PD-1/PD-L1 抑制剂;PD-1/PD-L1 Inhibitors;;InformationBMS-1166 BMS-1166 is a novel and potent small molecule inhibitor of the PD-1/PD-L1 interaction with an IC50 of 1.4 nM.TargetsPD-1/PD-L1 interaction 1.4 nMIn vitroBMS-1166 presents low toxicity towards tested cell lines and blocks the interaction of soluble PD-L1 with the cell surface-expressed PD-1. BMS-1166 alleviates the inhibitory effect of the soluble PD-L1 on the T-cell receptor-mediated activation of T-lymphocytes.
靶点:
IC50: 1.4 nM (PD-1/PD-L1 interaction).
参考文献:
1. Guzik K, et al. Small-Molecule Inhibitors of the Programmed Cell Death-1/Programmed Death-Ligand 1 (PD-1/PD-L1) Interaction via Transiently Induced Protein States and Dimerization of PD-L1. J Med Chem. 2017 Jul 13;60(13):5857-5867. 2. Skalniak L, et al. Small-molecule inhibitors of PD-1/PD-L1 immune checkpoint alleviate the PD-L1-induced exhaustion of T-cells. Oncotarget. 2017 Aug 7;8(42):72167-72181.