[CAS NO. 113906-27-7]  PNU-74654

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PRODUCTS SPECIFICATIONS [113906-27-7]

Catalog
SLK-S8429
Brand
Selleck
CAS
113906-27-7

DESCRIPTION [113906-27-7]

Overview

MDLMFCD12912438
Molecular Weight320.34
Molecular FormulaC19H16N2O3
SMILESO=C(N/N=C/C1=CC=C(C)O1)C2=CC=CC=C2OC3=CC=CC=C3

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM3.1217 mL15.6084 mL31.2168 mL
5 mM0.6243 mL3.1217 mL6.2434 mL
10 mM0.3122 mL1.5608 mL3.1217 mL
50 mM0.0624 mL0.3122 mL0.6243 mL

Description

PNU-75654 disrupts the via inhibition of the interaction (KD50=450 nM) between β-catenin and Tcf4.

Targets

Wnt/β-catenin [1]
(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,PNU-74654 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, PNU-74654 decreases cortisol, testosterone and androstenedione secretion 24 and 48 h after treatment. Additionally, in NCI-H295 cells, PNU-74654 decreases 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 impairs corticosterone secretion 24 h after treatment but does not decrease cell viability.