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Beschreibung

A cell-permeable oxopyrrolyl benzoate compound that blocks the assembly of eukaryotic translation initiation factor (eIF) 4F complex (eIF4F) as well as disrupts preformed eIF4F by competing against eIF4G for eIF4E binding. Specifically blocks cap-dependent, but not cap-independent, protein translations in cell-free translation assays and inhibits protein, but not DNA or RNA, synthesis in MDA-MB-231 and HeLa cultures (50 µ,M) in a reversible manner. Although not effective when administered alone (15 mg/kg, i.p. daily for 5 days), 4E1RCat is shown to significantly prolong Pten+/-Eµ,-myc and Tsc+/-Eµ,-myc, but not Eµ,-myc, tumor remission time when combined with Doxorubicin (Cat. No. 324380) treatment (10 mg/kg, i.p. once on day 2) in mice in vivo. Unlike 4EGI-1 (Cat. No. 324517), 4E1RCat also blocks eIF4E and 4E-BP1 interaction., A cell-permeable oxopyrrolyl benzoate compound that blocks the assembly of eukaryotic translation initiation factor (eIF) 4F complex (eIF4F) as well as disrupts preformed eIF4F by competing against eIF4G for eIF4E binding. Specifically blocks cap-dependent, but not cap-independent, protein translations in cell-free translation assays and inhibits protein, but not DNA or RNA, synthesis in MDA-MB-231 and HeLa cultures (50 µ,M) in a reversible manner. Although not effective when administered alone (15 mg/kg, i.p. daily for 5 days), 4E1RCat is shown to significantly prolong Pten+/-Eµ,-myc and Tsc+/-Eµ,-myc, but not Eµ,-myc, tumor remission time when combined with Doxorubicin (Cat. No. 324380) treatment (10 mg/kg, i.p. once on day 2) in mice in vivo. Unlike 4EGI-1 (Cat. No. 324517), 4E1RCat also blocks eIF4E and 4E-BP1 interaction.