BMS-1001
目录号 : GC25160BMS-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.
Cas No.:2113650-03-4
Sample solution is provided at 25 µL, 10mM.
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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.
BMS-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.[1]
[1] Lukasz Skalniak, et al. Oncotarget. 2017 Aug 7;8(42):72167-72181.
Cas No. | 2113650-03-4 | SDF | Download SDF |
分子式 | C35H34N2O7 | 分子量 | 594.65 |
溶解度 | DMSO: 50 mg/mL (84.08 mM);Water: Insoluble;Ethanol: Insoluble | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg | |
1 mM | 1.6817 mL | 8.4083 mL | 16.8166 mL |
5 mM | 0.3363 mL | 1.6817 mL | 3.3633 mL |
10 mM | 0.1682 mL | 0.8408 mL | 1.6817 mL |
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2.
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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.PMID:29069777DOI:10.18632/oncotarget.20050.
Antibodies targeting the PD-1/PD-L1 immune checkpoint achieved spectacular success in anticancer therapy in the recent years. In contrast, no small molecules with cellular activity have been reported so far. Here we provide evidence that small molecules are capable of alleviating the PD-1/PD-L1 immune checkpoint-mediated exhaustion of Jurkat T-lymphocytes. The two optimized small-molecule inhibitors of the PD-1/PD-L1 interaction, BMS-1001 and BMS-1166, developed by Bristol-Myers Squibb, bind to human PD-L1 and block its interaction with PD-1, when tested on isolated proteins. The compounds present low toxicity towards tested cell lines and block the interaction of soluble PD-L1 with the cell surface-expressed PD-1. As a result, BMS-1001 and BMS-1166 alleviate the inhibitory effect of the soluble PD-L1 on the T-cell receptor-mediated activation of T-lymphocytes. Moreover, the compounds were effective in attenuating the inhibitory effect of the cell surface-associated PD-L1. We also determined the X-ray structures of the complexes of BMS-1001 and BMS-1166 with PD-L1, which revealed features that may be responsible for increased potency of the compounds compared to their predecessors. Further development may lead to the design of an anticancer therapy based on the orally delivered immune checkpoint inhibition.