activation, in U87 cells[3].

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

    4EGI-1 Related Antibodies
    In Vivo

    4EGI-1 (75 mg/kg, i.p.) inhibits breast cancer stem cells (CSC) tumor growth and tumorangiogenesis in vivo[2]. 4EGI-1 (75 mg/kg, i.p.) shows inhibitory effect on the tumor volume and weight in mice bearing U87 cells[3].

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

    451.28

    Formula

    C18H12Cl2N4O4S
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to khaki

    SMILES

    O=C(O)/C(CC1=CC=CC=C1[N+]([O-])=O)=N/NC2=NC(C3=CC=C(Cl)C(Cl)=C3)=CS2
    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 : ≥ 35 mg/mL (77.56 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 2.2159 mL 11.0796 mL 22.1592 mL
    5 mM 0.4432 mL 2.2159 mL 4.4318 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)

    Mass
    =
    Concentration
    ×
    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

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    Volume (final)

    V2

    In Vivo:

    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    90% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (5.54 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    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.
    Purity & Documentation

    Purity: 99.91%

    SDS (393 KB)

    COA (251 KB) LCMS (274 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [2]

    1 × 104 breast CSCs HMLER (CD44high/CD24low)FA cells and other indicated breast cancer cells are treated with DMSO, or [E]-4EGI-1 or [Z]-4EGI-1 at series of concentrations for 24 hours. The cells are performed cell viability assays with cell viability assay kit. Three independent experiments are performed. Average IC50 results are shown (mean ± SD, t-test, two-tailed)[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2]

    Mice[2]
    In the tumor xenografted assay, 1×105 breast cancer stem cells (CSCs) are mixed with 100 μL Matrigel/DMEM mixture (Matrigel: DMEM = 1:2). Breast CSCs/Matrigel/DMEM mixtures are injected into NOD/SCID female mice mammary glands by subcutaneous injection. After the tumor formation (about 75 mm3 in volume, 5 mice/group), DMSO, or 75 mg/kg [E]-4EGI-1, or 75 mg/kg [Z]-4EGI-1 is injected into the mice by intraperitoneal injection daily for 30 days. Tumor volumes are measured every three days. At the 30th day, mice are sacrificed and tumors are excised. Tumors weights are measured. Tumor tissue samples are used for immunohistostaining, Western blot and immunoprecipitation analyses[2].

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

    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 2.2159 mL 11.0796 mL 22.1592 mL 55.3980 mL
    5 mM 0.4432 mL 2.2159 mL 4.4318 mL 11.0796 mL
    10 mM 0.2216 mL 1.1080 mL 2.2159 mL 5.5398 mL
    15 mM 0.1477 mL 0.7386 mL 1.4773 mL 3.6932 mL
    20 mM 0.1108 mL 0.5540 mL 1.1080 mL 2.7699 mL
    25 mM 0.0886 mL 0.4432 mL 0.8864 mL 2.2159 mL
    30 mM 0.0739 mL 0.3693 mL 0.7386 mL 1.8466 mL
    40 mM 0.0554 mL 0.2770 mL 0.5540 mL 1.3849 mL
    50 mM 0.0443 mL 0.2216 mL 0.4432 mL 1.1080 mL
    60 mM 0.0369 mL 0.1847 mL 0.3693 mL 0.9233 mL
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    4EGI-1 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.

    Keywords:

    4EGI-1315706-13-9Eukaryotic Initiation Factor (eIF)AutophagyApoptosisInhibitorinhibitorinhibit

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