Thalidomide -piperazine hydrochloride is a synthetic E3 ligase ligand-linker conjugate, containing a cereblon ligand based on Thalidomide and one linker. Thalidomide -piperazine hydrochloride can be used in studies related to PROTAC synthesis [1] [2] [3].
In Vitro, Thalidomide-piperazine hydrochloride (a derived PROTAC) induces dose-dependent IDO1 degradation and kynurenine inhibition in KNS-42, PC-3, MDA-MB-231, SW-1990 and SKOV-3 cells[3].
References:
[1]. Wang H, et al. Degradation of androgen receptor (ar) by conjugation of ar antagonists with e3 ligase ligand and methods of use. WO2021058017A1, 2021.
[2]. Fischer ES, et al. Structure of the DDB1-CRBN E3 ubiquitin ligase in complex with thalidomide. Nature. 2014;512(7512):49-53.
[3]. Monsen PJ, et al. Rational Design and Optimization of a Potent IDO1 Proteolysis Targeting Chimera (PROTAC). J Med Chem. 2025;68(4):4961-4987.
In Vitro, Thalidomide-piperazine hydrochloride (a derived PROTAC) induces dose-dependent IDO1 degradation and kynurenine inhibition in KNS-42, PC-3, MDA-MB-231, SW-1990 and SKOV-3 cells[3].
References:
[1]. Wang H, et al. Degradation of androgen receptor (ar) by conjugation of ar antagonists with e3 ligase ligand and methods of use. WO2021058017A1, 2021.
[2]. Fischer ES, et al. Structure of the DDB1-CRBN E3 ubiquitin ligase in complex with thalidomide. Nature. 2014;512(7512):49-53.
[3]. Monsen PJ, et al. Rational Design and Optimization of a Potent IDO1 Proteolysis Targeting Chimera (PROTAC). J Med Chem. 2025;68(4):4961-4987.