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- PD-1/PD-L1
- BMS-1166-N-piperidine-COOH
BMS-1166-N-piperidine-COOH
BMS-1166-N-piperidine-COOH，以 BMS-1166 为基础结构，通过一个 linker 与 E3 连接酶配体结合形成 PROTAC PD-1/PD-L1 degrader-1 来降解 PD-1/PD-L1。BMS-1166 是 PD-1/PD-L1 相互作用的有效抑制剂，其 IC50 值为 1.4 nM。BMS-1166 可拮抗 PD-1/PD-L1 免疫检查点对 T 细胞活化的抑制作用。$
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包装价格促销价数量
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5mg￥6475.005180.00- +
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10mg￥11337.009070.00- +
- 货号: ajcx35874
- CAS: 2447066-00-2
- 别名:
- 分子式: C37H35ClN2O6
- 分子量: 639.14
- 纯度: ＞98%
- 溶解度:
- 储存: Store at -20°C, sealed storage, away from moisture and light
- 库存: 现货
Background
BMS-1166-N-piperidine-COOH, the BMS-1166-based moiety, binds to E3 ligase ligand via a linker to form PROTAC PD-1/PD-L1 degrader-1 to degrade PD-1/PD-L1[1]. BMS-1166 is a potent PD-1/PD-L1 interaction inhibitor with an IC50 of 1.4 nM. BMS-1166 antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation[2].
[1]. Binbin Cheng, et al. Discovery of Novel Resorcinol Diphenyl Ether-Based PROTAC-like Molecules as Dual Inhibitors and Degraders of PD-L1. Eur J Med Chem. 2020 Aug 1;199:112377.
[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.
