Biological Activity
VHL ligand 2 hydrochloride is a Ligand for E3 Ligase extracted from patent WO/2017/030814A1 compound example 202, used in PROTAC technology.
In Vitro
E3 ligase Ligand 1 is a VHL E3 ligase-binding ligand[1]. E3 ligase Ligand 1 is used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC. ARV-771, a small-molecule pan-BET degrader based on proteolysis-targeting chimera (PROTAC) technology, demonstrates dramatically improved efficacy in cellular models of castration-resistant prostate cancer (CRPC) as compared with BET inhibition[2].
In Vivo
No in vivo data are provided in the current product source. Contact us for further information.
Target
Ligand for E3 Ligase[1]
References & source
[1]. WO/2017/030814A1
[2]. Kanak R, et al. PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer. Proceedings of the National Academy of Sciences of the United States of America (2016), 113(26), 7124-7129
Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.











