4EGI-1

Catalog No.S7369

4EGI-1 Chemical Structure

Molecular Weight(MW): 451.28

4EGI-1 is a competitive eIF4E/eIF4G interaction inhibitor by binding to eIF4E with KD of 25 μM.

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Cited by 4 Publications

2 Customer Reviews

  • Hep3B and PC3 cells were treated with 50 μmol/L 4EGI-1 or 5 μmol/L ABT alone or their combination for 48 hours, and then the cell viability was examined by CCK-8 assay. p, phosphorylated; t, total; T, Thr; S, Ser; *, P < 0.05; **, P < 0.01; ***, P < 0.001.

    Mol Cancer Ther, 2017, 16(9):1806-1818. 4EGI-1 purchased from Selleck.

    (C) C200 cells were treated with indicated concentrations of cisplatin in the absence and presence of 4egi-1 for 48 h. The numbers above the lines are combination indexes for the combination of cisplatin and 4egi-1.

    Int J Oncol, 2015, 47(6):2217-25.. 4EGI-1 purchased from Selleck.

Purity & Quality Control

Biological Activity

Description 4EGI-1 is a competitive eIF4E/eIF4G interaction inhibitor by binding to eIF4E with KD of 25 μM.
Targets
eIF4E/eIF4G [1]
(Cell-free assay)
25 μM(Kd)
In vitro

4EGI-1 disrupts the eIF4F complex and inhibits Cap-dependent translation in vitro. 4EGI-1 has proapoptotic activity in Jurkat cells, and potently inhibits cell growth with IC50 of approximately 6 μM in A549 lung cancer cells. [1] 4EGI-1 augments TRAIL-induced apoptosis through induction of DR5 and down-regulation of c-FLIP, independent of inhibition of cap-dependent protein translation in human lung cancer cells. [2] In addition, 4EGI-1, restores sensitivity to ABT-737 apoptosis through cap-dependent and -independent mechanisms in chronic lymphocytic leukemia. [3]

Protocol

Cell Research:[1]
+ Expand
  • Cell lines: Jurkat cells and A549 lung cancer cells.
  • Concentrations: ~60 μM
  • Incubation Time: 24 hours
  • Method: Cell viability is measured by treatment of Jurkat cells with compound for 24 h and by determination of intracellular ATP using the CellTiterGlo assay. For measurement of apoptotic DNA fragmentation, cells are treated for 24 h with 60 μM EGI-1 or 6.65 μM camptothecin in the presence or absence of 100 mM zVAD-FMK, a broad-spectrum caspase inhibitor. After fixation and staining with PI, cellular DNA content is determined by FACS analysis in a FACS Calibur machine. Nuclear morphology after 24 h EG1-1 treatment is visualized by staining of cells with Hoechst dye and fluorescence microscopy. For the A549 lung cancer cells, cell growth in the presence of 4EGI-1 is determined using the SRB staining method.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 90 mg/mL (199.43 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5%DMSO+pbs
For best results, use promptly after mixing.
4mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 451.28
Formula

C18H12Cl2N4O4S

CAS No. 315706-13-9
Storage powder
in solvent
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Frequently Asked Questions

  • Question 1:

    We were wondering if you had data on the racemic mixture composition of this compound. Specifically, the ratio of E to Z enantiomers.

  • Answer:

    The ratio of E to Z form is about 94.6 : 4.7. Please kindly find the HPLC enclosed, in which the E and Z form are seperated.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID