2. Immunology/Inflammation Metabolic Enzyme/Protease Apoptosis Anti-infection
  3. COX Acyltransferase Apoptosis HSV CMV Influenza Virus
  4. Xanthohumol

Xanthohumol is one of the principal flavonoids isolated from hops, the inhibitor of diacylglycerol acetyltransferase (DGAT), COX-1 and COX-2, and shows anti-cancer and anti-angiogenic activities. Xanthohumol also has antiviral activity against bovine viral diarrhea virus (BVDV), rhinovirus, HSV-1, HSV-2 and cytomegalovirus (CMV).

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

Xanthohumol Chemical Structure

Xanthohumol Chemical Structure

CAS No. : 6754-58-1

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Solid + Solvent
10 mM * 1 mL in DMSO
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Solution
10 mM * 1 mL in DMSO USD 85 In-stock
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5 mg USD 77 In-stock
10 mg USD 132 In-stock
25 mg USD 286 In-stock
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Customer Review

Based on 11 publication(s) in Google Scholar

Other Forms of Xanthohumol:

Xanthohumol Related Antibodies

Top Publications Citing Use of Products

    Xanthohumol purchased from MedChemExpress. Usage Cited in: Phytother Res. 2023 Mar 7.  [Abstract]

    Xanthohumol (XN; 10, 15, 20 μM; 36 h) suppresses the serum-induced migratory ability of A549 cells.

    Xanthohumol purchased from MedChemExpress. Usage Cited in: Phytother Res. 2023 Mar 7.  [Abstract]

    Xanthohumol (XN; 10, 15, 20 μM; 36 h) results in a dose-dependent inhibition of TOPK phosphorylation (Thr9), and inhibits the phosphorylation of histone H3 and Akt, in both HCC827 cells (fig c) and HCT116 cells (Fig d).

    Xanthohumol purchased from MedChemExpress. Usage Cited in: Phytother Res. 2023 Mar 7.  [Abstract]

    Xanthohumol (XN; 25 mg/kg; i.p.; single daily for 30 days) significantly suppresses the tumor growth and reduces the final tumor weight by 50.4% (Fig a-c).

    View All COX Isoform Specific Products:

    View All Isoforms
    COX COX-1 COX-2 COX-3

    View All Acyltransferase Isoform Specific Products:

    View All Isoforms
    ACAT1 ACAT2 MGAT2 ACAT

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Xanthohumol is one of the principal flavonoids isolated from hops, the inhibitor of diacylglycerol acetyltransferase (DGAT), COX-1 and COX-2, and shows anti-cancer and anti-angiogenic activities. Xanthohumol also has antiviral activity against bovine viral diarrhea virus (BVDV), rhinovirus, HSV-1, HSV-2 and cytomegalovirus (CMV).

    IC50 & Target[1][2][3][4][5]

    COX-1

     

    COX-2

     

    HSV-1

     

    HSV-2

     

    DGAT1

    40 μM (IC50)

    DGAT2

    40 μM (IC50)

    CMV

     

