4EGI-1
Based on 17 publication(s) in Google Scholar
4EGI-1 is an inhibitor of eIF4E/eIF4G interaction, with a Kd of 25 μM against eIF4E binding.
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- Pureza: 98.69%
- No. CAS: 315706-13-9
- Fòrmula: C18H12Cl2N4O4S
- Peso molecular:451.28
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Publications Citing Use of MedChemExpress (MCE) 4EGI-1
More- Nature. 2025 May;641(8065):1319-1328. [Abstract]
- Nat Commun. 2017 Jun 8;8:15617. [Abstract]
- Adv Sci (Weinh). 2024 Mar;11(11):e2305260. [Abstract]
- Leukemia. 2026 May;40(5):955-969. [Abstract]
- Nucleic Acids Res. 2022 Aug 12;50(14):8060-8079. [Abstract]
- Sci Adv. 2022 Jun 24;8(25):eabo1782. [Abstract]
- MedComm (2020). 2025 Feb 18;6(3):e70107. [Abstract]
- Cell Death Dis. 2020 Nov 15;11(11):982. [Abstract]
- Cell Commun Signal. 2023 May 9;21(1):107. [Abstract]
- Sci Signal. 2025 Sep 2;18(902):eadw3231. [Abstract]
- Mol Cancer Ther. 2018 Dec;17(12):2676-2688. [Abstract]
- Cancer Gene Ther. 2024 Oct;31(10):1486-1497. [Abstract]
- J Mol Med (Berl). 2019 Aug;97(8):1183-1193. [Abstract]
- J Neurochem. 2025 Mar;169(3):e70026. [Abstract]
- J Biol Chem. 2024 Jul 4:107530. [Abstract]
- Research Square Print. 2022 Jun.
- Patent. US20210299105A1.
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Bio/Physico-chemical Assay
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Flow Cytometry
Actividad biológica
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eIF4 |
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Cell Line
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Type | Value | Description | References |
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| A549 | IC50 |
6 μM
Compound: 28; 4EGI-1
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Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 70 mins by SRB dye based spectrophotometric analysis
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 70 mins by SRB dye based spectrophotometric analysis
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[PMID: 37669595] |
4EGI-1 is an inhibitor of eIF4E/eIF4G interaction, with a Kd of 25 μM against eIF4E binding. 4EGI-1 disrupts the eIF4F complex and inhibits expression of oncogenic proteins in mammalian cells. 4EGI-1 (0-40 μM) also exhibits proapoptotic activity and inhibits the growth of multiple cancer cell lines[1]. 4EGI-1 is cytotoxic to breast cancer cells, such as SKBR-3, MCF-7 and MDA-MB-231 cells, with the IC50 of appr 30 μM, and to the non-CSCs (Cancer stem cells), the IC50 is about 22 μM. 4EGI-1 enhances breast CSC differentiation (40 μM), and suppresses breast CSC induced HUVEC tube-like structure formation (8 μM). Moreover, 4EGI-1 selectively inhibits translation that persists in CSC maintenance and dissemination[2]. 4EGI-1 (50 μM) impairs the formation of eIF4F complex in U87 cells. 4EGI-1 (10, 50 and 100 μM) inhibits cell proliferation via inducing apoptosis in U87 cells, and the apoptosis is via Bax activation. 4EGI-1 causes mitochondrial dysfunction, and induces ER stress via GRP-78 activation, in U87 cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 315706-13-9
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Appearance Solid
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Peso molecular 451.28
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Fòrmula C18H12Cl2N4O4S
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Color Light yellow to khaki
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SMILES
O=C(O)/C(CC1=CC=CC=C1[N+]([O-])=O)=N/NC2=NC(C3=CC=C(Cl)C(Cl)=C3)=CS2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (17)
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Journal Impact Factor
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Most Recent
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Nature
2025 May;641(8065):1319-1328. PMID: 40140574
4EGI-1 purchased from MedChemExpress. Usage Cited in: Nature. 2025 May;641(8065):1319-1328. [Abstract]
4EGI-1 (200 μM; 5 h) induced disruption of the s-ISR-dependent induction of ATF4 in MEFs expressing control (shCon) or Eif2b5 shRNA (shEif2b5).
