eif4e in 1

eIF4E-IN-1 (WO2021003194A1, compound Y), is a highly effective inhibitor of eIF4E, a key protein involved in immunosuppression. By targeting immune checkpoint proteins such as PD-1, PD-L1, LAG3, TIM3, and IDO, eIF4E-IN-1 functions to disrupt immune suppression and promote immune release in specific diseases such as cancer and infectious diseases.

ROTACMNK1degrader-1 is a selective MNK1 PROTAC degrader with a DC50 of 11.92 nM and a Dmax greater than 96% in MV4-11 cells. It significantly reduces p-eIF4E levels with an IC50 of 22.07 nM, induces apoptosis, and causes cell cycle arrest at the G1 phase. This compound exhibits potent antitumor activity, demonstrating strong anti-leukemic effects in MV4-11 xenograft mouse models with acceptable drug safety.

(Z)-4EGI-1, the Z-isomer of 4EGI-1, serves as an inhibitor of both the eIF4E/eIF4G interaction and translation initiation. It effectively binds to eIF4E, exhibiting an IC50 of 43.5 μM and a Kd value of 8.74 μM. Notably, (Z)-4EGI-1 possesses anticancer activity[1][2].

m7GTP sodium (7-Methyl-guanosine-5'-triphosphate sodium) is a structural analog of the mRNA cap that inhibits protein synthesis in vitro by binding to eIF4E (eukaryotic translation initiation factor), and is commonly used to study protein synthesis involving mRNA.

eIF4E-IN-5 (Compound 6n) is a cell-permeable inhibitor of eIF4E that binds to capped mRNA, inhibiting cap-dependent translation [1].

eIF4E-IN-6 (Compound 4b), a GMP analog, is designed to inhibit the eIF4E protein's ability to bind to cap mRNA. It demonstrates cytotoxic effects on Caco-2, HepG-2, and MCF-7 cell lines with IC50 values of 31, 27, and 21 μM, respectively [1].