PROTAC ERRα Degrader-2 is a compound consisting of an MDM2 ligand binding group, a linker, and an estrogen-related receptor alpha (ERRα) binding group. This compound is designed to specifically degrade estrogen-related receptor alpha (ERRα), acting as an ERRα degrader[1].
(rel)-PROTAC ERRα Degrader-1 is a relative configuration of PROTAC ERRα Degrader-1, which is an estrogen-related receptor alpha (ERRa) degrader. PROTAC ERRα Degrader-1 consists of an MDM2 ligand binding moiety, a linker and an ERRa binding moiety [1].
PROTAC ERRα Degrader-3 is a highly effective and selective von Hippel-Lindau-based ligand that efficiently degrades the ERRα protein. At a concentration of 30 nM, this compound exhibits a remarkable degradation capability, reducing the ERRα protein levels by >80%. Importantly, PROTAC ERRα Degrader-3 shows no activity against the ERRβ and ERRγ proteins.
PROTAC_ERRalpha is a proteolysis targeting chimeras (PROTAC) which provides broad tissue distribution and knockdown of the targeted ERRalpha protein in tumor xenografts.