NRX-252262

SKU: orb1298303

Description

NRX-252262 is a small molecule that potently enhances the interaction between β-catenin and the SCFβ-TrCP E3 ligase, leading to targeted degradation of mutant β-catenin with an EC50 of 3.8 nM. It serves as a valuable chemical probe for studying Wnt/β-catenin signaling in cancer research and has demonstrated proof-of-concept efficacy in cellular models of oncogenesis.

Research Area

Metabolism Research, Pharmacology & Drug Discovery, Protein Biochemistry, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 2438637-61-5
• MW: 545.36
• Purity: 99.87% (May vary between batches)
• Formula: C₂₃H₁₇Cl₂F₃N₂O₄S
• SMILES: COc1cc2CN(Cc2cc1OC)C(=O)c1c(Sc2c(Cl)cccc2Cl)cc([nH]c1=O)C(F)(F)F
• Target: E1/E2/E3 Enzyme,Wnt/beta-catenin,Molecular Glues
• Solubility: DMSO:8 mg/mL (14.67 mM)

Bioactivity

• Target IC50:
  β-catenin/SCFβ-TrCP:3.8 nM (EC50)
• In Vitro:
  NRX-252262 also induces S33E/S37A mutant β-catenin degradation at an even lower concentration of ~35 μM

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Beta catenin, betacatenin, beta-catenin, bcatenin, Inhibitor, inhibit, NRX252262, NRX-252262, NRX 252262, SCF(β-TrCP)-E3 ligase, Wnt/β-catenin, Wnt, Wnt/b-catenin, Wnt/betacatenin, βcatenin, β-catenin

Compound Identifiers

PubChem CID

138319682