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| Cas No.: | 2763260-39-3 |
| Chemical Name: | NRX-252114 |
| Synonyms: | 1H-Isoindole-4-carbonitrile, 2-[[4-[(2,6-dichlorophenyl)thio]-1,2-dihydro-2-oxo-6-(trifluoromethyl)-3-pyridinyl]carbonyl]-2,3-dihydro-;NRX-252114 |
| SMILES: | C1C2=C(C(C#N)=CC=C2)CN1C(C1=C(SC2=C(Cl)C=CC=C2Cl)C=C(C(F)(F)F)NC1=O)=O |
| Formula: | C22H12Cl2F3N3O2S |
| M.Wt: | 510.31579208374 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | NRX-252114 is a potent enhancer of the interaction between β-catenin, and its cognate E3 ligase, SCFβ-TrCP. NRX-252114 enhances the binding of pSer33/S37A β-catenin peptide for β-TrCP with an EC50 of 6.5 nM and a Kd of 0.4 nM. NRX-252114 induces mutant β-catenin degradation. |
| Target: | EC50: 6.5 nM (β-catenin:β-TrCP Interaction) Kd: 0.4 nM (β-catenin:β-TrCP Interaction) |
| In Vitro: | NRX-252114 (20 μM) enhances the binding of pSer33/S37A β-catenin peptide for β-TrCP, with more than 1500-fold co-operativity. NRX-252114 (0-25 μM) increases the ubiquitylation of pSer33/S37A β-catenin peptide to form long ubiquitin chains. NRX-252114 (0-25 μM) enhances the ubiquitylation of S33E/S37A β-catenin protein, as well as unphosphorylated Ser33/S37A β-catenin peptides. NRX-252114 (20 μM, 6 h) results in robust S33E/S37A β-catenin:β-TrCP interaction in the transfected HEK293T cells. |