1. Metabolic Enzyme/Protease
  2. Tyrosinase Endogenous Metabolite
  3. Arbutin

Arbutin (β-Arbutin) is a competitive inhibitor of tyrosinase, with Kiapp values of 1.42 mM for monophenolase; 0.9 mM for diphenolase. Arbutin is also used as depigmenting agents. Arbutin is a natural polyphenol isolated from the bearberry plant Arctostaphylos uvaursi, possesses with anti-oxidant, anti-inflammatory and anti-tumor properties.

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

CAS No. : 497-76-7

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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of Arbutin:

Top Publications Citing Use of Products

    Arbutin purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2025 Oct 24.

    Cell viability after treatment with Arbutin (0–50000 μM) .

    Arbutin purchased from MedChemExpress. Usage Cited in: FEBS Open Bio. 2021 Jan;11(1):289-299.  [Abstract]

    The proliferative ability was explored using CCK‐8 kit in MG‐63 and SW1353 cells treated with 10, 20, 50, 100, 200 and 500 μm Arbutin.

    Arbutin purchased from MedChemExpress. Usage Cited in: FEBS Open Bio. 2021 Jan;11(1):289-299.  [Abstract]

    The expression of MTHFD1L, CCND1, AKT/p-AKT, and mTOR/p-mTOR in arbutin-treated osteosarcoma cells was detected by Western blotting.

    View All Endogenous Metabolite Isoform Specific Products:

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Arbutin (β-Arbutin) is a competitive inhibitor of tyrosinase, with Kiapp values of 1.42 mM for monophenolase; 0.9 mM for diphenolase. Arbutin is also used as depigmenting agents[1]. Arbutin is a natural polyphenol isolated from the bearberry plant Arctostaphylos uvaursi, possesses with anti-oxidant, anti-inflammatory and anti-tumor properties[2][3].

    IC50 & Target

    Human Endogenous Metabolite

     