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Nat Commun
2017 Jun 8;8:15617. PMID: 28593995
4EGI-1 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2017 Jun 8;8:15617. [Abstract]
Immunoblot analysis of KRAS protein levels in parental (P) and resistant derivatives (R1 and R2) following 4 h treatment with the corresponding inhibitor 4EGI-1.
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Adv Sci (Weinh)
SHMT2 Mediates Small-Molecule-Induced Alleviation of Alzheimer Pathology Via the 5'UTR-dependent ADAM10 Translation Initiation. [Abstract]2024 Mar;11(11):e2305260. PMID: 38183387
4EGI-1 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Mar;11(11):e2305260. [Abstract]
4EGI-1 (50 µM; 24 h) significantly reduced the basal ADAM10 protein level in SH-SY5Y cells and further attenuated the enhancement of ADAM10 by KEN.
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Leukemia
BCR::ABL1 tyrosine kinase inhibitors induce ribosome collisions to activate ZAK-dependent ribotoxic stress and apoptosis in chronic myeloid leukemia. [Abstract]2026 May;40(5):955-969. PMID: 41912913 -
Nucleic Acids Res
LncRNA CTBP1-DT-encoded microprotein DDUP sustains DNA damage response signalling to trigger dual DNA repair mechanisms. [Abstract]2022 Aug 12;50(14):8060-8079. PMID: 35849344
4EGI-1 purchased from MedChemExpress. Usage Cited in: Nucleic Acids Res. 2022 Aug 12;50(14):8060-8079. [Abstract]
4EGI-1 (25 μM; 10-30 min) effectively blocked CPT-induced DDUP upregulation in 293T and HeLa cells.
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Sci Adv
2022 Jun 24;8(25):eabo1782. PMID: 35749506
4EGI-1 purchased from MedChemExpress. Usage Cited in: Sci Adv. 2022 Jun 24;8(25):eabo1782. [Abstract]
4EGI-1 (10-25 μM; 4 h) caused a rapid twofold reduction in BCL6 protein levels of CD4+ T cells from mice immunized with OVA/Alum.
4EGI-1 purchased from MedChemExpress. Usage Cited in: Sci Adv. 2022 Jun 24;8(25):eabo1782. [Abstract]
4EGI-1 (25 mg/kg; i.p.; 7 d) significantly reduced TFH cells in the spleen, identified using well-established double-positive biomarkers CXCR5 and PD-1 on CD4+ T cells.
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MedComm (2020)
Noncanonical feedback loop between "RIP3-MLKL" and "4EBP1-eIF4E" promotes neuronal necroptosis. [Abstract]2025 Feb 18;6(3):e70107. PMID: 39974664 -
Cell Death Dis
A small natural molecule CADPE kills residual colorectal cancer cells by inhibiting key transcription factors and translation initiation factors. [Abstract]2020 Nov 15;11(11):982. PMID: 33191401 -
Cell Commun Signal
25KDa branched polyethylenimine increases interferon-γ production in natural killer cells via improving translation efficiency. [Abstract]2023 May 9;21(1):107. PMID: 37161542 -
Sci Signal
MAPK and mTORC1 signaling converge to drive cyclin D1 protein production to enable cell cycle reentry in melanoma persister cells. [Abstract]2025 Sep 2;18(902):eadw3231. PMID: 40892895 -
Mol Cancer Ther
mTORC1/2 and Protein Translation Regulate Levels of CHK1 and the Sensitivity to CHK1 Inhibitors in Ewing Sarcoma Cells. [Abstract]2018 Dec;17(12):2676-2688. PMID: 30282812
4EGI-1 purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2018 Dec;17(12):2676-2688. [Abstract]
Immunoblot assessing protein synthesis, using puromycin labeling, and CHK1 levels of cell lines treated with the protein translation inhibitor 4EGI-1.
