BMS-1166-N-piperidine-COOH |
رقم الكتالوجGC63536 |
BMS-1166-N-piperidine-COOH ، الشق القائم على BMS-1166 ، يرتبط بـ E3 ligase عبر رابط لتشكيل PROTAC PD-1 / PD-L1 degrader-1 لتحطيم PD-1 / PD-L1BMS-1166 هو مثبط فعال لتفاعل PD-1 / PD-L1 مع IC من 1.4 نانومتريعادي BMS-1166 التأثير المثبط لنقطة التفتيش المناعية PD-1 / PD-L1 على تنشيط الخلايا التائية
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Cas No.: 2447066-00-2
Sample solution is provided at 25 µL, 10mM.
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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