الصفحة الرئيسية>>Signaling Pathways>> PROTAC>> PROTAC and Building Blocks>>PROTAC ERRα Degrader-3

PROTAC ERRα Degrader-3

رقم الكتالوجGC62307

PROTAC ERRα ؛ Degrader-3 هو ERR&88#945 قوي وانتقائي ؛ degrader على أساس يجند فون هيبل لينداو. PROTAC ERRα ؛ Degrader-3 قادر على تحطيم ERRα على وجه التحديد ؛ البروتين بنسبة> 80٪ بتركيز 30 نانومتر. PROTAC ERRα ؛ Degrader-3 غير نشط مقابل ERRβ ؛ و ERRγ ؛ البروتينات.

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PROTAC ERRα Degrader-3 التركيب الكيميائي

Cas No.: 2306388-65-6

الحجم السعر المخزون الكميّة
5 mg
270٫00
متوفر
10 mg
432٫00
متوفر
25 mg
855٫00
متوفر
50 mg
1305٫00
متوفر

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مراجعات العميل

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Sample solution is provided at 25 µL, 10mM.

Description Chemical Properties Product Documents

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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