| Identification | Back Directory | [Name]
L-Prolinamide, N-[3-[2-[(5Z)-5-[[4-[4-cyano-2-(trifluoromethyl)phenoxy]-3-methoxyphenyl]methylene]-2,4-dioxo-3-thiazolidinyl]ethoxy]-1-oxopropyl]-3-methyl-L-valyl-4-hydroxy-N-[[4-(4-methyl-5-thiazolyl)phenyl]methyl]-, (4R)- | [CAS]
1801547-15-8 | [Synonyms]
PROTAC_ERRα
L-Prolinamide, N-[3-[2-[(5Z)-5-[[4-[4-cyano-2-(trifluoromethyl)phenoxy]-3-methoxyphenyl]methylene]-2,4-dioxo-3-thiazolidinyl]ethoxy]-1-oxopropyl]-3-methyl-L-valyl-4-hydroxy-N-[[4-(4-methyl-5-thiazolyl)phenyl]methyl]-, (4R)- | [Molecular Formula]
C46H47F3N6O9S2 | [MOL File]
1801547-15-8.mol | [Molecular Weight]
949.03 |
| Hazard Information | Back Directory | [Uses]
PROTAC_ERRα is a potent and selective ERRα PROTAC degrader (DC50: 100 nM in MCF-7 cells). PROTAC_ERRα induces proteasomal degradation and has capable of specifically degrading ERRα protein by >80%. Blue: VHL ligand (HY-125845), Pink: ERRα ligand (HY-U00425), black: linker[1]. | [in vivo]
PROTAC_ERRα (100 mg/kg; i.p.; every eight hours) degrades ERRα level in vivo[1]. | Animal Model: | Female CD-1 mice[1] | | Dosage: | 100 mg/kg | | Administration: | Intraperitoneal injection ; every eight hours. | | Result: | Reduced ERRα levels in mouse heart and kidney and MDA-MB-231 tumors by approximately 44%, 44% and 39%, respectively. |
| [References]
[1] Bondeson DP, et al. Catalytic in vivo protein knockdown by small-molecule PROTACs. Nat Chem Biol. 2015 Aug;11(8):611-7. DOI:10.1038/nchembio.1858 |
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