BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride

BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride incorporates a ligand for PD-1/PD-L1 immune checkpoint, and a PROTAC linker. BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride can be used in the synthesis of PD-1/PD-L1 degrader-1.html" class="link-product" target="_blank">PROTAC PD-1/PD-L1 degrader-1 (HY-131183). PROTAC PD-1/PD-L1 degrader-1 inhibits PD-1/PD-L1 interaction with an IC50 of 39.2 nM[1].

Research Areas >> Cancer

PROTAC 包含两个不同的配体，通过一个接头连接；一个是 E3 泛素连接酶的配体，另一个是靶蛋白的配体。PROTAC 利用细胞内泛素-蛋白酶体系统选择性降解靶蛋白[1]。

[1]. Cheng B, Ren Y, Cao H, Chen J. Discovery of novel resorcinol diphenyl ether-based PROTAC-like molecules as dual inhibitors and degraders of PD-L1. Eur J Med Chem. 2020;199:112377.