NRX-2663 is an enhancer of the interaction between β-catenin, and its cognate E3 ligase, SCFβ-TrCP. NRX-2663 enhances the binding of β-catenin peptide for β-TrCP with an EC50 of 22.9 µM and a Kd of 54.8 nM.

Product information

Molecular Weight: 418.32

Formula: C20H13F3N2O5

Chemical Name: 3-[2-oxo-4-phenoxy-6-(trifluoromethyl)-1,2-dihydropyridine-3-amido]benzoic acid

Smiles: OC(=O)C1C=C(C=CC=1)NC(=O)C1=C(C=C(NC1=O)C(F)(F)F)OC1C=CC=CC=1

InChiKey: QMARDTCIJVODCK-UHFFFAOYSA-N

InChi: InChI=1S/C20H13F3N2O5/c21-20(22,23)15-10-14(30-13-7-2-1-3-8-13)16(18(27)25-15)17(26)24-12-6-4-5-11(9-12)19(28)29/h1-10H,(H,24,26)(H,25,27)(H,28,29)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

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.

Products are for research use only. Not for human use.