BMS-1166-N-piperidine-COOH |
| カタログ番号GC63536 |
BMS-1166ベースの部分であるBMS-1166-N-ピペリジン-COOHは、リンカーを介してE3リガーゼリガンドに結合し、PROTAC PD-1/PD-L1 degrader-1を形成してPD-1/PD-L1を分解します。 BMS-1166 は、1.4 nM の IC50 を持つ強力な PD-1/PD-L1 相互作用阻害剤です。 BMS-1166 は、T 細胞活性化に対する PD-1/PD-L1 免疫チェックポイントの阻害効果に拮抗します。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2447066-00-2
Sample solution is provided at 25 µL, 10mM.
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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.
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