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Chemical Structure : NRX-252114
CAS No.: 2763260-39-3
Catalog No.: PC-36151Not For Human Use, Lab Use Only.
NRX-252114 (NRX 252114, NRX252114) is a potent, small molecule β-TrCP-based degrader of β-catenin, potentiates pSer33/S37A β-catenin binding and ubiquitylation (EC50=6.5 nM).
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NRX-252114 (NRX 252114, NRX252114) is a potent, small molecule β-TrCP-based degrader of β-catenin, potentiates pSer33/S37A β-catenin binding and ubiquitylation (EC50=6.5 nM).
NRX-252114 enhances the binding of pSer33/S37A β-catenin peptide for β-TrCP with >1500-fold cooperativity, surpassing the affinity of WT doublyphosphorylated peptide in vitro, induces the degradation of an engineered mutant β-Catenin in a cellular system; inserts into a naturally occurring PPI interface, with contacts optimized for both the substrate and ligase within the same small molecule entity, which is distinct from PROTACs.
| M.Wt | 510.312 | |
| Formula | C22H12Cl2F3N3O2S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
2-(4-((2,6-dichlorophenyl)thio)-2-oxo-6-(trifluoromethyl)-1,2-dihydropyridine-3-carbonyl)isoindoline-4-carbonitrile |
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1. Simonetta KR, et al. Nat Commun. 2019 Mar 29;10(1):1402.
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