1818314-88-3

BMS-1166 is a potent PD-1/PD-L1 immune checkpoint inhibitor. BMS-1166 induces dimerization of PD-L1 and blocks its interaction with PD-1, with an IC50 of 1.4 nM. BMS-1166 antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation[1][2].

BMS-1166 is a novel and potent inhibitor of PD-1/PD-L1 interaction with IC50 of 1.4 nM.

BMS-1166 had low toxicity to the tested cell lines and prevented the interaction of soluble PD-L1 with PD-1 receptors expressed on the cell surface. It attenuates the inhibitory effect of PD-L1 on T cell receptor-mediated T lymphocyte activation.

Target	Value
PD-1/PD-L1 interaction ()	1.4 nM

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[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. DOI:10.1021/acs.jmedchem.7b00293
[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. DOI:10.18632/oncotarget.20050