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

4EGI-1 

Cat. No.: HY-19831 Purity: 99.91%
COA Handling Instructions

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
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 131 In-stock
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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 11 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

    Appearance

    Solid

    Formula

    C18H12Cl2N4O4S
    CAS No.
    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)

    *"≥" 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
    10 mM 0.2216 mL 1.1080 mL 2.2159 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

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

    Purity: 99.91%

    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
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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.

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

    This equation is commonly abbreviated as: C1V1 = C2V2

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    × = ×
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    Keywords:

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

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