1. Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease Stem Cell/Wnt
  2. PPAR Wnt β-catenin
  3. FH535

FH535 is an inhibitor of Wnt/β-catenin and PPAR, with anti-tumor activities.

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

FH535 Chemical Structure

FH535 Chemical Structure

CAS No. : 108409-83-2

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Solid + Solvent
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 42 In-stock
10 mg USD 66 In-stock
50 mg USD 204 In-stock
100 mg USD 352 In-stock
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Customer Review

Based on 13 publication(s) in Google Scholar

Top Publications Citing Use of Products

    FH535 purchased from MedChemExpress. Usage Cited in: Neurochem Res. 2022 Nov 12.  [Abstract]

    FH535 (2.5 µM; 1 h) significantly inhibits β-catenin and cyclin D1 expressions, and attenuates the effect of SOX6 knockdown on Wnt/β-catenin pathway, in OGD/R-triggered HT22 cells.

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    FH535 is an inhibitor of Wnt/β-catenin and PPAR, with anti-tumor activities.

    IC50 & Target[1]

    PPAR

     

    β-catenin

     

    In Vitro

    FH535 is an inhibitor of Wnt/β-catenin and PPAR. FH535 inhibits PPARγ and PPARδ transactivation in HCT116 cells. FH535 (15 μM) activities depend on functional PPARδ but does not require a cysteine residue in the PPAR ligand-binding domain. FH535 inhibits recruitment of the coactivators GRIP1 and β-catenin to PPARδ and PPARγ. FH535 shows toxic effects on 12 carcinoma cell lines expressing wnt/β-catenin pathway[1].
    FH535 (20 μM) suppresses the β-catenin pathway in pancreatic cancer cells, and inhibits pancreatic cancer cell migration. Furthermore, FH535 (20, 40 μM) inhibits pancreatic cancer cell invasion and cell growth[2].
    FH535 represses angiogenesis-related genes in pancreatic cancer cells[3].

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

    In Vivo

    FH535 (25 mg/kg, i.p.) exhibits an anti-tumor effect on pancreatic cancer xenografts in mice. FH535 also represses angiogenesis in pancreatic cancer xenografts[2].

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

    Molecular Weight

    361.20

    Formula

    C13H10Cl2N2O4S

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=S(C1=CC(Cl)=CC=C1Cl)(NC2=CC=C([N+]([O-])=O)C=C2C)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

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

    DMSO : 33.33 mg/mL (92.28 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.7685 mL 13.8427 mL 27.6855 mL
    5 mM 0.5537 mL 2.7685 mL 5.5371 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, 1 years; -20°C, 6 months. When stored at -80°C, please use it within 1 years. When stored at -20°C, please use it within 6 months.

    • 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

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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 (6.92 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% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (6.92 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

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    Dosing volume
    (per animal)

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    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
    [2]

    Cell growth is evaluated using the MTT assay. Cells (5 × 104/well) are seeded in 24-well tissue culture plates. Blank control is treated with DMSO. After FH535 treatment, MTT is added to each well (final concentration, 0.5 mg/mL), followed by 4-hour incubation at 37°C. The medium is removed, and 800 μL of DMSO is added to each well. The absorbance of the mixture is measured at 490 nm using a microplate enzyme-linked immunosorbent assay reader. The relative cell viability is calculated as follows: relative cell viability = (mean experimental absorbance/mean control absorbance) ×100%[2].

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

    Animal Administration
    [3]

    Four-week-old female BALB/c athymic nude mice receive humane care. PANC-1 cells stably expressing firefly luciferase are injected into the left flanks of the mice in a total volume of 100 μL (0.5 × 107 cells), and the mice are randomly assigned to a DMSO [intraperitoneally injected with 100 μL DMSO/DMEM (1:1)] or FH535 group [intraperitoneally injected with 25 mg/kg FH535 dissolved in 100 μL DMSO/DMEM (1:1)]. Treatment is conducted every 2 days for 20 days; tumor volume is measured with a caliper using the formula: volume = length × width2/2. At the end of the experiment, the mice are anaesthetized and given D-luciferin in PBS. Twenty minutes after the injection, bioluminescence is imaged with a charge-coupled device camera. Then, the tumor tissue is stripped and formalin-fixed, paraffin-embedded, cut into 4-μm sections, and immunohistochemically stained[3].

    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, 1 years; -20°C, 6 months. When stored at -80°C, please use it within 1 years. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.7685 mL 13.8427 mL 27.6855 mL 69.2137 mL
    5 mM 0.5537 mL 2.7685 mL 5.5371 mL 13.8427 mL
    10 mM 0.2769 mL 1.3843 mL 2.7685 mL 6.9214 mL
    15 mM 0.1846 mL 0.9228 mL 1.8457 mL 4.6142 mL
    20 mM 0.1384 mL 0.6921 mL 1.3843 mL 3.4607 mL
    25 mM 0.1107 mL 0.5537 mL 1.1074 mL 2.7685 mL
    30 mM 0.0923 mL 0.4614 mL 0.9228 mL 2.3071 mL
    40 mM 0.0692 mL 0.3461 mL 0.6921 mL 1.7303 mL
    50 mM 0.0554 mL 0.2769 mL 0.5537 mL 1.3843 mL
    60 mM 0.0461 mL 0.2307 mL 0.4614 mL 1.1536 mL
    80 mM 0.0346 mL 0.1730 mL 0.3461 mL 0.8652 mL
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    • 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.

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    Product Name:
    FH535
    Cat. No.:
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