NRX-252114

SKU: orb1686525

Description

NRX-252114 is a potent small molecule that enhances the interaction between mutant β-catenin (pSer33/S37A) and the E3 ubiquitin ligase SCFβ-TrCP, promoting targeted degradation with high affinity (Kd = 0.4 nM). This molecular glue has been utilized in vitro and in vivo to study Wnt/β-catenin signaling dysregulation in cancer models, offering a research tool for targeted protein degradation.

Research Area

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

Key Properties

• CAS Number: 2763260-39-3
• MW: 510.32
• Purity: 98.13% (May vary between batches)
• Formula: C₂₂H₁₂Cl₂F₃N₃O₂S
• SMILES: S(C1=C(C(=O)N2CC=3C(C2)=CC=CC3C#N)C(=O)NC(C(F)(F)F)=C1)C4=C(Cl)C=CC=C4Cl
• Target: Molecular Glues,Wnt/beta-catenin
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.92 mM);DMSO:50 mg/mL (97.98 mM)

Bioactivity

• Target IC50:
  β-catenin-β-TrCP:6.5 nM(EC50)|β-catenin-β-TrCP:0.4 nM(Kd)

Storage & Handling

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

Alternative Names

beta-catenin, betacatenin, bcatenin, NRX252114, NRX-252114, NRX 252114, Wnt/betacatenin, Wnt/β-catenin, Wnt/b-catenin, Wnt, β-catenin, βcatenin

Compound Identifiers

PubChem CID

162640509