NRX-103094

SKU: orb1686616

Description

NRX-103094 is a potent small molecule that enhances the binding of phosphorylated β-catenin to the SCFβ-TrCP E3 ligase, with an EC50 of 62 nM and a Kd of 0.6 nM. This action promotes β-catenin degradation, making it a valuable research tool for studying Wnt/β-catenin signaling in cancer and other diseases in both cellular and animal models.

Research Area

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

Key Properties

• CAS Number: 2763260-36-0
• MW: 503.28
• Purity: 99.50% (May vary between batches)
• Formula: C₂₀H₁₁Cl₂F₃N₂O₄S
• SMILES: S(C1=C(C(NC2=CC(C(O)=O)=CC=C2)=O)C(=O)NC(C(F)(F)F)=C1)C3=C(Cl)C=CC=C3Cl
• Target: Wnt/beta-catenin,Molecular Glues
• Solubility: DMSO:40 mg/mL (79.48 mM)

Bioactivity

• Target IC50:
  β-catenin-β-TrCP:0.6 nM(Kd)|β-catenin-β-TrCP:62 nM(EC50)
• In Vitro:
  RX-103094 demonstrates high potency against the pSer33/Ser37 β-catenin peptide with an EC50 of 457 nM. At 250 nM, NRX-103094 enhances the ubiquitylation of the pSer33/S37A β-catenin peptide to levels surpassing those of the wild-type pSer33/pSer37. NRX-103094 significantly enhances the binding affinity of the S33E/S37A phosphomimetic peptide for β-TrCP, reducing it from >5 μM in the absence of the compound to 22 nM in the presence of 40 μM NRX-103094. In the presence of 20 μM NRX-103094, we observe robust, time-dependent ubiquitylation of the S33E/S37A β-catenin peptide. Similarly, when 20 μM NRX-103094 is present, the full-length S33E/S37A β-catenin protein undergoes strong ubiquitylation, with ubiquitylation levels approaching those of the WT full-length β-catenin protein.
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Storage & Handling

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

Alternative Names

bcatenin, beta-catenin, betacatenin, NRX 103094, NRX103094, NRX-103094, Wnt/β-catenin, Wnt/betacatenin, Wnt/b-catenin, Wnt, βcatenin, β-catenin

Compound Identifiers

PubChem CID

137628320