1801547-15-8
Chemical Structure
PROTAC_ERRα
- CAS No.: 1801547-15-8
- Formula:C46H47F3N6O9S2
- Molecular Weight:949.03
IUPAC Name: 4-(((5-methoxy-2-(3,4,5-trimethoxyphenyl)chroman-7-yl)oxy)methyl)-1-(4-(trifluoromethyl)benzyl)-1H-1,2,3-triazole
InChIKey: IIJORMBEWMYDEN-FRKKMCEPSA-N
SMILES: O=C(/C(SC1=O)=C/C2=CC(OC)=C(C=C2)OC3=C(C=C(C=C3)C#N)C(F)(F)F)N1CCOCCC(N[C@@H](C(C)(C)C)C(N4[C@@H](C[C@H](C4)O)C(NCC5=CC=C(C6=C(N=CS6)C)C=C5)=O)=O)=O
Biological Activity: PROTAC_ERRα is a potent and selective ERRα PROTAC degrader (DC50: ~100 nM in MCF-7 cells). PROTAC_ERRα recruits the VHL E3 ubiquitin ligase to ERRα, inducing ERRα ubiquitination and proteasomal degradation in a VHL-dependent manner. PROTAC_ERRα can be used in breast cancer-related research[1][2][3].
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PROTAC_ERRα | 99.71% | PROTAC_ERRα is a potent and selective ERRα PROTAC degrader (DC50: ~100 nM in MCF-7 cells). PROTAC_ERRα recruits the VHL E3 ubiquitin ligase to ERRα, inducing ERRα ubiquitination and proteasomal degradation in a VHL-dependent manner. PROTAC_ERRα can be used in breast cancer-related research. | ||||||||||||||||||||
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- [1]. Bondeson DP, et al. Catalytic in vivo protein knockdown by small-molecule PROTACs. Nature chemical biology. 2015 Aug;11(8):611-7. [Content Brief]
- [2]. Gu S, et al. PROTACs: An Emerging Targeting Technique for Protein Degradation in Drug Discovery. Bioessays. 2018 Apr;40(4):e1700247. [Content Brief]
- [3]. Coleman K G, et al. Proteolysis-targeting chimeras: harnessing the ubiquitin-proteasome system to induce degradation of specific target proteins[J]. Annual Review of Cancer Biology, 2018, 2: 41-58.
Keywords
