113906-27-7
113906-27-7 structure
- Name: PNU 74654
- Chemical Name: PNU 74654,2-Phenoxybenzoicacid-[(5-methyl-2-furanyl)methylene]hydrazide
- CAS Number: 113906-27-7
- Molecular Formula: C19H16N2O3
- Molecular Weight: 320.342
- Catalog: Signaling Pathways Stem Cell/Wnt Wnt
- Create Date: 2016-09-02 05:40:09
- Modify Date: 2024-01-12 09:35:45
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PNU-74654 is an inhibitor of Wnt/β-catenin pathway with an IC50 of 129.8 μM in NCI-H295 cell.
| Name | PNU 74654,2-Phenoxybenzoicacid-[(5-methyl-2-furanyl)methylene]hydrazide |
|---|---|
| Synonyms |
Benzoic acid, 2-phenoxy-, 2-[(1E)-(5-methyl-2-furanyl)methylene]hydrazide
N'-[(E)-(5-Methyl-2-furyl)methylene]-2-phenoxybenzohydrazide N'-[(E)-(5-methylfuran-2-yl)methylidene]-2-phenoxybenzohydrazide PNU-74654 |
| Description | PNU-74654 is an inhibitor of Wnt/β-catenin pathway with an IC50 of 129.8 μM in NCI-H295 cell. |
|---|---|
| Related Catalog | |
| Target |
129.8 μM (Wnt/β-catenin, NCI-H295 cell)[1] |
| In Vitro | PNU-74654 binds to β-catenin with a KD of 450 nM. The Tcf3/Tcf4-binding surface on β-catenin contains a well-defined hot spot around residues K435 and R469. The binding mode of PNU-74654 involves the two narrow pockets on either side of this hot spot[2]. In NCI-H295 cells,PNU-74654 significantly decreases cell proliferation 96 h after treatment, increases early and late apoptosis, decreases nuclear beta-catenin accumulation, impairs CTNNB1/beta-catenin expression and increases beta-catenin target genes 48 h after treatment. No effects are observed on HeLa cells. In NCI-H295 cells, PNU-74654 decreases cortisol, testosterone and androstenedione secretion 24 and 48 h after treatment. The SF1 and CYP21A2 mRNA expression as well as the protein levels of STAR and aldosterone synthase are decreased in NCI-H295 cells after 48 h PNU-74654 treatment. In Y1 cells, PNU-74654 impairs corticosterone secretion 24 h after treatment but does not decrease cell viability[1]. |
| Cell Assay | The PNU-74654 compound is dissolved in DMSO at stock concentrations of 31.2 mM. For working solutions, PNU-74654 is diluted 100X in growth medium with no serum deprivation. NCI-H295 cells are plated at 200,000 cells per well in 24-well plates for gene expression, protein analysis and adrenal steroid measurements. After 48 h, cells are treated with vehicle (0.1%-0.4% DMSO) or 10, 50, 100 and 200 μM PNU-74654. After 24 and 48 h, medium supernatants are collected for adrenal steroid measurements[1]. |
| References |
| Density | 1.2±0.1 g/cm3 |
|---|---|
| Molecular Formula | C19H16N2O3 |
| Molecular Weight | 320.342 |
| Exact Mass | 320.116089 |
| PSA | 63.83000 |
| LogP | 3.90 |
| Index of Refraction | 1.593 |
| Storage condition | -20℃ |
