NRX-2663 is an enhancer of the interaction between β-catenin, and its cognate E3 ligase, SCF. 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.
NRX-2663 displays both improved potency in the binding assay with pSer33/Ser37 β-catenin (EC50?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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Kyle R Simonetta, et al. Prospective discovery of small molecule enhancers of an E3 ligase-substrate interaction. Nat Commun. 2019 Mar 29;10(1):1402.