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PNU-74654 Wnt/beta-catenin inhibitor

Cat.No.S8429

PNU-74654 disrupts the Wnt signaling pathway via inhibition of the interaction (KD50=450 nM) between β-catenin and Tcf4.
PNU-74654 Wnt/beta-catenin inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 320.34

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Quality Control

Batch: Purity: 99.66%
99.66

Solubility

In vitro
Batch:

DMSO : 64 mg/mL (199.78 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 5 mg/mL

Water : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 320.34 Formula

C19H16N2O3

 Storage (From the date of receipt)
CAS No. 113906-27-7 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC1=CC=C(O1)C=NNC(=O)C2=CC=CC=C2OC3=CC=CC=C3

Mechanism of Action

Targets/IC50/Ki
Wnt/β-catenin
(Cell-free assay)
450 nM(Kd)
In vitro

The PNU-74654 (PNU) compound is a non-FDAapproved drug which prevents that Tcf from binding to beta-catenin, acting as a Wnt/beta-catenin antagonist. In NCI-H295 cells, this compound significantly decreases cell proliferation 96 h after treatment, increases early and late apoptosis, decreases nuclear betacatenin accumulation, impairs CTNNB1/beta-catenin expression and increases betacatenin target genes 48 h after treatment. No effects are observed on HeLa cells. In NCI-H295 cells, this chemical decreases cortisol, testosterone and androstenedione secretion 24 and 48 h after treatment. Additionally, in NCI-H295 cells, it decreases SF1 and CYP21A2 mRNA expression as well as the protein levels of STAR and aldosterone synthase 48 h after treatment. In Y1 cells, this compound impairs corticosterone secretion 24 h after treatment but does not decrease cell viability.
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