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1801547-15-8

1801547-15-8 structure
1801547-15-8 structure
  • Name: PROTAC_ERRα
  • Chemical Name: PROTAC_ERRα
  • CAS Number: 1801547-15-8
  • Molecular Formula: C46H47F3N6O9S2
  • Molecular Weight: 949.03
  • Catalog: Signaling Pathways Epigenetics Epigenetic Reader Domain
  • Create Date: 2022-08-11 17:42:13
  • Modify Date: 2024-01-15 23:38:14
  • 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].

Name PROTAC_ERRα
Description 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].
Related Catalog
In Vitro 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%.
In Vivo 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.
References

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

Molecular Formula C46H47F3N6O9S2
Molecular Weight 949.03