PROTAC ERRα Degrader-3

PROTAC ERRα 降解剂-3

PROTAC ERRα Degrader-3

P656295-1ml

1ml

10mM in DMSO

-80℃储存

超低温冰袋运输

PROTAC ERRα Degrader-3 is a potent and selective ERRα degrader based on von Hippel-Lindau ligand. 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 In Vitro 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. PROTAC ERRα Degrader-3 exhibits an IC 50 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: MDA-MB-231 cells Concentration: 0.3 nM, 1 nM, 3 nM, 10 nM, 30 nM, 100 nM, 300 nM, 1 μM, 3 μM, 10 μM Incubation Time: 4 hours Result: Dose-dependently induced ERRα degradation. IC50& Target:ERRα VHL

PROTAC ERRα 降解剂-3 是一种基于 von Hippel-Lindau 配体的强效、选择性 ERRα 降解剂。在 30 nM 的浓度下，PROTAC ERRα 降解剂-3 能够特异性降解 ERRα 蛋白，降解率大于 80%。PROTAC ERRα 降解剂-3 对ERRβ没有活性。

2306388-65-6(DMSO)

C47H50F6N6O7S

956.99 g/mol

COC(C=C1/C=C(C#N)/C(NCCCCC(N[C@@H](C(C)(C)C)C(N2[C@@H](C[C@H](C2)O)C(NCC3=CC=C(C4=C(C)N=CS4)C=C3)=O)=O)=O)=O)=C(C=C1)OCC5=C(C=C(C=C5)C(F)(F)F)C(F)(F)F