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 is the Z-isomer of 4EGI-1 and is an inhibitor of eIF4E eIF4G interaction and of translation initiation. (Z)-4EGI-1 effectively binds to eIF4E with an IC50 of 43.5 μM and a Kd value of 8.74 μM. (Z)-4EGI-1 has anticancer activity[1][2]. [1]. Khuloud Takrouri, et al. Structure-activity Relationship Study of 4EGI-1, Small Molecule eIF4E eIF4G Protein-Protein Interaction Inhibitors. Eur J Med Chem. 2014 Apr 22;77:361-77. [2]. Poornachandran Mahalingam, et al. Synthesis of Rigidified eIF4E eIF4G inhibitor-1 (4EGI-1) Mimetic and Their in Vitro Characterization as Inhibitors of Protein-Protein Interaction. J Med Chem. 2014 Jun 26;57(12):5094-111.

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（化合物4b）是一种针对eIF4E设计的抑制剂，可阻止其与cap mRNA的结合，其化学结构为GMP类似物。该化合物在Caco-2、HepG-2和MCF-7细胞系中显示出细胞毒性效果，其IC50值分别约为31、27和21 μM。

MNK1 2-IN-7（compound 20j）是一种口服有效的 MNK1 2 抑制剂，具有抗癌活性和 hERG 安全性。它还能抑制 eIF4E 的磷酸化，并阻断 MNK eIF4E 信号通路以及癌细胞增殖。MNK1 2-IN-7 与 Ibrutinib 显示出协同作用。