PD-1/PD-L1 抑制剂;PD-1/PD-L1 Inhibitors;中文介绍:BMS-1001 是一种有效的 PD-1/PD-L1 相互作用的抑制剂,EC50值为253 nM。BMS-1001 可减轻可溶性PD-L1对T细胞受体介导的T淋巴细胞活化的抑制作用。;InformationBMS-1001 BMS-1001 is a potent inhibitor of PD-1/PD-L1 interaction with EC50 of 253 nM. BMS-1001 alleviates the inhibitory effect of the soluble PD-L1 on the T-cell receptor-mediated activation of T-lymphocytes.TargetsPD-1/PD-L1 (Cell-free assay) 253 nM(EC50)In vitroBMS-1001 alleviates the inhibitory effect of the soluble PD-L1 on the T-cell receptor-mediated activation of T-lymphocytes. BMS-1001 is effective in attenuating the inhibitory effect of the cell surface-associated PD-L1.Cell Research(from reference)Cell lines:PD-L1+ aAPC/CHO-K1 cells (aAPCs), PD-1 Effector Cells (ECs) Concentrations:0.12 μM, 0.3 μM, 1.2 μM, 3 μM Incubation Time:24 h
参考文献:
1. 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. 2. 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.