PD-1/PD-L1-IN-29

PD-1/PD-L1-IN-29 (S4-1) is a potent PD-1/PD-L1 inhibitor with an IC50 value of 6.1 nM. PD-1/PD-L1-IN-29 binds PD-L1 and disrupts PD-1/PD-L1 interactions, induces PD-L1 dimerization and internalization, improves its localization to the endoplasmic reticulum, and promotes PD-L1 entry into the endoplasmic reticulum. PD-1/PD-L1-IN-29 has anticancer activity[1].

Research Areas >> Cancer

Signaling Pathways >> Immunology/Inflammation >> PD-1/PD-L1

PD-1/PD-L1-IN-29(S4-1)(10 or 20 μM, 48 h) 可以通过阻断 PD-1/PD-L1 相互作用，恢复 PBMCs 的活化状态，增加 PBMCs 对A375 肿瘤细胞的细胞毒性，而对肿瘤细胞的直接杀伤作用很小[1]。

PD-1/PD-L1-IN-29(S4-1)(10 or 25 mg/kg, i.p., 12 days) 在 MC38 结直肠肿瘤小鼠模型中，可以显著抑制肿瘤的生长，低剂量组和高剂量组（10 和 25 mg/kg）均可观察到，且抑制率分别为 65.9% 和 88.8%[1]。

[1]. Chengliang Sun, et al. Novel Small-Molecule PD-L1 Inhibitor Induces PD-L1 Internalization and Optimizes the Immune Microenvironment. J Med Chem. 2022 Dec 29.