4EGI-1

- Overview
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    Background
    
    4EGI-1 is a small-molecule inhibitor of eIF4E/eIF4G interaction with IC50 value of 125μM [1].
    The eIF4E/eIF4G complex plays a key role in gene translation initiation and is regulated by 4E-BP. Overexpression of eIF4E or eIF4G can induce malignant transformation in mammalian cells. As a mimic peptide of 4E-BP, 4EGI-1 competes with eIF4G and disrupts the association of eIF4E/eIF4G. The KD value for 4EGI-1 binding to eIF4E is 25μM. 4EGI-1 can not affect the binding of 4E-BP to eIF4E and instead causes increase of this binding level. In addition, 4EGI-1 is found to inhibit the Cap-dependent translation while enhances the initiation factor-independent translation. In Jurkat leukemia T cells, 4EGI-1 also causes eIF4G to be displaced from eIF4E [1].
    
    [1] Moerke N J, Aktas H, Chen H, et al. Small-molecule inhibition of the interaction between the translation initiation factors eIF4E and eIF4G. Cell, 2007, 128(2): 257-267.
- Properties
  - Alternative Name
    
    (E)-2-(2-(4-(3,4-dichlorophenyl)thiazol-2-yl)hydrazono)-3-(2-nitrophenyl)propanoic acid
    
    CAS Number
    
    315706-13-9
    
    Molecular Formula
    
    C18H12Cl2N4O4S
    
    Molecular Weight
    
    451.28
    
    Appearance
    
    A solid
    
    Purity
    
    98.97%
    
    Solubility
    
    ≥22.56 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Haimov O, Sehrawat U, et al. "Dynamic interactions of eIF4G1 with eIF4E and eIF1 underlie scanning dependent and independent translation." Mol Cell Biol. 2018 Jul 9. pii: MCB.00139-18. PMID:29987188
    2. Lee YC, Wang LJ, et al. "ABT-263-induced MCL1 upregulation depends on autophagy-mediated 4EBP1 downregulation in human leukemia cells." Cancer Lett. 2018 Jun 15;432:191-204. PMID:29913235

4EGI-1

Background

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