PROTAC_ERRα

PROTAC_ERRα is a potent and selective ERRα degrader. PROTAC_ERRα induces proteasomal degradation and has capable of specifically degrading ERRα protein by >80%[1].

Research Areas >> Cancer

Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain

PROTAC_ERRα (0-1000 nM; 8 hours; MCF7 cells) down-regulates ERRα protein levels in a dose-dependent fashion[1]. PROTAC_ERRα (100-500 nM; 4-24 hours; MCF7 cells) possesses good selectivity for ERRα target and decreases protein levels of ERRα downstream target genes[1]. Western Blot Analysis[1] Cell Line: MCF7 cells Concentration: 0, 10, 30, 100, 300 and 1000 nM Incubation Time: 8 hours Result: Decreased in ERRα level in a dose-dependent fashion and the maximal level of degradation (D50) is 86%.

PROTAC_ERRα (100 mg/kg; i.p.; every eight hours) degrades ERRα level in vivo[1]. Animal Model: Female CD-1 mice[1] Dosage: 100 mg/kg Administration: Intraperitoneal injection ; every eight hours. Result: Reduced ERRα levels in mouse heart and kidney and MDA-MB-231 tumors by approximately 44%, 44% and 39%, respectively.

[1]. Bondeson DP, et al. Catalytic in vivo protein knockdown by small-molecule PROTACs. Nat Chem Biol. 2015 Aug;11(8):611-7.