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PROTAC ERRα Degrader-3

Catalog No. T39837   CAS 2306388-65-6

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.

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PROTAC ERRα Degrader-3 Chemical Structure
PROTAC ERRα Degrader-3, CAS 2306388-65-6
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5 mg Inquiry $ 249.00
10 mg Inquiry $ 398.00
25 mg Inquiry $ 788.00
50 mg Inquiry $ 1,190.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description 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.
In vitro PROTAC ERRα Degrader-3 (compound 6c; 0.3 nM-10 μM; 4 hours) effectively induces the degradation of ERRα in a dose-dependent manner, achieving significant degradation with doses as low as 3.0 nM within 4 hours. This compound also significantly reduces the levels of ERRα downstream target genes, such as ATP5B, medium-chain acyl CoA dehydrogenase (MCAD), and pyruvate dehydrogenase kinase 4 (PDK4), in MDA-MB-231 cells following 24 hours of exposure. Furthermore, PROTAC ERRα Degrader-3 disrupts the protein-protein interaction between ERRα and the PGC-1α peptide, marked by an IC50 of 12.67 nM, and induces approximately 96% degradation of the ERRα protein at a concentration of 100 nM after 4 hours. Western Blot analysis in MDA-MB-231 cells across a range of concentrations (0.3 nM to 10 μM) and a 4-hour incubation period corroborates the dose-dependent mechanism of ERRα degradation.
Molecular Weight 957.0
Formula C47H50F6N6O7S
CAS No. 2306388-65-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

1. Lijie Peng, et al. Identification of New Small-Molecule Inducers of Estrogen-related Receptor α (ERRα) Degradation. ACS Med Chem Lett. 2019 Apr 12;10(5):767-772.

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Keywords

PROTAC ERRα Degrader-3 2306388-65-6 PROTAC ERRalpha Degrader-3 PROTAC ERRα Degrader3 PROTAC ERRα Degrader 3 PROTAC ERRa Degrader-3 inhibitor inhibit

 

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