ERRα Inhibitor

PROTAC ERRα Degrader-3 is a potent and selective ERRα degrader based on von Hippel-Lindau ligand. PROTAC ERRα Degrader-3 is capable of specifically degrading ERRα protein by >80% at a concentration of 30 nM. PROTAC ERRα Degrader-3 is inactive against ERRβ and ERRγ proteins.

Estrogen receptor-IN-2 is a potent estrogen receptor inhibitor formed by the conjugation of Tam (HY-13757)-NHC and gold (I). Estrogen receptor-IN-2 significantly downregulates estrogen receptor (ER) levels, inhibits ER-mediated downstream signaling pathways, and induces immunogenic cell death (ICD) mediated by damage-associated molecular patterns (DAMPs). Estrogen receptor-IN-2 can overcome drug resistance in MCF-7^Y537S mutant cells via the RAMP3/CALCR signaling pathway. It is suitable for research on endocrine-resistant breast cancer.

PROTAC ERRα Degrader-1 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRα Degrader-1 is an PROTAC estrogen-related receptor alpha (ERRa) degrader.