| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C18H12Cl2N4O4S |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
4EGI-1 is an inhibitor of the eIF4E/eIF4G interaction, with a Kd of 25 μM against eIF4E binding. It is supplied as a light yellow to khaki solid (C18H12Cl2N4O4S, MW 451.28) at 98.69% purity.
Physical & Chemical Properties
| CAS Number | 315706-13-9 |
|---|---|
| Molecular Formula | C18H12Cl2N4O4S |
| Molecular Weight | 451.28 g/mol |
| Purity | 98.69% |
| Appearance | Solid |
| Color | Light yellow to khaki |
| SMILES | O=C(O)/C(CC1=CC=CC=C1[N+]([O-])=O)=N/NC2=NC(C3=CC=C(Cl)C(Cl)=C3)=CS2 |
| Target | eIF4 |
| Signaling Pathway | Cell Cycle/DNA Damage; Autophagy; Apoptosis |
| Solubility | In Vitro: DMSO: 100 mg/mL (221.59 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 2 years; -20°C, 1 year. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 100 mg/mL (221.59 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 2 years) or -20°C (up to 1 year); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.5 mg/mL (5.54 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | 2.5 mg/mL (5.54 mM); suspension; requires sonication |
| How to prepare | Gives a suspension at 2.5 mg/mL. The suspension is suitable for oral and intraperitoneal dosing. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Data provided by the manufacturer.
In Vitro
4EGI-1 inhibits the eIF4E/eIF4G interaction, with a Kd of 25 μM for eIF4E binding. 4EGI-1 disrupts the eIF4F complex and suppresses expression of oncogenic proteins in mammalian cells. 4EGI-1 (0-40 μM) also shows proapoptotic activity and inhibits growth of several cancer cell lines[1]. 4EGI-1 exerts cytotoxicity on breast cancer cells such as SKBR-3, MCF-7 and MDA-MB-231, with an IC50 of approximately 30 μM, and its IC50 is about 22 μM for non-CSCs (Cancer stem cells). 4EGI-1 promotes breast CSC differentiation (40 μM) and suppresses HUVEC tube-like structure formation induced by breast CSC (8 μM). Moreover, 4EGI-1 selectively inhibits translation that sustains CSC maintenance and dissemination[2]. In U87 cells, 4EGI-1 (50 μM) impairs eIF4F complex formation. 4EGI-1 (10, 50 and 100 μM) inhibits U87 cell proliferation by inducing apoptosis, which proceeds through Bax activation. 4EGI-1 causes mitochondrial dysfunction and induces ER stress through GRP-78 activation in U87 cells[3].
In Vivo
4EGI-1 (75 mg/kg, i.p.) suppresses tumor growth and tumor angiogenesis of breast cancer stem cells (CSC) in vivo[2]. In mice bearing U87 cells, 4EGI-1 (75 mg/kg, i.p.) reduces tumor volume and weight[3].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
Cell Assay[2]
Treat 1 × 104 breast CSCs HMLER (CD44high/CD24low)FA cells along with the other indicated breast cancer cells with DMSO, or [E]-4EGI-1 or [Z]-4EGI-1 at a series of concentrations for 24 hours. Measure cell viability with a cell viability assay kit. Run three independent experiments. Report average IC50 results as mean ± SD (t-test, two-tailed)[2].
Animal Administration[2]
Mice[2] For the tumor xenograft assay, mix 1×105 breast cancer stem cells (CSCs) with 100 μL Matrigel/DMEM mixture (Matrigel: DMEM = 1:2). Inject the breast CSCs/Matrigel/DMEM mixtures subcutaneously into the mammary glands of NOD/SCID female mice. After tumors form (about 75 mm3 in volume, 5 mice/group), inject DMSO, or 75 mg/kg [E]-4EGI-1, or 75 mg/kg [Z]-4EGI-1 by intraperitoneal injection daily for 30 days. Measure tumor volumes every three days. On the 30th day, sacrifice the mice and excise the tumors. Weigh the tumors. Use tumor tissue samples for immunohistostaining, Western blot and immunoprecipitation analyses[2].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Plasticity of the mammalian integrated stress response. Nature 2025 May;641(8065):1319-1328. PMID: 40140574
Codon bias imposes a targetable limitation on KRAS-driven therapeutic resistance. Nat Commun 2017 Jun 8:8:15617.
LncRNA CTBP1-DT-encoded microprotein DDUP sustains DNA damage response signalling to trigger dual DNA repair mechanisms. Nucleic Acids Res 2022 Aug 12;50(14):8060-8079. PMID: 35849344
Noncanonical feedback loop between "RIP3-MLKL" and "4EBP1-eIF4E" promotes neuronal necroptosis. MedComm (2020) 2025 Feb 18;6(3):e70107. PMID: 39974664
SHMT2 Mediates Small-Molecule-Induced Alleviation of Alzheimer Pathology Via the 5'UTR-dependent ADAM10 Translation Initiation. Adv Sci (Weinh) 2024 Mar;11(11):e2305260. PMID: 38183387
Translational regulation of TFH cell differentiation and autoimmune pathogenesis. Sci Adv 2022 Jun 24;8(25):eabo1782. PMID: 35749506
A small natural molecule CADPE kills residual colorectal cancer cells by inhibiting key transcription factors and translation initiation factors. Cell Death Dis 2020 Nov 15;11(11):982. PMID: 33191401
25KDa branched polyethylenimine increases interferon-γ production in natural killer cells via improving translation efficiency. Cell Commun Signal 2023 May 9;21(1):107. PMID: 37161542
BCR::ABL1 tyrosine kinase inhibitors induce ribosome collisions to activate ZAK-dependent ribotoxic stress and apoptosis in chronic myeloid leukemia. Leukemia 2026 May;40(5):955-969. PMID: 41912913
MAPK and mTORC1 signaling converge to drive cyclin D1 protein production to enable cell cycle reentry in melanoma persister cells. Sci Signal 2025 Sep 2;18(902):eadw3231. PMID: 40892895
