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PNU 74654 binds to β-catenin (Kd = 450 nM), inhibiting its interaction with the transcription factor T cell factor 4 (Tcf4) resulting in disruption of the Wnt signaling pathway.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $51 | In Stock | |
10 mg | $72 | In Stock | |
25 mg | $153 | In Stock | |
50 mg | $286 | In Stock | |
100 mg | $515 | In Stock | |
200 mg | $747 | In Stock | |
1 mL x 10 mM (in DMSO) | $58 | In Stock |
Description | PNU 74654 binds to β-catenin (Kd = 450 nM), inhibiting its interaction with the transcription factor T cell factor 4 (Tcf4) resulting in disruption of the Wnt signaling pathway. |
Targets&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[1]. |
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)[1]. |
Molecular Weight | 320.34 |
Formula | C19H16N2O3 |
Cas No. | 113906-27-7 |
Smiles | Cc1ccc(\C=N\NC(=O)c2ccccc2Oc2ccccc2)o1 |
Relative Density. | 1.17 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 30 mg/mL (93.65 mM) | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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