    Cellular Effect
    Cell Line Type Value Description References
    B16 IC50
    116 μM
    Compound: Arbutin
    Inhibition of melanogenesis in theophylline-stimulated mouse B16-4A5 cells after 72 hrs
    Inhibition of melanogenesis in theophylline-stimulated mouse B16-4A5 cells after 72 hrs
    [PMID: 19615910]
    B16 IC50
    120 μM
    Compound: Arbutin
    Inhibition of alpha-MSH -stimulated melanogenesis in mouse B16 cells assessed as melanin release after 3 days
    Inhibition of alpha-MSH -stimulated melanogenesis in mouse B16 cells assessed as melanin release after 3 days
    [PMID: 21388810]
    B16 IC50
    140 μM
    Compound: Arbutin
    Inhibition of melanin production in alpha-MSH stimulated mouse B16 cells after 72 hrs by spectrophotometry
    Inhibition of melanin production in alpha-MSH stimulated mouse B16 cells after 72 hrs by spectrophotometry
    [PMID: 23623417]
    B16 IC50
    1550 μM
    Compound: 2
    Inhibition of tyrosinase activity in alpha-MSH-stimulated mouse B16 cells using L-tyrosine as substrate
    Inhibition of tyrosinase activity in alpha-MSH-stimulated mouse B16 cells using L-tyrosine as substrate
    [PMID: 21429753]
    B16 IC50
    180 μM
    Compound: Arbutin
    Inhibition of alpha-MSH-induced melanin production in mouse B16 cells after 72 hrs
    Inhibition of alpha-MSH-induced melanin production in mouse B16 cells after 72 hrs
    [PMID: 20044259]
    B16 IC50
    180 μM
    Compound: Arbutin
    Antimelanogenic activity in mouse B16 cells assessed as inhibition of alpha-MSH-induced melanogenesis
    Antimelanogenic activity in mouse B16 cells assessed as inhibition of alpha-MSH-induced melanogenesis
    [PMID: 20638280]
    B16 IC50
    180 μM
    Compound: Arbutin
    Inhibition of alpha-MSH-induced melanin production in mouse B16 cells after 3 days
    Inhibition of alpha-MSH-induced melanin production in mouse B16 cells after 3 days
    [PMID: 21601449]
    B16 IC50
    180 μM
    Compound: Arbutin
    Antimelanogenic activity at alpha-MSH-stimulated mouse melanoma B16 cells after 3 days by spectrophotometry
    Antimelanogenic activity at alpha-MSH-stimulated mouse melanoma B16 cells after 3 days by spectrophotometry
    [PMID: 22217872]
    B16 IC50
    180 μM
    Compound: arbutin
    Inhibition of alpha-MSH-induced melanin production in mouse B16 cells after 72 hrs
    Inhibition of alpha-MSH-induced melanin production in mouse B16 cells after 72 hrs
    [PMID: 20097083]
    B16 IC50
    247 μM
    Compound: Arbutin
    Inhibition of melanin production in alpha-MSH-stimulated mouse B16 cells incubated for 24 hrs followed by alpha-MSH stimulation for 72 hrs in presence of compound
    Inhibition of melanin production in alpha-MSH-stimulated mouse B16 cells incubated for 24 hrs followed by alpha-MSH stimulation for 72 hrs in presence of compound
    [PMID: 29526485]
    B16 IC50
    400 μM
    Compound: Arbutin
    Inhibition of alpha-MSH-stimulated melanogenesis in mouse B16 cells assessed as reduction in melanin formation
    Inhibition of alpha-MSH-stimulated melanogenesis in mouse B16 cells assessed as reduction in melanin formation
    [PMID: 28619537]
    B16 IC50
    64 μM
    Compound: Arbutin
    Inhibition of alpha-MSH-stimulated melanogenesis in mouse B16 cells assessed as reduction in melanin production incubated for 3 days
    Inhibition of alpha-MSH-stimulated melanogenesis in mouse B16 cells assessed as reduction in melanin production incubated for 3 days
    [PMID: 31387790]
    B16 IC50
    67.9 μg/mL
    Compound: Arbutin
    Inhibition of alpha-MSH-stimulated melanogenesis in mouse B16 cells assessed as melanin release after 72 hrs
    Inhibition of alpha-MSH-stimulated melanogenesis in mouse B16 cells assessed as melanin release after 72 hrs
    [PMID: 22450129]
    B16 IC50
    99 μM
    Compound: 2
    Inhibition of alpha-MSH-induced melanin synthesis in mouse B16 cells grown in a 5% CO2-95% air atmosphere after 3 days
    Inhibition of alpha-MSH-induced melanin synthesis in mouse B16 cells grown in a 5% CO2-95% air atmosphere after 3 days
    [PMID: 21429753]
    B16-4A5 IC50
    174 μM
    Compound: Arbutin
    Inhibition of theophylline-stimulated melanogenesis in mouse B16-4A5 cells after 72 hrs
    Inhibition of theophylline-stimulated melanogenesis in mouse B16-4A5 cells after 72 hrs
    [PMID: 20189399]
    B16-4A5 IC50
    174 μM
    Compound: Arbutin
    Inhibition of theophylline-induced melanogenesis in mouse B16-4A5 cells after 72 hrs by spectrophotometric analysis relative to control
    Inhibition of theophylline-induced melanogenesis in mouse B16-4A5 cells after 72 hrs by spectrophotometric analysis relative to control
    [PMID: 23376010]
    B16-4A5 IC50
    174 μM
    Compound: Arbutin
    Inhibition of melanogenesis in mouse B16-4A5 cells after 72 hrs by spectrophotometry relative to control
    Inhibition of melanogenesis in mouse B16-4A5 cells after 72 hrs by spectrophotometry relative to control
    [PMID: 24601675]
    B16-4A5 IC50
    174 μM
    Compound: Arutin
    Inhibition of melanogenesis in mouse B16-4A5 cells after 72 hrs by spectrophotometry
    Inhibition of melanogenesis in mouse B16-4A5 cells after 72 hrs by spectrophotometry
    [PMID: 23270663]
    B16-4A5 IC50
    174 μM
    Compound: arbutin
    Inhibition of melanogenesis in theophylline-stimulated mouse B16-4A5 cells after 72 hrs by microplate reader analysis
    Inhibition of melanogenesis in theophylline-stimulated mouse B16-4A5 cells after 72 hrs by microplate reader analysis
    [PMID: 25987378]
    B16-4A5 IC50
    > 1000 μM
    Compound: Arbutin
    Inhibition of theophylline-stimulated mouse B16-4A5 cell proliferation assessed as cell viability after 68 hrs by WST8 assay
    Inhibition of theophylline-stimulated mouse B16-4A5 cell proliferation assessed as cell viability after 68 hrs by WST8 assay
    [PMID: 19615910]
    B16-F1 IC50
    122 μM
    Compound: Arbutin
    Inhibition of melanin production in C57BL/6J mouse B16-F1 cells incubated for 5 days
    Inhibition of melanin production in C57BL/6J mouse B16-F1 cells incubated for 5 days
    [PMID: 27720556]
    B16-F1 IC50
    148.3 μM
    Compound: Arbutin
    Antimelanogenic activity in mouse B16-F1 cells assessed as reduction in alpha-MSH-stimulated melanin production preincubated for 72 hrs followed by alpha-MSH-stimulation and measured after 2 hrs
    Antimelanogenic activity in mouse B16-F1 cells assessed as reduction in alpha-MSH-stimulated melanin production preincubated for 72 hrs followed by alpha-MSH-stimulation and measured after 2 hrs
    [PMID: 30446440]
    B16-F1 IC50
    87.5 μM
    Compound: Arbutin
    Inhibition of tyrosinase in mouse B16-F1 cells
    Inhibition of tyrosinase in mouse B16-F1 cells
    [PMID: 30446440]
    B16-F10 IC50
    391.2 μM
    Compound: Arbutin
    Cytotoxicity against mouse B16-F10 cells assessed as reduction in cell viability incubated for 72 hrs by XTT assay
    Cytotoxicity against mouse B16-F10 cells assessed as reduction in cell viability incubated for 72 hrs by XTT assay
    [PMID: 27720556]
    Melan-a IC50
    98.05 μM
    Compound: Arbutin
    Inhibition of melanin formation in mouse Melan-a cells after 5 days by ELISA
    Inhibition of melanin formation in mouse Melan-a cells after 5 days by ELISA
    [PMID: 20022495]
    P388 IC50
    > 25 μg/mL
    Compound: 3
    Cytotoxicity against mouse P388 cells
    Cytotoxicity against mouse P388 cells
    [PMID: 9214736]
    In Vitro

