PROTAC ERRα Degrader-3 是一种基于 PROTAC 的强效选择性 ERRα 降解剂。PROTAC ERRα Degrader-3 能够在 30 nM 的浓度下将 ERRα 蛋白特异性降解 >80%。PROTAC ERRα Degrader-3 对 ERRβ 和 ERRγ 蛋白无活性。
货号:ajcx33464
CAS:2306388-65-6
分子式:C47H50F6N6O7S
分子量：956.99
溶解度:DMSO : 80 mg/mL (83.60 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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.