4E1RCat

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.

4E1RCat was used to inhibit new protein synthesis in transformed primary chicken embryo fibroblasts.

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.

eIF4

[1] REGINA CENCIC. Reversing chemoresistance by small molecule inhibition of the translation initiation complex eIF4F.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2011, 108 3: 1046-1051. DOI: 10.1073/pnas.1011477108