Identification | Back Directory | [Name]
4E1RCat | [CAS]
328998-25-0 | [Synonyms]
4E1RCat CS-1228 4-[(3E)-3-[[5-(4-nitrophenyl)furan-2-yl]methylidene]-2-oxo-5-phenylpyrrol-1-yl]benzoic acid 4-[2,3-Dihydro-3-[[5-(4-nitrophenyl)-2-furanyl]methylene]-2-oxo-5-phenyl-1H-pyrrol-1-yl]benzoic acid Benzoic acid, 4-[2,3-dihydro-3-[[5-(4-nitrophenyl)-2-furanyl]Methylene]-2-oxo-5-phenyl-1H-pyrrol-1-yl]- 4-[(3E)-3-[[5-(4-Nitrophenyl)furan-2-yl]methylidene]-2-oxo-5-phenyl-2,3-dihydro-1H-pyrrol-1-yl]benzoic acid | [Molecular Formula]
C28H18N2O6 | [MDL Number]
MFCD01931282 | [MOL File]
328998-25-0.mol | [Molecular Weight]
478.45 |
Hazard Information | Back Directory | [Description]
4E1RCat is an inhibitor of the eIF4F translation initiation complex that blocks eIF4E:eIF4G and eIF4E:4E-BP1 interactions. It has been shown to prevent the assembly of the eIF4F complex and to inhibit cap-dependent translation with an IC50 value of ~4 μM. 4E1RCat was shown to reverse tumor chemoresistance in a mouse model of lymphoma by sensitizing cells to the proapoptotic action of DNA damage. | [Uses]
4E1RCat was used to inhibit new protein synthesis in transformed primary chicken embryo fibroblasts. | [Biochem/physiol Actions]
4E1RCat ilnhibits the eIF4F translation initiation complex by binding to IF4E b and inhibiting the interaction between IF4E:eIF4G (IC50 = 3.2 μM). In in vitro translation experiments using MDA-MB-231 cells, 4E1RCat dose dependently inhibited cap-dependent translation, led to a decrease in polysome and 80S ribosomal subunits and reduced levels of the eIF4F-dependant proteins Mcl-1 and c-Myc. |
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