PROTAC ERRα Degrader-3 |
カタログ番号GC62307 |
PROTAC ERRα Degrader-3 は強力で選択的な ERRα です。 von Hippel-Lindau 配位子に基づく分解剤。 PROTAC ERRα Degrader-3 は、ERRα を特異的に分解することができます。 30 nM の濃度で >80% のタンパク質。 PROTAC ERRα Degrader-3 は ERRβ に対して非アクティブです。 ERRγタンパク質。
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Cas No.: 2306388-65-6
Sample solution is provided at 25 µL, 10mM.
PROTAC ERRα Degrader-3 is a potent and selective ERRα degrader based on PROTAC. 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[1].
PROTAC ERRα Degrader-3 (compound 6c; 0.3 nM-10 μM; 4 hours) dose-dependently induces ERRα degradation with an efficacious dose as low as 3.0 nM at 4.0 h. PROTAC ERRα Degrader-3 potently decreases protein levels of ERRα downstream target genes, e.g., ATP5B, medium-chain acyl CoA dehydrogenase (MCAD), and pyruvate dehydrogenase kinase 4 (PDK4) in the MDA-MB-231 cells after a 24 h treatment[1].PROTAC ERRα Degrader-3 exhibits an IC50 value of 12.67 nM to block the protein-protein interaction of ERRα with PGC-1α peptide and induces approximately 96% protein degradation at 100 nM (D100 nM) after 4.0 h treatment[1].
[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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