BMS-1166 is a potent PD-1/PD-L1 immune checkpoint inhibitor. BMS-1166 induces PD-L1 dimerisation and blocks its interaction with PD-1 with an IC50 of 1.4 nM. BMS-1166 antagonises the inhibitory effect of PD-1/PD-L1 immune checkpoints on T-cell activation[1][2].BMS-1166 is a potent PD-1/PD-L1 interaction inhibitor with an IC50 of 1.4 nM in homogenous time-resolved fluorescence binding assay[1].BMS-1166 antagonises the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation. BMS-1166 dose-dependently abrogates the inhibitory effect of sPD-L1 on EC stimulation[2].
BMS-1166 细胞实验
Cell Line
Concentration
Treated Time
Description
References
MDA-MB-231
10 μM
48 hours
To evaluate the inhibitory effect of BMS-1166 and BMS-T7 on PD-L1 expression in MDA-MB-231 cells. Results showed that BMS-T7 was more effective than the naked drug in inhibiting PD-L1 expression.
Int J Nanomedicine. 2025 Jan 8;20:293-308.
Human pluripotent stem cell-derived macrophages
500 nM or 1 µM
around two weeks
BMS-1166 reduced the percentage of CD45+CD11B+ macrophages, phenocopying the effect of PD-L1 knockout.
Life Sci Alliance. 2023 Nov 10;7(2):e202302461.
Jurkat T-lymphocytes
40.5 µM
48 hours
Assessed the toxicity of BMS-1166 on Jurkat T cells, showing low toxicity.
Oncotarget. 2017 Aug 7;8(42):72167-72181.
H1975
10 μM
17 hours
BMS1166 altered the glycosylation pattern of PD-L1 in H1975 cells.
Oncoimmunology. 2020 Oct 14;9(1):1831153.
Jurkat/PD-1
10 μM
17 hours
BMS1166 inhibited PD-L1/PD-1 signaling and restored effector T cell function.
Oncoimmunology. 2020 Oct 14;9(1):1831153.
PC9/PD-L1
10 μM
17 hours
BMS1166 partially inhibited N-glycosylation of PD-L1 and prevented the transport of under-glycosylated PD-L1 from the endoplasmic reticulum (ER) to the Golgi, leading to accumulation of PD-L1 in the ER.
Oncoimmunology. 2020 Oct 14;9(1):1831153.
SW480R cells
1 μM
24 hours
Evaluate the inhibitory effect of BMS-1166 on SW480R cell proliferation and migration, results showed that BMS-1166 inhibited cell proliferation and migration.
Int J Med Sci. 2024 Jul 9;21(10):1814-1823.
SW480 cells
0.5 μM
24 hours
Evaluate the inhibitory effect of BMS-1166 on SW480 cell proliferation and migration, results showed that BMS-1166 inhibited cell proliferation and migration.
Int J Med Sci. 2024 Jul 9;21(10):1814-1823.
BMS-1166 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
A53T-syn transgenic mice
In vitro culture
1 μM
Single treatment, 48 hours
To evaluate the reversal effect of BMS-1166 on T cell suppression induced by A53T-syn sEVs, results showed that BMS-1166 significantly reversed the inhibitory effects of A53T-syn sEVs on cytokine production in CD4+ and CD8+ T cells
搜索
