NRX-103094

NRX-103094 is a potent enhancer of the interaction between β-catenin , and its cognate E3 ligase , SCF β-TrCP . NRX-103094 enhances the binding of pSer33/Ser37 β-catenin peptide for β-TrCP with an EC 50 of 62 nM and a K d of 0.6 nM In Vitro NRX-103094 shows high potency with pSer33/Ser37 β-catenin peptide (EC 50 of 457 nM). NRX-103094 potentiates the ubiquitylation of pSer33/S37A β-catenin peptide to levels greater than wild-type pSer33/pSer37 levels at 250 nM. NRX-103094 enhances the S33E/S37A phosphomimetic peptide binding affinity for β-TrCP from >5 μM in the absence of compound to 22 nM in the presence of 40 μM compound. In the presence of 20 μM NRX-103094, robust time-dependent ubiquitylation of S33E/S37A β-catenin peptide is observed. Likewise, the full-length S33E/S37A β-catenin protein is strongly ubiquitylated in the presence of 20 μM NRX-103094, with the ubiquitylation levels approaching that of WT full-length β-catenin protein. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:EC50: 62 nM (β-catenin:β-TrCP Interaction), Kd: 0.6 nM (β-catenin:β-TrCP Interaction)

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