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.

(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.

m7GTP sodium(7-甲基-鸟苷-5'-三磷酸钠盐)是mRNA帽结构类似物，通过结合eIF4E（真核翻译起始因子）抑制体外蛋白质合成，常用于研究mRNA参与的蛋白质合成。

eIF4E-IN-5（Compound 6n）为细胞渗透性eIF4E抑制剂，能与加帽mRNA结合，从而抑制帽依赖性翻译。

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。