| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C28H18N2O6 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
4E1RCat is an inhibitor of cap-dependent translation that inhibits the eIF4E:eIF4GI interaction, with an IC50 of ~4 μM. It is supplied as a brown to purplish red solid (C28H18N2O6, MW 478.45) at 99.04% purity.
Physical & Chemical Properties
| CAS Number | 328998-25-0 |
|---|---|
| Molecular Formula | C28H18N2O6 |
| Molecular Weight | 478.45 g/mol |
| Purity | 99.04% |
| Appearance | Solid |
| Color | Brown to purplish red |
| SMILES | O=C(O)C1=CC=C(N2C(/C(C=C2C3=CC=CC=C3)=C\C4=CC=C(C5=CC=C([N+]([O-])=O)C=C5)O4)=O)C=C1 |
| Target | eIF4 |
| Signaling Pathway | Cell Cycle/DNA Damage; Autophagy |
| Solubility | In Vitro: DMSO: 18.33 mg/mL (38.31 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 | 18.33 mg/mL (38.31 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.
Data provided by the manufacturer.
In Vitro
4E1RCat inhibits the eIF4E:eIF4GI interaction, with an IC50 of ~4 μM. Binding of 4E1RCat to eIF4E also interferes with eIF4G and 4E-BP binding. 4E1RCat inhibits cap-dependent ribosome recruitment to mRNA[1]. 4E1RCat blocks capped mRNA translation, which is activated by CDK1/CYCB1. In HeLa and U2OS cells, nearly all newly made protein in mitosis and in interphase relies on the cap and is sensitive to 4E1RCat treatment[2].
In Vivo
4E1RCat (15 mg/kg, i.p.) affects the chemosensitivity of Pten+/-Eμ-Myc tumors in mice. 4E1RCat (15 mg/kg, i.p.) makes Pten+/-Eμ-Myc and Tsc2+/-Eμ-Myc lymphomas more sensitive to doxorubicin (Dxr) cytotoxicity, and in mice 4E1RCat acts on translation[1].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
Cell Assay[1]
Seed TSC2+/-Eμ-Myc and Eμ-Myc lymphomas in 96-well plates at 106 cells/mL with increasing concentrations of doxorubicin (Dxr) (3.9 nM to 250 nM) and 4E1RCat (78.13 nM to 10 000 nM) at a constant ratio of 20:1 or 40:1. Twenty four hours later, perform an MTS assay: add Cell Proliferation Assay to the plates, incubate the plates for up to 3 h, then measure the OD490. Standardize the values to DMSO controls[1].
Animal Administration[1]
Mice[1] Inject lymphoma cells (secondary Pten+/-Eμ-Myc, Tsc2+/-Eμ-Myc, or Eμ-Myc; one million) via the tail vein into 6-8 week old female C57BL/6 mice. Once tumors are palpable, treat the mice with rapamycin (4 mg/kg; 5 d, daily) or 4E1RCat (15 mg/kg; 5 d, daily), or once with doxorubicin (10 mg/kg), delivering every compound by intraperitoneal (i.p.) injection in 5.2% PEG 400/ 5.2% Tween 80. In combination studies, inject rapamycin or 4E1RCat i.p. daily for five consecutive days and give doxorubicin once on day two. Palpate the animals daily to monitor tumor onset. Define tumor-free survival as the interval between disappearance and reappearance of tumors. Analyze the data with the log-rank test for statistical significance and present them in Kaplan-Meier format[1].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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eIF4F controls ERK MAPK signaling in melanomas with BRAF and NRAS mutations. Proc Natl Acad Sci U S A 2024 Oct 29;121(44):e2321305121. PMID: 39436655
Combination of PARP inhibitor and temozolomide to suppress chordoma progression. J Mol Med (Berl) 2019 Aug;97(8):1183-1193.
Salubrinal in Combination With 4E1RCat Synergistically Impairs Melanoma Development by Disrupting the Protein Synthetic Machinery. Front Oncol 2020 Jun 19:10:834. PMID: 32637352
Res Sq. 2026 Jun 5.