4EGI-1
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].
References:
[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.
- 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
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 451.28 |
| Cas No. | 315706-13-9 |
| Formula | C18H12Cl2N4O4S |
| Solubility | ≥22.56 mg/mL in DMSO |
| Chemical Name | (E)-2-(2-(4-(3,4-dichlorophenyl)thiazol-2-yl)hydrazono)-3-(2-nitrophenyl)propanoic acid |
| SDF | Download SDF |
| Canonical SMILES | O=C(O)/C(CC1=CC=CC=C1[N+]([O-])=O)=N/NC2=NC(C3=CC=C(Cl)C(Cl)=C3)=CS2 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
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Cell lines |
Jurkat cells |
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Preparation method |
The solubility of this compound in DMSO is > 22.6 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
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Reacting condition |
0 ~ 200 μM; 24 hrs |
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Applications |
In Jurkat cells, 4EGI-1 (> 50 μM) treatment induced cell death after 24 hrs. In addition, 4EGI-1 significantly increased subG1 DNA content, which was inhibited by cotreatment with the caspase inhibitor zVAD-FMK. |
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References: [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. |
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| Description | 4EGI-1 is a competitive inhibitor of eIF4E/eIF4G interaction by binding to eIF4E with KD of 25 μM. | |||||
| Targets | eIF4E/eIF4G | |||||
| IC50 | 25 μM (KD) | |||||
Quality Control & MSDS
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Chemical structure
Related Biological Data
Related Biological Data
