Description
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.
Product information
CAS Number: 2306388-65-6
Molecular Weight: 956.99
Formula: C47H50F6N6O7S
Chemical Name: (2S, 4R)-1-[(2S)-2-{5-[(2E)-3-(4-{[2, 4-bis(trifluoromethyl)phenyl]methoxy}-3-methoxyphenyl)-2-cyanoprop-2-enamido]pentanamido}-3, 3-dimethylbutanoyl]-4-hydroxy-N-{[4-(4-methyl-1, 3-thiazol-5-yl)phenyl]methyl}pyrrolidine-2-carboxamide
Smiles: CC(C)(C)[C@H](NC(=O)CCCCNC(=O)/C(=C/C1=CC=C(OCC2=CC=C(C=C2C(F)(F)F)C(F)(F)F)C(=C1)OC)/C#N)C(=O)N1C[C@H](O)C[C@H]1C(=O)NCC1=CC=C(C=C1)C1SC=NC=1C
InChiKey: POTUUCUOBIVSIX-BDUCEWPUSA-N
InChi: InChI=1S/C47H50F6N6O7S/c1-27-40(67-26-57-27)30-12-9-28(10-13-30)23-56-43(63)36-21-34(60)24-59(36)44(64)41(45(2,3)4)58-39(61)8-6-7-17-55-42(62)32(22-54)18-29-11-16-37(38(19-29)65-5)66-25-31-14-15-33(46(48,49)50)20-35(31)47(51,52)53/h9-16,18-20,26,34,36,41,60H,6-8,17,21,23-25H2,1-5H3,(H,55,62)(H,56,63)(H,58,61)/b32-18+/t34-,36+,41-/m1/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 80 mg/mL (83.60 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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 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.
Products are for research use only. Not for human use.
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