NRX-252114 (C09-1157-431)

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 degradationIn VitroNRX-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:SolidIC50& Target:EC50: 6.5 nM (β-catenin:β-TrCP Interaction), Kd: 0.4 nM (β-catenin:β-TrCP Interaction). Specification: 0.99 Molecular Formula: C22H12Cl2F3N3O2S Molecular Weight: 510.32