NRX-252262

• CAT Number: I019391
• CAS Number: 2438637-61-5
• Molecular Formula: C23H17Cl2F3N2O4S
• Molecular Weight: 545.36
• Purity: ≥95%
• Synonyms: 4-(2,6-dichlorophenyl)sulfanyl-3-(5,6-dimethoxy-1,3-dihydroisoindole-2-carbonyl)-6-(trifluoromethyl)-1H-pyridin-2-one
• InChI: InChI=1S/C23H17Cl2F3N2O4S/c1-33-15-6-11-9-30(10-12(11)7-16(15)34-2)22(32)19-17(8-18(23(26,27)28)29-21(19)31)35-20-13(24)4-3-5-14(20)25/h3-8H,9-10H2,1-2H3,(H,29,31)
• InChIKey: SPAYLOCXFWJEBL-UHFFFAOYSA-N
• SMILES: COC1=C(C=C2CN(CC2=C1)C(=O)C3=C(C=C(NC3=O)C(F)(F)F)SC4=C(C=CC=C4Cl)Cl)OC

NRX-252262 is a potent enhancer of the interaction between β-Catenin, and its cognate E3 ligase, SCFβ-TrCP, induces mutant β-catenin degradation, with an EC50 of 3.8 nM[1].
NRX-252262 (35 μM) causes S33E/S37A mutant β-catenin degradation in cells[1].

Reference

[1]. Kyle R. Simonetta, et al. Prospective discovery of small molecule enhancers of an E3 ligase-substrate interaction. Nature Communications. 2019 March.