PNU-74654

SKU: orb1299981

Description

PNU 74654 is a small molecule inhibitor that disrupts Wnt/β-catenin signaling by binding β-catenin (Kd = 450 nM) and blocking its interaction with Tcf4. This tool compound is used in vitro and in vivo to study oncogenesis and stem cell biology driven by aberrant Wnt pathway activation.

Research Area

Cell Biology, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 113906-27-7
• MW: 320.34
• Purity: 98.00% (May vary between batches)
• Formula: C₁₉H₁₆N₂O₃
• SMILES: Cc1ccc(\C=N\NC(=O)c2ccccc2Oc2ccccc2)o1
• Target: Apoptosis,Wnt/beta-catenin
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (6.24 mM);DMSO:30 mg/mL (93.65 mM)

Bioactivity

• Target IC50:
  Wnt/β-catenin (NCI-H295 cells):129.8 μM
• In Vitro:
  In NCI-H295 cells, PNU 74654 significantly decreased cell proliferation 96 h after treatment, increased early and late apoptosis, decreased nuclear beta-catenin accumulation, impaired CTNNB1/beta-catenin expression and increased beta-catenin target genes 48 h after treatment. No effects were observed on HeLa cells. In NCI-H295 cells, PNU 74654 decreased cortisol, testosterone and androstenedione secretion 24 and 48 h after treatment. Additionally, in NCI-H295 cells, PNU 74654 decreased SF1 and CYP21A2 mRNA expression as well as the protein levels of STAR and aldosterone synthase 48 h after treatment. In Y1 cells, PNU 74654 impaired corticosterone secretion 24 h after treatment but did not decrease cell viability.
• Cell Research:
  Adrenal (NCI-H295 and Y1) and non-adrenal (HeLa) cell lines were treated with PNU 74654 (5-200 μM) for 24-96 h to assess cell viability (MTS-based assay), apoptosis (Annexin V), expression/localization of beta-catenin (qPCR, immunofluorescence, immunocytochemistry and western blot), expression of beta-catenin target genes (qPCR and western blot), and adrenal steroidogenesis (radioimmunoassay, qPCR and western blot).

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

bcatenin, Apoptosis, Beta catenin, betacatenin, beta-catenin, inhibit, Inhibitor, Wnt/betacatenin, Wnt/b-catenin, Wnt, Wnt/β-catenin, PNU 74654, PNU74654, PNU-74654, β-catenin, βcatenin

Compound Identifiers

PubChem CID

9836739