1. Cell Cycle/DNA Damage
  2. Eukaryotic Initiation Factor (eIF)

4EGI-1 

Cat. No.: HY-19831 Purity: >98.0%
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

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 119 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
5 mg USD 108 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 144 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
25 mg USD 264 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 420 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg USD 672 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

    4EGI-1 purchased from MCE. Usage Cited in: Nat Commun. 2017 Jun 8;8:15617.

    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.

    Featured Recommendations

    Related Small Molecules:

    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

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

    IC50 & Target

    Kd: 25 μM (eIF4E/eIF4G)[1]

    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].

    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].

    References
    Preparing Stock Solutions
    Concentration Volume 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.
    Cell Assay
    [2]

    4EGI-1 is dissolved in DMSO[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]

    4EGI-1 is dissolved in DMSO[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
    Molecular Weight

    451.28

    Formula

    C₁₈H₁₂Cl₂N₄O₄S

    CAS No.

    315706-13-9

    SMILES

    O=C(O)/C(CC1=CC=CC=C1[N+]([O-])=O)=N/NC2=NC(C3=CC=C(Cl)C(Cl)=C3)=CS2

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 35 mg/mL

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product name

     

    Salutation

    Applicant name *

     

    Email address *

    Phone number *

     

    Organization name *

    Country or Region *

     

    Requested quantity *

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    4EGI-1
    Cat. No.:
    HY-19831
    Quantity: