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 (HY-131183) 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。
货号:ajcx35874
CAS:2447066-00-2
分子式:C37H35ClN2O6
分子量：639.14
溶解度:N/A
纯度：98%
存储：Store at -20°C
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 (HY-131183) 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.