1. Apoptosis Metabolic Enzyme/Protease
  2. Caspase Lipoxygenase Apoptosis
  3. Wedelolactone

Wedelolactone suppresses LPS-induced caspase-11 expression by directly inhibits the IKK Complex. Wedelolactone also inhibits 5-lipoxygenase (5-Lox) with an IC50 of 2.5 μM. Wedelolactone induces caspase-dependent apoptosis in prostate cancer cells via downregulation of PKCε without inhibiting Akt. Wedelolactone can extract from Eclipta alba, and it can be used for the research of cancer.

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

CAS No. : 524-12-9

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Customer Review

Based on 24 publication(s) in Google Scholar

Other Forms of Wedelolactone:

Top Publications Citing Use of Products

    Wedelolactone purchased from MedChemExpress. Usage Cited in: J Hematol Oncol. 2022 Jul 14;15(1):93.  [Abstract]

    Wedelolactone (WE) had substantial activity in activating the catalytic activity of GPD1.

    Wedelolactone purchased from MedChemExpress. Usage Cited in: J Hematol Oncol. 2022 Jul 14;15(1):93.  [Abstract]

    The results showed that the binding affinity for Wedelolactone (WE) had a dissociation constant (Kd) of 505 nM.

    Wedelolactone purchased from MedChemExpress. Usage Cited in: J Hematol Oncol. 2022 Jul 14;15(1):93.  [Abstract]

    Wedelolactone (WE) on the catalytic activity of GPD1 in bladder cell lines, we monitored G3P and NAD+ levels in the 5637 and T24 cell lines after WE treatment. We found that WE increased both G3P and NAD+ at a concentration of 10 µM.

    Wedelolactone purchased from MedChemExpress. Usage Cited in: J Hematol Oncol. 2022 Jul 14;15(1):93.  [Abstract]

    To further investigate the function of WE in bladder cancer, we assessed the growth and death of bladder cancer cells after Wedelolactone (WE) treatment. Our results showed that WE reduced the proliferation ability of 5637 and T24 cells by CCK-8 cell assay, while other compounds found in virtual screening did not affect proliferation.

    Wedelolactone purchased from MedChemExpress. Usage Cited in: J Hematol Oncol. 2022 Jul 14;15(1):93.  [Abstract]

    The colony formation assay indicated that Wedelolactone (WE) significantly decreased the colony number of 5637 cells and T24 cells.

    Wedelolactone purchased from MedChemExpress. Usage Cited in: J Hematol Oncol. 2022 Jul 14;15(1):93.  [Abstract]

    Wedelolactone (WE) induced apoptosis in 5637 cells and T24 cells.

    Wedelolactone purchased from MedChemExpress. Usage Cited in: J Hematol Oncol. 2022 Jul 14;15(1):93.  [Abstract]

    To determine whether Wedelolactone (WE) might suppress bladder cells in vivo, we implanted 5637 cells or T24 cells into BALB/c Nude mice. Compared with the control group, Wedelolactone (WE) treatment significantly reduced tumor weight.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Wedelolactone suppresses LPS-induced caspase-11 expression by directly inhibits the IKK Complex. Wedelolactone also inhibits 5-lipoxygenase (5-Lox) with an IC50 of 2.5 μM. Wedelolactone induces caspase-dependent apoptosis in prostate cancer cells via downregulation of PKCε without inhibiting Akt. Wedelolactone can extract from Eclipta alba, and it can be used for the research of cancer[1][2][3].

    IC50 & Target[1][2][3]

    Caspase-11

     

    5-LOX

    2.5 μM (IC50)

    Apoptosis

     

    Cellular Effect
    Cell Line Type Value Description References
    OVCAR-3 EC50
    10.64 μM
    Compound: Wedelolactone
    Inhibition of colony formation in human OVCAR-3 cells overexpressing G6PD incubated for 14 days by crystal violet staining based assay
    Inhibition of colony formation in human OVCAR-3 cells overexpressing G6PD incubated for 14 days by crystal violet staining based assay
    [PMID: 33689874]
    Vero CC50
    373.5 μM
    Compound: Wedelolactone
    Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
    Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
    [PMID: 38879995]
    In Vitro

    Wedelolactone (0-5 μg/mL; 0-21 d) enhances bone marrow mesenchymal stem cells (BMSC) differentiation towards osteoblasts[3].
    Wedelolactone (0-6 μg/mL; 0-9 d) inhibits GSK3β activity and increases β-catenin and runx2 nuclear accumulation in BMSC, and inhibits the effect of RANKL[3].
    Wedelolactone (0-5 μg/ml; 60 min) inhibits GSK3β activity and proves GSK3β is the target of wedelolactone[3].
    Wedelolactone (0-5 μg/ml; 6 d) inhibits c-src, c-fos and cathepsin k expression level[3].

