1. Stem Cell/Wnt
  2. Porcupine
    Wnt

Wnt-C59 (Synonyms: C59)

Cat. No.: HY-15659 Purity: 99.56%
Handling Instructions

Wnt-C59 is a potent PORCN enzymatic activity and Wnt inhibitor.

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

Wnt-C59 Chemical Structure

Wnt-C59 Chemical Structure

CAS No. : 1243243-89-1

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 92 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
5 mg USD 84 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 119 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 300 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg USD 540 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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    Wnt-C59 purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2017 Nov 28;44(3):1251-1262.

    The protein levels of Wnt3a and β-catenin are examined in MCF-7 spheres and MDA-MB-231 spheres with Wnt-C59 treatment or not via western blot analysis.

    Wnt-C59 purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2017 Nov 28;44(3):1251-1262.

    The inhibitor of NRP-1 called EG00229 decreases sphere and clone formation in MDA-MB-231 cells.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Wnt-C59 is a potent PORCN enzymatic activity and Wnt inhibitor.

    IC50 & Target

    PORCN[1]
    Wnt[2]

    In Vitro

    Wnt-C59 (C59) inhibits PORCN activity at nanomolar concentrations, as assessed by inhibition of Wnt palmitoylation, Wnt interaction with the carrier protein Wntless/WLS, Wnt secretion, and Wnt activation of β-catenin reporter activity. Wnt-C59 inhibits WNT3A-mediated activation of a multimerized TCF-binding site driving luciferase with an IC50 of 74 pM. Wnt-C59 is a nanomolar inhibitor of mammalian PORCN acyltransferase activity and blocks activation of all evaluated human Wnts[1]. WNT-C59 is a WNT inhibitor, efficiently induces anterior cortex that includes cortical motor neurons from human pluripotent stem cells. Both CNE1 and HNE1 cells show reduced growth abilities in the higher Wnt-C59 concentration (20 μM), while HK1 cells are sensitive to all concentrations (5 μM, 10 μM, and 20 μM) of Wnt-C59 treatments. A low concentration (1 μM) of Wnt-C59 treatment suppresses SUNE1 cells and 3D growth is clearly inhibited compared to control untreated cells. The inhibitory effects of Wnt-C59 are dosage-dependent in these NPC cells; both 5 μM and 20 μM Wnt-C59 treatments can arrest sphere formation in both HNE1 and SUNE1 cell lines, but not CNE1 cells. However, cells showing a monolayer growth with Wnt-C59 treatments are continuously expanding and both 3D inhibition and monolayer growth are consistent, as observed from weeks 1 to 3[2].

    In Vivo

    In mice, Wnt-C59 (C59) displays good bioavailability, as once daily oral administration is sufficient to maintain blood concentrations well above the IC50. Wnt-C59 blocks progression of mammary tumors in MMTV-WNT1 transgenic mice while downregulating Wnt/β-catenin target genes. After either intravenous (2.5 mg/kg) or oral administration (5 mg/kg), the compound half-life in blood is approximately 1.94 hours. Following development of palpable tumors, mice are treated with either vehicle or C59, 10 mg/kg/d for 17 days. Wnt-C59 administration arrested or reversed tumor growth in all treated mice (n=22). After 17 days of treatment, the tumors are removed and further analyzed. Final tumor weights are significantly different[1].

    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 2.6354 mL 13.1770 mL 26.3539 mL
    5 mM 0.5271 mL 2.6354 mL 5.2708 mL
    10 mM 0.2635 mL 1.3177 mL 2.6354 mL
    Please refer to the solubility information to select the appropriate solvent.
    Cell Assay
    [1]

    Wnt-C59 (C59) is dissolved in DMSO (10 mM) and stored, and then diluted with appropriate medium before use[1].

    Approximately, 1×104 cells are seeded in 24-well plates, and Wnt-C59 (5 μM, 10 μM, and 20 μM) is added the next day. Each group is tested in triplicate and control groups with addition of DMSO are also established. Cell confluence is determined by microscopy at 24, 48, 72, and 96 hours after seeding of cells. The IC50 of Wnt-C59 is determined by MTT assay, using 96-well dishes. Next day, various concentrations of Wnt-C59 are added, and cellular viabilities are measured by a spectrophotometer at both 24 and 48 hours. For sphere formation, approximately one hundred cells are seeded onto the Low Cell Bind Surface 24-well Nunc dish. Each group is done in triplicate and each well had 2 mL medium. Media are changed twice a week, and only half of the media is changed each time. Approximately, 1×103 cells are seeded for each well in the sphere inhibition assay. At 1 to 5 days after plating, all tested cells formed small spheres. Five days later, Wnt-C59 (1 μM, 5 μM, and 20 μM) is added into experimental groups. Abilities for cell growth and sphere images are compared and recorded at the end of the first, second, and third weeks after addition of Wnt-C59, or DMSO in control groups. The sphere growths are observed and recorded daily under microscopy, and the area of spheres is analyzed using Metamorph and recorded as average area (μm2)[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    Wnt-C59 (C59) is resuspended by sonication for 20 minutes in a mixture of 0.5% methylcellulose and 0.1% Tween-80[1].

    Mice[1]
    A total of 1×107 cells in 200 μL DMEM are injected into 4-8 week old nude mice subcutaneously. Next day, mice are randomly divided into two groups, experimental and control, and are given Wnt-C59 via vein injection. Based on previous reports, Wnt-C59 is dissolved in 30% propylene glycol for intravenous tail vein administration (2.5 mg/kg). After 48 hours, Wnt-C59 is added into drinking water (5 mg/kg/day) for experimental groups. Fresh water with Wnt-C59 is changed every 48 hours in dark bottles avoiding light; water consumption is recorded and calculated. Mice in control groups are treated with injection of 30% propylene glycol and given fresh water containing DMSO. Tumor sizes are measured three times a week until the last day of the experiment. Injected tumor cell nodule growth or shrinkage is recorded and only progressively growing tumors, confirmed by both gross and histology examinations, are counted. Tumor incidence is determined based on tumor numbers on the last day of experiment and termination day of assay is decided depending on possible appearance of ulcers on the surface of fast-growing tumors in control animals. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    379.45

    Formula

    C₂₅H₂₁N₃O

    CAS No.

    1243243-89-1

    SMILES

    O=C(NC1=CC=C(C2=CC=CN=C2)C=C1)CC3=CC=C(C4=CC(C)=NC=C4)C=C3

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 73.3 mg/mL

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    Purity: 99.56%

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    Product Name:
    Wnt-C59
    Cat. No.:
    HY-15659
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