NRX-103094 是一种有效的 β-catenin 与 同源 E3 ligase SCF^β-TrCP 的相互作用增强剂，增强 pSer33/Ser37 β-catenin 与 β-TrCP 的结合，EC₅₀ 为 62 nM，K_d 为 0.6 nM。

NRX-103094 is a potent enhancer of the interaction between β-catenin, and its cognate E3 ligase, SCF. 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.

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EC50: 62 nM (β-catenin:β-TrCP Interaction)
Kd: 0.6 nM (β-catenin:β-TrCP Interaction)

NRX-103094 shows high potency with pSer33/Ser37 β-catenin peptide (EC50?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. has not independently confirmed the accuracy of these methods. They are for reference only.

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[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.