Purity/Purification
98%
CAS
2306388-65-6
Solubility
<1mg/ml refers to the product slightly soluble or insoluble
In vitro
PROTAC ERRalpha Degrader-3 (compound 6c; 0.3 nM-10 uM; 4 hours) dose-dependently induces ERRalpha degradation with an efficacious dose as low as 3.0 nM at 4.0 h. PROTAC ERRalpha Degrader-3 potently decreases protein levels of ERRalpha 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 ERRalpha Degrader-3 exhibits an IC 50 value of 12.67 nM to block the protein-protein interaction of ERRalpha with PGC-1alpha peptide and induces approximately 96% protein degradation at 100 nM (D100 nM) after 4.0 h treatment[1]. Western Blot Analysis[1]Cell Line: MDA-MB-231 cells Concentration: 0.3 nM, 1 nM, 3 nM, 10 nM, 30 nM, 100 nM, 300 nM, 1 uM, 3 uM, 10 uM Incubation Time: 4 hours. Result: Dose-dependently induced ERRalpha degradation.
Preparation and Storage
Powder: -20 degree C for 3 years
In solvent: -80 degree C for 2 years
In solvent: -80 degree C for 2 years
Related Product Information for PROTAC ERRalpha Degrader-3 biochemical
PROTAC ERRalpha Degrader-3 is a potent and selective ERRalpha degrader based on von Hippel-Lindau ligand. PROTAC ERRalpha Degrader-3 is capable of specifically degrading ERRalpha protein by 80% at a concentration of 30 nM. PROTAC ERRalpha Degrader-3 is inactive against ERRbeta and ERRgamma proteins.
References
1. Dietrich JD, et al. Development of Orally Efficacious Allosteric Inhibitors of TNFalpha via Fragment-Based Drug Design. J Med Chem. 2021 Jan 14;64(1):417-429.
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Product Notes
The PROTAC ERRalpha Degrader-3 (Catalog #AAA228310) is a Biochemical and is intended for research purposes only. The product is available for immediate purchase. It is sometimes possible for the material contained within the vial of "PROTAC ERRalpha Degrader-3, Biochemical" to become dispersed throughout the inside of the vial, particularly around the seal of said vial, during shipment and storage. We always suggest centrifuging these vials to consolidate all of the liquid away from the lid and to the bottom of the vial prior to opening. Please be advised that certain products may require dry ice for shipping and that, if this is the case, an additional dry ice fee may also be required.Precautions
All products in the AAA Biotech catalog are strictly for research-use only, and are absolutely not suitable for use in any sort of medical, therapeutic, prophylactic, in-vivo, or diagnostic capacity. By purchasing a product from AAA Biotech, you are explicitly certifying that said products will be properly tested and used in line with industry standard. AAA Biotech and its authorized distribution partners reserve the right to refuse to fulfill any order if we have any indication that a purchaser may be intending to use a product outside of our accepted criteria.Disclaimer
Though we do strive to guarantee the information represented in this datasheet, AAA Biotech cannot be held responsible for any oversights or imprecisions. AAA Biotech reserves the right to adjust any aspect of this datasheet at any time and without notice. It is the responsibility of the customer to inform AAA Biotech of any product performance issues observed or experienced within 30 days of receipt of said product. To see additional details on this or any of our other policies, please see our Terms & Conditions page.Item has been added to Shopping Cart
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