1. Anti-infection Metabolic Enzyme/Protease NF-κB Cell Cycle/DNA Damage
  2. Parasite Tyrosinase NF-κB CDK
  3. Kojic acid

Kojic acid is a substance produced by Aspergillus oryzae that is orally effective and can also be absorbed transdermally. Kojic acid exhibits various biological activities, including anti-aging, anti-nematode, antimicrobial, antioxidant, and anti-inflammatory effects. Kojic acid is a Tyrosinase inhibitor with an Mushroom Tyrosinase IC50 of 182.7 μM. Kojic acid prevents melanin production by capturing copper ions that bind to the tyrosinase active site, thus inhibiting its activation. Kojic acid also suppresses the NF-κB and p21 signaling pathways in human keratinocytes. Kojic acid derivatives have anticancer activity.

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Kojic acid Chemical Structure

Kojic acid Chemical Structure

CAS No. : 501-30-4

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Based on 1 publication(s) in Google Scholar

Other Forms of Kojic acid:

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

Kojic acid is a substance produced by Aspergillus oryzae that is orally effective and can also be absorbed transdermally. Kojic acid exhibits various biological activities, including anti-aging, anti-nematode, antimicrobial, antioxidant, and anti-inflammatory effects. Kojic acid is a Tyrosinase inhibitor with an Mushroom Tyrosinase IC50 of 182.7 μM. Kojic acid prevents melanin production by capturing copper ions that bind to the tyrosinase active site, thus inhibiting its activation. Kojic acid also suppresses the NF-κB and p21 signaling pathways in human keratinocytes. Kojic acid derivatives have anticancer activity[1][2][3][4][5][6][7][8].

