eif4e in 2

eIF4E-IN-2 is a highly effective inhibitor of eukaryotic initiation factor 4e (eIF4e). This compound exhibits significant potential in the investigation of eIF4e dependent diseases, particularly in the context of cancer research.

(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].

Tomivosertib, also known as eFT508 is a MNK1 2 inhibitor. Tomivosertib binds to and inhibits the activity of MNK1 and 2. This prevents MNK1 2-mediated signaling, and inhibits the phosphorylation of certain regulatory proteins, including eukaryotic translation initiation factor 4E (eIF4E), that regulate the translation of messenger RNAs (mRNAs) involved in tumor cell proliferation, angiogenesis, survival and immune signaling.

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].

MNK1 2-IN-7 (compound 20j) serves as an orally administered inhibitor targeting MNK1 2, known for its anticancer properties and hERG safety. It also blocks the phosphorylation of eIF4E, thereby disrupting the MNK eIF4E signaling pathway and reducing cancer cell growth. Additionally, MNK1 2-IN-7 synergizes effectively with Ibrutinib. [15] [1]