4EGI-1

SKU: orb1305195

Description

4EGI-1 is a small molecule inhibitor that competitively disrupts the eIF4E/eIF4G interaction with a binding affinity (K_D) of 25 µM. It serves as a valuable research tool for studying cap-dependent translation initiation in cancer biology and has been utilized in both cellular and in vitro assays to investigate oncogenic protein synthesis.

Research Area

Cell Biology

Key Properties

• CAS Number: 315706-13-9
• MW: 451.28
• Purity: 99.59% (May vary between batches)
• Formula: C₁₈H₁₂Cl₂N₄O₄S
• SMILES: OC(=O)C(\Cc1ccccc1[N+]([O-])=O)=N\Nc1nc(cs1)-c1ccc(Cl)c(Cl)c1
• Target: Autophagy,PERK,Apoptosis
• Solubility: DMSO:100 mg/mL (221.59 mM)

Bioactivity

• Target IC50:
  eIF4E-eIF4G:25 μM(Kd)
• In Vivo:
  In Jurkat cells, 4EGI-1 promotes apoptosis. It effectively inhibits cell growth in A549 lung cancer cells (IC50=6 μM). In human lung cancer cells, 4EGI-1 enhances TRAIL-induced apoptosis by inducing DR5 and downregulating c-FLIP, thereby inhibiting cap-dependent protein translation.
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• Cell Research:
  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 uorescence 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)
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

4EGI 1, 4EGI1, 4EGI-1, Autophagy, Apoptosis, inhibit, Inhibitor, eIF-4E/eIF-4G, Eukaryotic Initiation Factor (eIF)

Compound Identifiers

PubChem CID

5717952