Cellular Effect
Cell Line Type Value Description References
A-375 GI50
> 100 μM
Compound: 1; KA
Cytotoxicity against human A-375 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human A-375 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 35114540]
B16 IC50
> 50 μM
Compound: Kojic acid
Inhibition of alpha-MSH-induced melanin production in mouse B16 cells after 48 hrs
Inhibition of alpha-MSH-induced melanin production in mouse B16 cells after 48 hrs
[PMID: 20149498]
B16 IC50
> 500 μM
Compound: Kojic acid
Inhibition of alpha-MSH-stimulated melanin production in mouse B16 cells after 72 hrs by microplate reader analysis
Inhibition of alpha-MSH-stimulated melanin production in mouse B16 cells after 72 hrs by microplate reader analysis
[PMID: 26706112]
B16 IC50
111 μM
Compound: Kojic acid
Antimelanogenic activity in mouse B16 cells assessed as inhibition of intracellular melanin accumulation after 2 days
Antimelanogenic activity in mouse B16 cells assessed as inhibition of intracellular melanin accumulation after 2 days
[PMID: 19524439]
B16 IC50
15.8 μM
Compound: Kojic acid
Inhibition of alpha-MSH -stimulated melanogenesis in mouse B16 cells assessed as melanin release after 72 hrs by spectrometric analysis
Inhibition of alpha-MSH -stimulated melanogenesis in mouse B16 cells assessed as melanin release after 72 hrs by spectrometric analysis
[PMID: 21978680]
B16 IC50
39 μM
Compound: Kojic acid
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
5.5 μg/mL
Compound: Kojic acid
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
70 μM
Compound: Kojic acid
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
70 μM
Compound: Kojic acid
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
70 μM
Compound: kojic acid
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
70 μM
Compound: Kojic acid
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-F10 IC50
144.4 μM
Compound: 1a; KA
Cytotoxicity against mouse B16-F10 cells assessed as reduction in cell viability by MTT assay
Cytotoxicity against mouse B16-F10 cells assessed as reduction in cell viability by MTT assay
[PMID: 32652434]
B16-F10 IC50
500 μM
Compound: Kojic acid
Antimelanogenic activity in mouse B16F10 cells assessed as inhibition of melanin production after 4 days
Antimelanogenic activity in mouse B16F10 cells assessed as inhibition of melanin production after 4 days
[PMID: 25597012]
B16-F10 IC50
84.54 μM
Compound: Kojic acid
Inhibition of alpha-MSH-induced melanogenesis in mouse B16F10 cells after 3 days by spectrophotometric analysis
Inhibition of alpha-MSH-induced melanogenesis in mouse B16F10 cells after 3 days by spectrophotometric analysis
[PMID: 23063404]
BV-2 IC50
> 500 μM
Compound: KA
Cytotoxicity against mouse BV-2 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
Cytotoxicity against mouse BV-2 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
[PMID: 36846369]
G-361 IC50
571.17 μM
Compound: Kojic acid
Competitive inhibition of tyrosinase in human G-361 cells incubated for 10 mins measured for 2 hrs by MBTH-based spectrophotometry
Competitive inhibition of tyrosinase in human G-361 cells incubated for 10 mins measured for 2 hrs by MBTH-based spectrophotometry
[PMID: 25288494]
H9c2 IC50
> 500 μM
Compound: KA
Cytotoxicity against rat H9c2 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
Cytotoxicity against rat H9c2 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
[PMID: 36846369]
HEK293 IC50
2 μM
Compound: 6a, Kojic acid
Inhibition of human recombinant DAAO expressed in HEK293 cell lysate assessed as D-Serine conversion to H2O2 after 20 mins by spectrophotometric analysis
Inhibition of human recombinant DAAO expressed in HEK293 cell lysate assessed as D-Serine conversion to H2O2 after 20 mins by spectrophotometric analysis
[PMID: 23683589]
HFF IC50
> 150 μM
Compound: 1a; KA
Cytotoxicity against human HFF cells assessed as reduction in cell viability by MTT assay
Cytotoxicity against human HFF cells assessed as reduction in cell viability by MTT assay
[PMID: 32652434]
HT-22 IC50
> 500 μM
Compound: KA
Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
[PMID: 36846369]
L02 IC50
> 500 μM
Compound: KA
Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
[PMID: 36846369]
Melan-a IC50
1.6 mM
Compound: 1
Depigmentation activity in mouse Melan-a cells assessed as inhibition of melanin formation after 4 days
Depigmentation activity in mouse Melan-a cells assessed as inhibition of melanin formation after 4 days
[PMID: 22071299]
Melan-a IC50
1.64 mM
Compound: 1, Kojic acid
Depigmentation activity in mouse Melan-a cells after 4 days by spectrophotometry
Depigmentation activity in mouse Melan-a cells after 4 days by spectrophotometry
[PMID: 22579419]
Melan-a IC50
3.5 mM
Compound: 1
Cytotoxicity against mouse Melan-a cells by modified crystal voilet assay
Cytotoxicity against mouse Melan-a cells by modified crystal voilet assay
[PMID: 22071299]
Melan-a IC50
3.53 mM
Compound: 1, Kojic acid
Cytotoxicity against mouse Melan-a cells after 4 days by crystal voilet method
Cytotoxicity against mouse Melan-a cells after 4 days by crystal voilet method
[PMID: 22579419]
RAW264.7 IC50
> 100 μM
Compound: 1
Cytotoxicity against mouse RAW264.7 cells after 24 hrs by MTT assay
Cytotoxicity against mouse RAW264.7 cells after 24 hrs by MTT assay
[PMID: 20934336]
RAW264.7 IC50
89.41 μM
Compound: 1
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production treated for 30 mins before LPS challenge measured after 24 hrs by Griess reagent method
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production treated for 30 mins before LPS challenge measured after 24 hrs by Griess reagent method
[PMID: 20934336]
SH-SY5Y IC50
> 500 μM
Compound: KA
Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
[PMID: 36846369]
In Vitro

Kojic acid (1000 μM, 7 days) enhances the cell migration ability of HCEC cells and exhibits anti-aging activity[1].
Kojic acid (1000 μM, 7 days) may alleviate the angiogenesis of human umbilical vein endothelial cells (HUVEC), induced by senescent supernatant of HCEC cells, through NF-κB and p21 signaling pathways[1].
Kojic acid (1.4-1000 μg/mL, 3 days) exhibits dose-dependent mortality and hatch inhibition rates against Meloidogyne incognita, with EC50 values of 195.2 μg/mL and 238.3 μg/mL, respectively[4].
Kojic acid (500 or 1000 µM, 72 h) reduces tyrosinase expression in B16-4A5 and HMV-II cells, indicating that kojic acid inhibits melanogenesis by suppressing tyrosinase activity[6].
Kojic acid (10-2500 μM, 7 days) does not significantly affect the viability of HCEC cells[1].

