NRX-252114 is a potent enhancer of the interaction between β-catenin , and its cognate E3 ligase , SCF β-TrCP . NRX-252114 enhances the binding of pSer33/S37A β-catenin peptide for β-TrCP with an EC 50 of 6.5 nM and a K d of 0.4 nM. NRX-252114 induces mutant β-catenin degradation 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:EC50: 6.5 nM (β-catenin:β-TrCP Interaction), Kd: 0.4 nM (β-catenin:β-TrCP Interaction)
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NRX-252114
CAS number：2763260-39-3 molecular formula：C22H12Cl2F3N3O2S
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| Chinese alias | - | ||
| English alias | - | ||
| CAS number | 2763260-39-3 | molecular formula | C22H12Cl2F3N3O2S |
| molecular weight | 510.32 g/mol | Exact mass | ≥99% |
| PSA | - | logp | - |
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