NRX-2663 

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 EC₅₀ of 22.9 μM and a K_d of 54.8 nM^[1].

EC50: 22.9 µM (β-catenin:β-TrCP Interaction)^[1]
Kd: 54.8 nM (β-catenin:β-TrCP Interaction)^[1]

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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

418.32

C₂₀H₁₃F₃N₂O₅

2763260-34-8

Solid

White to light yellow

OC(C1=CC=CC(NC(C2=C(C=C(NC2=O)C(F)(F)F)OC3=CC=CC=C3)=O)=C1)=O

Room temperature in continental US; may vary elsewhere.

• [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.  [Content Brief]