PNU-74654

Catalog No.S8429 Batch:S842901

Technical Data

Formula	C₁₉H₁₆N₂O₃
Molecular Weight	320.34	CAS No.	113906-27-7
Solubility (25°C)*	In vitro	DMSO	64 mg/mL (199.78 mM)
		Ethanol	10 mg/mL (31.21 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

PNU-74654 disrupts the Wnt signaling pathway 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^[2].

Protocol (from reference)

Cell Assay:^{^[2]}	Cell lines Adrenal (NCI-H295 and Y1) and non-adrenal (HeLa) cell lines Concentrations 5-200 μM Incubation Time 24-96 h Method 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. Adherent cells are fixed for immunofluorescence or harvested for RNA and protein isolation.

Cell Assay:^{^[2]}

Cell lines
Adrenal (NCI-H295 and Y1) and non-adrenal (HeLa) cell lines
Concentrations
5-200 μM
Incubation Time
24-96 h
Method
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. Adherent cells are fixed for immunofluorescence or harvested for RNA and protein isolation.

References

Selleck's PNU-74654 has been cited by 22 publications

Retinoic acid enhances HIV-1 reverse transcription and transcription in macrophages via mTOR-modulated mechanisms [ Cell Rep, 2024, 43(7):114414]	PubMed: 38943643
Protective effects of emodin on subchondral bone and articular cartilage in osteoporotic osteoarthritis rats: A preclinical study [ Exp Gerontol, 2024, 190:112413]	PubMed: 38570055
GRIK5 stimulates colon cancer growth and metastasis through cAMP/PKA/CADM3 signaling [ Cell Biol Int, 2023, 47(7):1259-1266]	PubMed: 36959746
A specific upregulated lncRNA in colorectal cancer promotes cancer progression [ JCI Insight, 2022, e158855]	PubMed: 35617032
β-catenin regulates HIV latency and modulates HIV reactivation [ PLoS Pathog, 2022, 18(3):e1010354]	PubMed: 35255110
Tankyrase Regulates Neurite Outgrowth through Poly(ADP-ribosyl)ation-Dependent Activation of β-Catenin Signaling [ Int J Mol Sci, 2022, 23(5)2834]	PubMed: 35269974
C-Peptide Promotes Cell Migration by Controlling Matrix Metallopeptidase-9 Activity Through Direct Regulation of β-Catenin in Human Endometrial Stromal Cells [ Front Cell Dev Biol, 2022, 10:800181]	PubMed: 35127683
MDMX acts as a pervasive preleukemic-to-acute myeloid leukemia transition mechanism [ Cancer Cell, 2021, 39(4):529-547.e7]	PubMed: 33667384
Circ-Smad5 retards the G1/S transition of cell cycle via inhibiting the activity of wnt/lef/cyclind1 signaling in JB6 cells [ Genes Dis, 2021, 8(3):364-372]	PubMed: 33997183
β-catenin-promoted cholesterol metabolism protects against cellular senescence in naked mole-rat cells [ Commun Biol, 2021, 4(1):357]	PubMed: 33742113

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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