    In Vitro

    Xanthohumol significantly attenuates ADP-induced blood platelet aggregation, and significantly reduces the expression of fibrinogen receptor (activated form of GPIIbIIIa) on platelets' surface[1].
    Xanthohumol (5-50 nM) reduces the frequency of spontaneously occurring Ca2+ sparks and Ca2+ waves in control myocytes and in cells subjected to Ca2+ overload caused by: (1) exposure to low K+ solutions, (2) periods of high frequency electrical stimulation, (3) exposures to isoproterenol or (4) caffeine. Xanthohumol (50-100 nM) reduces the rate of relaxation of electrically- or caffeine-triggered Ca2+ transients, without suppressing ICa, but this effect is small and reversed by isoproterenol at physiological temperatures. Xanthohumol also suppresses the Ca2+ content of the SR, and its rate of recirculation[2].
    Treatment of endothelial cells with Xanthohumol leads to increased AMPK phosphorylation and activity. Functional studies using biochemical approaches confirm that AMPK mediates Xanthohumol anti-angiogenic activity. AMPK activation by Xanthohumol is mediated by CAMMKβ, but not LKB1. Analysis of the downstream mechanisms shows that Xanthohumol-induced AMPK activation reduces nitric oxide (NO) levels in endothelial cells by decreasing eNOS phosphorylation. Finally, AKT pathway is inactivated by Xanthohumol as part of its anti-angiogenic activity, but independently from AMPK, suggesting that these two signaling pathways proceed autonomously[3].
    Xanthohumol significantly reduces cell viability and induces apoptosis via pro-caspase-3/8 cleavage and poly(ADP ribose) polymerase (PARP) degradation. Pro-caspase-9 cleavage, Bcl2 family expression changes, mitochondrial dysfunction, and intracellular ROS generation also participate in Xanthohumol-induced glioma cell death. Xanthohumol's inhibition of the IGFBP2/AKT/Bcl2 pathway via miR-204-3p targeting plays a critical role in mediating glioma cell death[4].

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

    Xanthohumol Related Antibodies
    Clinical Trial
    Molecular Weight

    354.40

    Formula

    C21H22O5
    CAS No.
    Appearance

    Solid

    Color

    Yellow to orange

    SMILES

    O=C(C1=C(OC)C=C(O)C(C/C=C(C)\C)=C1O)/C=C/C2=CC=C(O)C=C2
    Structure Classification
    Initial Source
    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 : 83.33 mg/mL (235.13 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 2.8217 mL 14.1084 mL 28.2167 mL
    5 mM 0.5643 mL 2.8217 mL 5.6433 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)

    C1

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    Volume (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 (5.87 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% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.08 mg/mL (5.87 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 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

    mg/kg

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    (per animal)

    g

    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:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    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

    Purity: 99.97%

    COA (245 KB) HNMR (271 KB) LCMS (97 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [3]

    In vitro cell proliferation/viability is measured by the MTT test at different time points. 1000 cells/well are plated into 96-multiwell plates in complete medium. Following adhesion, medium is replaced with fresh medium containing the different treatments or vehicle (DMSO in medium). Xanthohumol and EGCG are used in a concentration range from 2.5 to 40 μM, up to 96 hours. 3 hours before each time point, MTT reagent (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) is added to the wells and plates are incubated at 37°C. At the indicated time points, absorbance at 540 nm is then measured by a FLUOstar spectrophotometer.

    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 2.8217 mL 14.1084 mL 28.2167 mL 70.5418 mL
    5 mM 0.5643 mL 2.8217 mL 5.6433 mL 14.1084 mL
    10 mM 0.2822 mL 1.4108 mL 2.8217 mL 7.0542 mL
    15 mM 0.1881 mL 0.9406 mL 1.8811 mL 4.7028 mL
    20 mM 0.1411 mL 0.7054 mL 1.4108 mL 3.5271 mL
    25 mM 0.1129 mL 0.5643 mL 1.1287 mL 2.8217 mL
    30 mM 0.0941 mL 0.4703 mL 0.9406 mL 2.3514 mL
    40 mM 0.0705 mL 0.3527 mL 0.7054 mL 1.7635 mL
    50 mM 0.0564 mL 0.2822 mL 0.5643 mL 1.4108 mL
    60 mM 0.0470 mL 0.2351 mL 0.4703 mL 1.1757 mL
    80 mM 0.0353 mL 0.1764 mL 0.3527 mL 0.8818 mL
    100 mM 0.0282 mL 0.1411 mL 0.2822 mL 0.7054 mL
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    Xanthohumol 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:

    Xanthohumol6754-58-1COXAcyltransferaseApoptosisHSVCMVInfluenza VirusCyclooxygenaseDiacylglycerol acyltransferaseDiglyceride acyltransferaseacyl-CoA:cholesterol acyltransferasemono- acylglycerol acyltransferaseHerpes simplex virusCytomegalovirusInhibitorinhibitorinhibit

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