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

    Cell Differentiation Assay[3]

    Cell Line: Mouse BMSC
    Concentration: 0-5 μg/mL
    Incubation Time: 0, 6, 9, 12 and 21 days
    Result: Increased Mouse BMSC into osteoblastic cells and dose-dependently increased the activity of alkaline phosphatase at incubation for 9 days.

    Western Blot Analysis[3]

    Cell Line: Mouse BMSC and RAW264.7 cells
    Concentration: 0-5 μg/mL
    Incubation Time: 0-9 days
    Result: Decreased GSK3β expression level and up-regulated GSK3β phosphorylation, nuclear accumulation of β-catenin and runx2 in BMSC. Inhibited RANKL-induced phosphorylation of NF-κB/p65 and the expression level of c-fos and c-Src.

    Cell Viability Assay[3]

    Cell Line: Mouse BMSC
    Concentration: 0.1, 1.25, 2.5, 5 μg/ml
    Incubation Time: 60 min
    Result: Inhibited GSK3β activity with an IC50 of 21.7 μM weeker than staurosporin which is a GSK3β inhibitor and proved GSK3β is a target.

    RT-PCR[3]

    Cell Line: RAW264.7 cells
    Concentration: 0, 0.6, 1.25, 2.5 and 5 μg/mL
    Incubation Time: 6 days
    Result: Inhibited the expression of osteoclast differentiation related marker genes c-src, c-fos and cathepsin in RAW264.7 cells.
    In Vivo

    Wedelolactone (10 mg/kg; i.p. every 2 days for 4 weeks) decreases bone volumn and trabecular number at the femur after ovarietomy, and prevents the VOX-induced bone loss[3].

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

    Animal Model: Ovariectomized 9-week-old mice[3]
    Dosage: 10 mg/kg
    Administration: Intraperitoneal injection; 10 mg/kg every 2 days; for 4 weeks
    Result: Inhibited osteoclast activity and stimulated osteoblast differentiation to achieved osteoprotective effect.
    Molecular Weight

    314.25

    Formula

    C16H10O7

    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    O=C1C2=C(OC3=CC(O)=C(O)C=C32)C4=C(O)C=C(OC)C=C4O1

    Structure Classification
    Initial Source
    Shipping

    Room temperature in continental US; may vary elsewhere.

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

    DMSO : 125 mg/mL (397.77 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 3.1822 mL 15.9109 mL 31.8218 mL
    5 mM 0.6364 mL 3.1822 mL 6.3644 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 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. 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

    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: ≥ 2.08 mg/mL (6.62 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (6.62 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

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

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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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    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

    Purity: 99.93%

    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 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. 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 3.1822 mL 15.9109 mL 31.8218 mL 79.5545 mL
    5 mM 0.6364 mL 3.1822 mL 6.3644 mL 15.9109 mL
    10 mM 0.3182 mL 1.5911 mL 3.1822 mL 7.9554 mL
    15 mM 0.2121 mL 1.0607 mL 2.1215 mL 5.3036 mL
    20 mM 0.1591 mL 0.7955 mL 1.5911 mL 3.9777 mL
    25 mM 0.1273 mL 0.6364 mL 1.2729 mL 3.1822 mL
    30 mM 0.1061 mL 0.5304 mL 1.0607 mL 2.6518 mL
    40 mM 0.0796 mL 0.3978 mL 0.7955 mL 1.9889 mL
    50 mM 0.0636 mL 0.3182 mL 0.6364 mL 1.5911 mL
    60 mM 0.0530 mL 0.2652 mL 0.5304 mL 1.3259 mL
    80 mM 0.0398 mL 0.1989 mL 0.3978 mL 0.9944 mL
    100 mM 0.0318 mL 0.1591 mL 0.3182 mL 0.7955 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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