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PNU-74654

Catalog No. T7204   CAS 113906-27-7

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.

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PNU-74654 Chemical Structure
PNU-74654, CAS 113906-27-7
Pack Size Availability Price/USD Quantity
5 mg In stock $ 51.00
10 mg In stock $ 72.00
25 mg In stock $ 153.00
50 mg In stock $ 286.00
100 mg In stock $ 515.00
200 mg In stock $ 747.00
1 mL * 10 mM (in DMSO) In stock $ 58.00
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Purity: 98%
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Biological Description
Chemical Properties
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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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 30 mg/mL (93.65 mM)

TargetMolReferences and Literature

1. Leal, Letícia F, Bueno A C , Gomes, Débora C, et al. Inhibition of the Tcf/beta-catenin complex increases apoptosis and impairs adrenocortical tumor cell proliferation and adrenal steroidogenesis[J]. Oncotarget, 2015, 6(40). 2. Durand J , Lampron A , Mazzuco T L , et al. Characterization of Differential Gene Expression in Adrenocortical Tumors Harboring β-Catenin ( CTNNB1 ) Mutations[J]. The Journal of Clinical Endocrinology and Metabolism, 2011, 96(7):E1206-11.

TargetMolCitations

1. He S, Lu M, Zhang L, et al.RSK4 promotes the macrophage recruitment and M2 polarization in esophageal squamous cell carcinoma.Biochimica et Biophysica Acta (BBA)-Molecular Basis of Disease.2023: 166996.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library NO PAINS Compound Library Anti-Aging Compound Library Bioactive Compound Library Stem Cell Differentiation Compound Library Bioactive Compounds Library Max Anti-Prostate Cancer Compound Library Osteogenesis Compound Library Anti-Obesity Compound Library Cytoskeletal Signaling Pathway Compound Library

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Keywords

PNU-74654 113906-27-7 Apoptosis Cytoskeletal Signaling Stem Cells Wnt/beta-catenin Wnt β-catenin Beta catenin PNU 74654 PNU74654 inhibit Inhibitor inhibitor

 

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