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

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
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 73 In-stock
Solution
10 mM * 1 mL in DMSO USD 73 In-stock
Solid
5 mg USD 66 In-stock
10 mg USD 99 In-stock
25 mg USD 198 In-stock
50 mg USD 352 In-stock
100 mg USD 627 In-stock
200 mg USD 1001 In-stock
500 mg   Get quote  
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Customer Review

Based on 12 publication(s) in Google Scholar

PNU-74654 Related Antibodies

Top Publications Citing Use of Products

    PNU-74654 purchased from MedChemExpress. Usage Cited in: J Cell Physiol. 2019 Jan 26.  [Abstract]

    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 MedChemExpress. Usage Cited in: J Cell Physiol. 2019 Jan 26.  [Abstract]

    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).

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    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].

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

    PNU-74654 Related Antibodies
    Molecular Weight

    320.34

    Formula

    C19H16N2O3
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    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 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 30 mg/mL (93.65 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 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

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

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

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    % 
    +
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    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation
    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

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.1217 mL 15.6084 mL 31.2168 mL 78.0421 mL
    5 mM 0.6243 mL 3.1217 mL 6.2434 mL 15.6084 mL
    10 mM 0.3122 mL 1.5608 mL 3.1217 mL 7.8042 mL
    15 mM 0.2081 mL 1.0406 mL 2.0811 mL 5.2028 mL
    20 mM 0.1561 mL 0.7804 mL 1.5608 mL 3.9021 mL
    25 mM 0.1249 mL 0.6243 mL 1.2487 mL 3.1217 mL
    30 mM 0.1041 mL 0.5203 mL 1.0406 mL 2.6014 mL
    40 mM 0.0780 mL 0.3902 mL 0.7804 mL 1.9511 mL
    50 mM 0.0624 mL 0.3122 mL 0.6243 mL 1.5608 mL
    60 mM 0.0520 mL 0.2601 mL 0.5203 mL 1.3007 mL
    80 mM 0.0390 mL 0.1951 mL 0.3902 mL 0.9755 mL
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    PNU-74654 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    PNU-74654113906-27-7PNU74654PNU 74654Wntβ-cateninApoptosisBeta cateninInhibitorinhibitorinhibit

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