4EGI-1

• CAT Number: I003126
• CAS Number: 315706-13-9
• Molecular Formula: C18H12Cl2N4O4S
• Molecular Weight: 451.3
• Purity: ≥95%
• Target: eIF4E/eIF4G
• Solubility: DMSO: ≥ 35 mg/mL
• Storage: -20°C
• IC50: 50μM (72h, for HNE1 cell)
• InChIKey: KFRKRECSIYXARE-HYARGMPZSA-N
• SMILES: ClC1=C(Cl)C=CC(C2=CSC(N/N=C(CC3=C([N+]([O-])=O)C=CC=C3)/C(O)=O)=N2)=C1

4EGI-1(CAT: 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

1: Wang W, Li J, Wen Q, Luo J, Chu S, Chen L, Qing Z, Xie G, Xu L, Alnemah MM, Li
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
inhibition of breast cancer proliferation by combined treatment with 4EGI-1 and
MK2206. Cell Cycle. 2015;14(2):232-42. doi: 10.4161/15384101.2014.977096. PubMed
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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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