4EGI-1

• CAT Number: I003126
• CAS Number: 315706-13-9
• Molecular Formula: C18H12Cl2N4O4S
• Molecular Weight: 451.30
• Purity: ≥95%
• Synonyms: eIF4E/eIF4G Interaction Inhibitor
• Target: eIF4E/eIF4G
• Solubility: DMSO: ≥ 35 mg/mL
• Storage: -20°C
• IC50: 50μM (72h, for HNE1 cell)
• IUPAC Name: (2E)-2-[[4-(3,4-dichlorophenyl)-1,3-thiazol-2-yl]hydrazinylidene]-3-(2-nitrophenyl)propanoic acid
• InChI: InChI=1S/C18H12Cl2N4O4S/c19-12-6-5-10(7-13(12)20)15-9-29-18(21-15)23-22-14(17(25)26)8-11-3-1-2-4-16(11)24(27)28/h1-7,9H,8H2,(H,21,23)(H,25,26)/b22-14+
• InChIKey: KFRKRECSIYXARE-HYARGMPZSA-N
• SMILES: C1=CC=C(C(=C1)C/C(=N\NC2=NC(=CS2)C3=CC(=C(C=C3)Cl)Cl)/C(=O)O)[N+](=O)[O-]

4EGI-1(Cat No.:I003126) is a small molecule inhibitor that specifically targets eIF4E/eIF4G interaction, disrupting the eukaryotic translation initiation complex. It inhibits the binding of eIF4E to eIF4G, preventing the assembly of the translation initiation complex and subsequently inhibiting protein synthesis. 4EGI-1 has been shown to selectively inhibit the translation of oncogenic mRNAs, leading to the suppression of tumor growth in various cancer cell lines and xenograft models. Additionally, 4EGI-1 has demonstrated anti-inflammatory effects by inhibiting the synthesis of pro-inflammatory cytokines. It has potential as a therapeutic agent for cancer and inflammatory diseases.

Reference

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M, Fan S, Zhang H. 4EGI-1 induces apoptosis and enhances radiotherapy sensitivity
in nasopharyngeal carcinoma cells via DR5 induction on 4E-BP1 dephosphorylation.
Oncotarget. 2016 Apr 19;7(16):21728-41. doi: 10.18632/oncotarget.7824. PubMed
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2: Wang H, Huang F, Wang J, Wang P, Lv W, Hong L, Li S, Zhou J. The synergistic
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MK2206. Cell Cycle. 2015;14(2):232-42. doi: 10.4161/15384101.2014.977096. PubMed
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6: Yefidoff-Freedman R, Chen T, Sahoo R, Chen L, Wagner G, Halperin JA, Aktas BH,
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7: Yi T, Kabha E, Papadopoulos E, Wagner G. 4EGI-1 targets breast cancer stem
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Aktas BH, Chorev M, Halperin JA, Wagner G. Structure of the eukaryotic
translation initiation factor eIF4E in complex with 4EGI-1 reveals an allosteric
mechanism for dissociating eIF4G. Proc Natl Acad Sci U S A. 2014 Aug
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(4EGI-1) mimetic and their in vitro characterization as inhibitors of
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