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Cancer Gene Ther
Arsenic trioxide and p97 inhibitor synergize against acute myeloid leukemia by targeting nascent polypeptides and activating the ZAKα-JNK pathway. [Abstract]2024 Oct;31(10):1486-1497. PMID: 39122830 -
J Mol Med (Berl)
2019 Aug;97(8):1183-1193. PMID: 31201471 -
J Neurochem
2025 Mar;169(3):e70026. PMID: 40026213 -
J Biol Chem
MGST3 regulates BACE1 protein translation and amyloidogenesis by controlling the RGS4-mediated AKT signaling pathway. [Abstract]2024 Jul 4:107530. PMID: 38971310 -
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Solvente y solubilidad
DMSO : 100 mg/mL (221.59 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.54 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.54 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
1 × 104 breast CSCs HMLER (CD44high/CD24low)FA cells and other indicated breast cancer cells are treated with DMSO, or [E]-4EGI-1 or [Z]-4EGI-1 at series of concentrations for 24 hours. The cells are performed cell viability assays with cell viability assay kit. Three independent experiments are performed. Average IC50 results are shown (mean ± SD, t-test, two-tailed)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[2]
In the tumor xenografted assay, 1×105 breast cancer stem cells (CSCs) are mixed with 100 μL Matrigel/DMEM mixture (Matrigel: DMEM = 1:2). Breast CSCs/Matrigel/DMEM mixtures are injected into NOD/SCID female mice mammary glands by subcutaneous injection. After the tumor formation (about 75 mm3 in volume, 5 mice/group), DMSO, or 75 mg/kg [E]-4EGI-1, or 75 mg/kg [Z]-4EGI-1 is injected into the mice by intraperitoneal injection daily for 30 days. Tumor volumes are measured every three days. At the 30th day, mice are sacrificed and tumors are excised. Tumors weights are measured. Tumor tissue samples are used for immunohistostaining, Western blot and immunoprecipitation analyses[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (281 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Portuguese - PT (396 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Moerke NJ, et al. Small-molecule inhibition of the interaction between the translation initiation factors eIF4E and eIF4G. Cell. 2007 Jan 26;128(2):257-67. [Content Brief]
[2]. Yi T, et al. 4EGI-1 targets breast cancer stem cells by selective inhibition of translation that persists in CSC maintenance, proliferation and metastasis. Oncotarget. 2014 Aug 15;5(15):6028-37. [Content Brief]
[3]. Wu M, et al. Anti-Cancer Effect of Cap-Translation Inhibitor 4EGI-1 in Human Glioma U87 Cells: Involvement of Mitochondrial Dysfunction and ER Stress. Cell Physiol Biochem. 2016;40(5):1013-1028. Epub 2016 Dec 12. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2159 mL | 11.0796 mL | 22.1592 mL | 55.3980 mL |
| 5 mM | 0.4432 mL | 2.2159 mL | 4.4318 mL | 11.0796 mL | |
| 10 mM | 0.2216 mL | 1.1080 mL | 2.2159 mL | 5.5398 mL | |
| 15 mM | 0.1477 mL | 0.7386 mL | 1.4773 mL | 3.6932 mL | |
| 20 mM | 0.1108 mL | 0.5540 mL | 1.1080 mL | 2.7699 mL | |
| 25 mM | 0.0886 mL | 0.4432 mL | 0.8864 mL | 2.2159 mL | |
| 30 mM | 0.0739 mL | 0.3693 mL | 0.7386 mL | 1.8466 mL | |
| 40 mM | 0.0554 mL | 0.2770 mL | 0.5540 mL | 1.3849 mL | |
| 50 mM | 0.0443 mL | 0.2216 mL | 0.4432 mL | 1.1080 mL | |
| 60 mM | 0.0369 mL | 0.1847 mL | 0.3693 mL | 0.9233 mL | |
| 80 mM | 0.0277 mL | 0.1385 mL | 0.2770 mL | 0.6925 mL | |
| 100 mM | 0.0222 mL | 0.1108 mL | 0.2216 mL | 0.5540 mL |
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