1. Stem Cell/Wnt
    Apoptosis
  2. Wnt
    Apoptosis
    β-catenin
  3. PNU-74654

PNU-74654 

Cat. No.: HY-101130 Purity: 99.83%
Handling Instructions

PNU-74654 is an inhibitor of Wnt/β-catenin pathway with an IC50 of 129.8 μM in NCI-H295 cell.

For research use only. We do not sell to patients.

PNU-74654 Chemical Structure

PNU-74654 Chemical Structure

CAS No. : 113906-27-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 90 In-stock
Estimated Time of Arrival: December 31
25 mg USD 180 In-stock
Estimated Time of Arrival: December 31
50 mg USD 320 In-stock
Estimated Time of Arrival: December 31
100 mg USD 570 In-stock
Estimated Time of Arrival: December 31
200 mg USD 910 In-stock
Estimated Time of Arrival: December 31
500 mg   Get quote  
1 g   Get quote  

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Customer Review

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products

Publications Citing Use of MCE PNU-74654

    PNU-74654 purchased from MCE. Usage Cited in: J Cell Physiol. 2019 Jan 26.

    Western blot analysis was used to confirm the total protein expression of β-catenin and AR in the LNCaP, DRCaP, BRCaP, and ERCaP cells treated with the wnt/β-catenin activator (AZD2858, 5 nM, 48 hr) or the wnt/β-catenin inhibitor (PNU74654, 129.8 μM, 48 hr).

    PNU-74654 purchased from MCE. Usage Cited in: J Cell Physiol. 2019 Jan 26.

    Western blot analysis was used to confirm the cytoplasmic and nuclear protein expression of β-catenin and AR in the LNCaP, DRCaP, BRCaP, and ERCaP cells treated with the wnt/β-catenin activator (AZD2858, 5 nM, 48 hr) or the wnt/β-catenin inhibitor (PNU74654, 129.8 μM, 48 hr).
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    Description

    PNU-74654 is an inhibitor of Wnt/β-catenin pathway with an IC50 of 129.8 μM in NCI-H295 cell.

    IC50 & 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].

    Molecular Weight

    320.34

    Formula

    C₁₉H₁₆N₂O₃

    CAS No.

    113906-27-7

    SMILES

    O=C(N/N=C/C1=CC=C(C)O1)C2=CC=CC=C2OC3=CC=CC=C3

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 30 mg/mL (93.65 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.1217 mL 15.6084 mL 31.2168 mL
    5 mM 0.6243 mL 3.1217 mL 6.2434 mL
    10 mM 0.3122 mL 1.5608 mL 3.1217 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (7.80 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (7.80 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Cell Assay
    [1]

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
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    Product name:
    PNU-74654
    Cat. No.:
    HY-101130
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