    Arbutin (0.3-5.4 mM; 24 hours, 48 hours, 72 hours; B16 murine melanoma cells) inhibites the viability of B16 murine melanoma cells in a time-and dose-dependent manner[2].
    ? Arbutin (1.4-5.4 mM; 24 hours) increases the apoptosis rate of B16 murine melanoma cell of treatment at a dose of 5.4 mM[2].

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

    Cell Viability Assay[2]

    Cell Line: B16 murine melanoma cells
    Concentration: 0.3 mM, 0.7 mM, 1.4 mM, 2.1 mM, 2.9 mM, 3.6 mM, 5.4 mM
    Incubation Time: 24 hours, 48 hours or 72 hours
    Result: Inhibited the viability of B16 murine melanoma cells in a time- and dose-dependent manner.

    Apoptosis Analysis[2]

    Cell Line: B16 murine melanoma cells
    Concentration: 1.4 mM, 2.9 mM, 5.4 mM
    Incubation Time: 24 hours
    Result: Caused apoptosis in 19.3% of the cells.
    In Vivo

    Arbutin (50 mg/kg, 100 mg/kg; oral administration; every day; for 17 days; male C57BL/6 mice) pretreatment exhibits markedly protective effects on ISO-induced cardiac hypertrophy in mice[3].

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

    Animal Model: Male C57BL/6 mice ( 20-25 g)[3]
    Dosage: 50 mg/kg, 100 mg/kg
    Administration: Oral administration; every day; for 17 days
    Result: Ameliorated the ISO-induced myocardial injury.
    Clinical Trial
    Molecular Weight

    272.25

    Formula

    C12H16O7

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O[C@H]([C@H]([C@@H]([C@@H](CO)O1)O)O)[C@@H]1OC2=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 : ≥ 50 mg/mL (183.65 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 33.33 mg/mL (122.42 mM; Need ultrasonic)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.6731 mL 18.3655 mL 36.7309 mL
    5 mM 0.7346 mL 3.6731 mL 7.3462 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.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • 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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    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 (9.18 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 (9.18 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.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  PBS

      Solubility: 100 mg/mL (367.31 mM); Clear solution; Need ultrasonic

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

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    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).
    Purity & Documentation

    Purity: 99.76%

    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
    H2O / DMSO 1 mM 3.6731 mL 18.3655 mL 36.7309 mL 91.8274 mL
    5 mM 0.7346 mL 3.6731 mL 7.3462 mL 18.3655 mL
    10 mM 0.3673 mL 1.8365 mL 3.6731 mL 9.1827 mL
    15 mM 0.2449 mL 1.2244 mL 2.4487 mL 6.1218 mL
    20 mM 0.1837 mL 0.9183 mL 1.8365 mL 4.5914 mL
    25 mM 0.1469 mL 0.7346 mL 1.4692 mL 3.6731 mL
    30 mM 0.1224 mL 0.6122 mL 1.2244 mL 3.0609 mL
    40 mM 0.0918 mL 0.4591 mL 0.9183 mL 2.2957 mL
    50 mM 0.0735 mL 0.3673 mL 0.7346 mL 1.8365 mL
    60 mM 0.0612 mL 0.3061 mL 0.6122 mL 1.5305 mL
    80 mM 0.0459 mL 0.2296 mL 0.4591 mL 1.1478 mL
    100 mM 0.0367 mL 0.1837 mL 0.3673 mL 0.9183 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    Product Name:
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    Cat. No.:
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