Drug intelligence / Profile preview

4E1RCat

Development stage
Preclinical
Modality
Small Molecules
Administration
Intraperitoneal
01

Overview

4E1RCat is a synthetic small-molecule inhibitor of the eukaryotic translation initiation factor eIF4E that disrupts its interactions with both eIF4G and the repressor protein 4E‑BP1, thereby preventing assembly of the eIF4F complex and selectively inhibiting cap‑dependent translation initiation.[1][3][4][7][9] By binding to eIF4E at the site used by eIF4G and 4E‑BP1, 4E1RCat reduces 80S ribosome formation on capped mRNAs, decreases protein synthesis, and downregulates oncogenic and pro‑survival proteins such as c‑Myc and Mcl‑1, which can reverse chemoresistance and enhance the antitumor efficacy of agents like doxorubicin in Myc‑driven lymphoma models.[1][7][9] It is widely used as an experimental research tool (not a marketed therapeutic) to probe translational control, chemosensitization, and eIF4E‑dependent signaling, and is supplied by multiple chemical vendors for in vitro and in vivo studies.[1][3][4][6][8][10][11][12]

Other names
4-[(3Z)-3-[[5-(4-nitrophenyl)furan-2-yl]methylidene]-2-oxo-5-phenylpyrrol-1-yl]benzoic acid(Z)-4-(3-((5-(4-nitrophenyl)furan-2-yl)methylene)-2-oxo-5-phenyl-2,3-dihydro-1H-pyrrol-1-yl)benzoic acidbenzoic acid, 4-[2,3-dihydro-3-[[5-(4-nitrophenyl)-2-furanyl]methylene]-2-oxo-5-phenyl-1H-pyrrol-1-yl]
02

Targets

Eukaryotic translation initiation factor 4E:Eukaryotic translation initiation factor 4 gamma protein-protein interactionEIF4EBP1

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