1. Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease Immunology/Inflammation NF-κB Apoptosis Autophagy
  2. ROR Reactive Oxygen Species Apoptosis Autophagy
  3. Nobiletin

Nobiletin is a poly-methoxylated flavone from the citrus peel that improves memory loss. Nobiletin is a retinoid acid receptor-related orphan receptors (RORs) agonist. Nobiletin can reduce reactive oxygen species (ROS) levels in differentiated C2C12 myotubes and has anti-inflammation and anti-cancer properties, including anti-angiogenesis, anti-proliferation, anti-metastasis and induced apoptosis.

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

Nobiletin Chemical Structure

Nobiletin Chemical Structure

CAS No. : 478-01-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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Customer Review

Based on 19 publication(s) in Google Scholar

Other Forms of Nobiletin:

Top Publications Citing Use of Products

    Nobiletin purchased from MedChemExpress. Usage Cited in: Nutrients. 2023 Apr 7, 15(8), 1801.

    Nobiletin (Nob; 100 mg/kg/day; s.c.; 10 weeks) markedly reduces D-gal (D-galactose)-induced increases in the ratio of p-FOXO 3a/FOXO and the expression of MAFbx and MuRF1 in mice.

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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Nobiletin is a poly-methoxylated flavone from the citrus peel that improves memory loss. Nobiletin is a retinoid acid receptor-related orphan receptors (RORs) agonist. Nobiletin can reduce reactive oxygen species (ROS) levels in differentiated C2C12 myotubes and has anti-inflammation and anti-cancer properties, including anti-angiogenesis, anti-proliferation, anti-metastasis and induced apoptosis[1][2][3][4].

    IC50 & Target

    Retinoid acid receptor-related orphan receptors (RORs)[1]; reactive oxygen species (ROS)[1]; apoptosis[2]

    Cellular Effect
    Cell Line Type Value Description References
    CWR22R IC50
    36.53 μM
    Compound: 44
    Antiproliferative activity against human 22Rv1 cells incubated for 24 hrs by CCK-8 assay
    Antiproliferative activity against human 22Rv1 cells incubated for 24 hrs by CCK-8 assay
    [PMID: 36459083]
    DU-145 IC50
    144.5 μM
    Compound: 44
    Antiproliferative activity against human DU-145 cells incubated for 24 hrs by CCK-8 assay
    Antiproliferative activity against human DU-145 cells incubated for 24 hrs by CCK-8 assay
    [PMID: 36459083]
    HL-60 IC50
    10 ng/mL
    Compound: Nobiletin
    Growth inhibition of human HL60 cells after 72 hrs by MTT assay
    Growth inhibition of human HL60 cells after 72 hrs by MTT assay
    [PMID: 31398616]
    HL-60 IC50
    41.5 μM
    Compound: I
    Antiproliferative activity against HL60 after 24 hrs
    Antiproliferative activity against HL60 after 24 hrs
    [PMID: 17391969]
    HT-29 IC50
    24 μM
    Compound: 4, Nobiletin
    Anticancer activity against human HT-29 cells after 72 hrs by MTT assay
    Anticancer activity against human HT-29 cells after 72 hrs by MTT assay
    [PMID: 19054677]
    LNCaP C4-2 IC50
    30.3 μM
    Compound: 44
    Antiproliferative activity against human C4-2 cells incubated for 24 hrs by CCK-8 assay
    Antiproliferative activity against human C4-2 cells incubated for 24 hrs by CCK-8 assay
    [PMID: 36459083]
    MCF7 IC50
    4.4 μM
    Compound: 20
    Inhibition of BCRP expressed in MCF-7 MX cells using Hoechst 33342 staining
    Inhibition of BCRP expressed in MCF-7 MX cells using Hoechst 33342 staining
    [PMID: 21354800]
    MDCK IC50
    4.9 μM
    Compound: 20
    Inhibition of BCRP expressed in MDCK cells using Hoechst 33342 staining
    Inhibition of BCRP expressed in MDCK cells using Hoechst 33342 staining
    [PMID: 21354800]
    Monocyte IC50
    10 μM
    Compound: Nobiletin
    Inhibition of TNFalpha expression in LPS-stimulated human monocytes treated 30 mins before LPS challenge measured after 14 hrs by ELISA
    Inhibition of TNFalpha expression in LPS-stimulated human monocytes treated 30 mins before LPS challenge measured after 14 hrs by ELISA
    [PMID: 10096854]
    PC-3 IC50
    122.6 μM
    Compound: 44
    Antiproliferative activity against human PC-3 cells incubated for 24 hrs by CCK-8 assay
    Antiproliferative activity against human PC-3 cells incubated for 24 hrs by CCK-8 assay
    [PMID: 36459083]
    In Vitro

