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在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
NRX-2663 is an enhancer of the interaction between β-catenin , and its cognate E3 ligase , SCF β-TrCP . NRX-2663 enhances the binding of β-catenin peptide for β-TrCP with an EC 50 of 22.9 µM and a K d of 54.8 nM
In Vitro
NRX-2663 displays both improved potency in the binding assay with pSer33/Ser37 β-catenin (EC 50 of 80 µM) and cooperativity of binding (13-fold). NRX-2663 also markedly enhances the ubiquitylation of the pSer33/Ser37 β-catenin peptide, with ubiquitin chain formation at ligand concentrations of 16 μM and above resembling ubiquitin chain formation on wild-type pSer33/pSer37 β-catenin peptide. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Form:Solid
IC50& Target:EC50: 22.9 µM (β-catenin:β-TrCP Interaction), Kd: 54.8 nM (β-catenin:β-TrCP Interaction)