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

Cell Viability Assay[1]

Cell Line: HCEC-B4G12 cells (human corneal endothelial cell line)
Concentration: 10, 100 , 1000, 2500, 5000 μM
Incubation Time: 7 days
Result: Did not influence the cell viability of HCEC after 7 days' treatment at 10-2500 μM but decreased the cell viability a little bit at 5000 μM.

Cell Migration Assay [1]

Cell Line: HCEC-B4G12 cells (human corneal endothelial cell line)
Concentration: 1000 μM
Incubation Time: 7 days
Result: Delayed the reduction in cell migration ability caused by aging in HCEC cells.

Western Blot Analysis[1]

Cell Line: HCEC-B4G12 cells (human corneal endothelial cell line)
Concentration: 1000 μM
Incubation Time: 7 days
Result: Inhibited the abnormal high expression of galectin 8, laminin α1, laminin α2, laminin γ1, and p21 in senescent HCEC, as well as the significant decrease in p-NF-κB protein expression.
In Vivo

Kojic acid (50 mg/kg, p.o., once daily for 3 weeks) exhibits antioxidant and anti-inflammatory activities in a mouse model of Alzheimer's disease induced by β-Amyloid (1-42), human (HY-P1363A) [8].
Kojic acid (4, 6.4, 10, 16 g/kg, p.o., single dose) does not exhibit significant toxicity in acute oral studies in JCL-Wistar rats[2].

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

Animal Model: β-Amyloid (1-42), human (HY-P1363A)-Induced Mouse Model of Alzheimer's Disease[8]
Dosage: 50 mg/kg
Administration: Oral gavage, once daily for 3 weeks
Result: Ameliorated β-Amyloid (1-42), human (HY-P1363A)-induced glial cell activation and reduced inflammatory markers in the hippocampus.
Reduced ROS and lipid peroxidase levels in Alzheimer's Disease mice model
Animal Model: JCL-Wistar rats[2]
Dosage: 4, 6.4, 10, 16 g/kg
Administration: Oral gavage (p.o.),single dose
Result: Had an oral LD50 in rats greater than 2 g/kg in acute toxicity studies[2].
Molecular Weight

142.11

Formula

C6H6O4

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C1C=C(CO)OC=C1O

Structure Classification
Initial Source

Aspergillus, Penicillium or Acetobacter spp

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (703.68 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 50 mg/mL (351.84 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 7.0368 mL 35.1840 mL 70.3680 mL
5 mM 1.4074 mL 7.0368 mL 14.0736 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* 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

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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: 5 mg/mL (35.18 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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 (17.59 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: 14.29 mg/mL (100.56 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

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)

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: 99.99%

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 7.0368 mL 35.1840 mL 70.3680 mL 175.9201 mL
5 mM 1.4074 mL 7.0368 mL 14.0736 mL 35.1840 mL
10 mM 0.7037 mL 3.5184 mL 7.0368 mL 17.5920 mL
15 mM 0.4691 mL 2.3456 mL 4.6912 mL 11.7280 mL
20 mM 0.3518 mL 1.7592 mL 3.5184 mL 8.7960 mL
25 mM 0.2815 mL 1.4074 mL 2.8147 mL 7.0368 mL
30 mM 0.2346 mL 1.1728 mL 2.3456 mL 5.8640 mL
40 mM 0.1759 mL 0.8796 mL 1.7592 mL 4.3980 mL
50 mM 0.1407 mL 0.7037 mL 1.4074 mL 3.5184 mL
60 mM 0.1173 mL 0.5864 mL 1.1728 mL 2.9320 mL
80 mM 0.0880 mL 0.4398 mL 0.8796 mL 2.1990 mL
100 mM 0.0704 mL 0.3518 mL 0.7037 mL 1.7592 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:
Kojic acid
Cat. No.:
HY-W050154
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