    Nobiletin (0-100 μM; 24 hours; U2OS and HOS cells) treatment progressively reduces protein expressions of MMP-2 and MMP-9. In U2OS and HOS cells, Nobiletin considerably reduces the phosphorylation of p-IKKα/β and p-IκBα, and protein expression of NF-κB in the cell nuclear fraction with the concomitant increase of the NF-κB expression in the cytosolic fraction. Nobiletin down-regulates the p-CREB and the SP-1 expressions in the nuclear fraction, whereas Nobiletin does not affect c-Jun and c-Fos expressions[1].
    Nobiletin (0-100 μM; 24 hours; U2OS and HOS cells) treatment significantly reduces mRNA expressions of MMP-2 and MMP-9 dose-dependently in U2OS and HOS cells[1].

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

    Western Blot Analysis[1]

    Cell Line: U2OS and HOS cells
    Concentration: 0 μM, 25 μM, 50 μM, 75 μM, 100 μM
    Incubation Time: 24 hours
    Result: Progressively reduced protein expressions of MMP-2 and MMP-9. Considerably reduced the phosphorylation of p-IKKα/β and p-IκBα, and protein expression of NF-κB in the cell nuclear fraction with the concomitant increase of the NF-κB expression in the cytosolic fraction. Down-regulated the p-CREB and the SP-1 expressions in the nuclear fraction in U2OS and HOS cells.

    RT-PCR[1]

    Cell Line: U2OS and HOS cells
    Concentration: 0 μM, 25 μM, 50 μM, 75 μM, 100 μM
    Incubation Time: 24 hours
    Result: Significantly reduced mRNA expressions of MMP-2 and MMP-9 dose-dependently in U2OS and HOS cells.
    In Vivo

    Nobiletin (0.1% of regular diet; oral administration; daily; for 20 weeks; male C57BL/6 mice) treatment restores glucose homeostasis and promots energy expenditure and circadian activity in aged mice[2].

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

    Animal Model: 20- to 22-month-old male C57BL/6 mice[2]
    Dosage: 0.1% of regular diet
    Administration: Oral administration; daily; for 20 weeks
    Result: Fully restored glucose tolerance in aged mice, and increased basal body temperature and cold tolerance in aged mice. Led to a twofold increase in distance run/day on voluntary wheels compared with aged regular diet-fed mice during the active phase.
    Molecular Weight

    402.39

    Formula

    C21H22O8

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C1C=C(C2=CC=C(OC)C(OC)=C2)OC3=C(OC)C(OC)=C(OC)C(OC)=C13

    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 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (124.26 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 2.4852 mL 12.4258 mL 24.8515 mL
    5 mM 0.4970 mL 2.4852 mL 4.9703 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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    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    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (6.21 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 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.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (5.17 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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    mg/kg

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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:
    %
    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: 99.79%

    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 2.4852 mL 12.4258 mL 24.8515 mL 62.1288 mL
    5 mM 0.4970 mL 2.4852 mL 4.9703 mL 12.4258 mL
    10 mM 0.2485 mL 1.2426 mL 2.4852 mL 6.2129 mL
    15 mM 0.1657 mL 0.8284 mL 1.6568 mL 4.1419 mL
    20 mM 0.1243 mL 0.6213 mL 1.2426 mL 3.1064 mL
    25 mM 0.0994 mL 0.4970 mL 0.9941 mL 2.4852 mL
    30 mM 0.0828 mL 0.4142 mL 0.8284 mL 2.0710 mL
    40 mM 0.0621 mL 0.3106 mL 0.6213 mL 1.5532 mL
    50 mM 0.0497 mL 0.2485 mL 0.4970 mL 1.2426 mL
    60 mM 0.0414 mL 0.2071 mL 0.4142 mL 1.0355 mL
    80 mM 0.0311 mL 0.1553 mL 0.3106 mL 0.7766 mL
    100 mM 0.0249 mL 0.1243 mL 0.2485 mL 0.6213 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:
    Nobiletin
    Cat. No.:
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