2. MAPK/ERK Pathway Autophagy Apoptosis
  3. p38 MAPK Autophagy Apoptosis
  4. Hesperetin

Hesperetin is a natural flavanone, and acts as a potent and broad-spectrum inhibitor against human UGT activity. Hesperetin regulates apoptosis.

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

Hesperetin Chemical Structure

Hesperetin Chemical Structure

CAS No. : 520-33-2

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Customer Review

Based on 17 publication(s) in Google Scholar

Other Forms of Hesperetin:

Hesperetin Related Antibodies

Top Publications Citing Use of Products

    Hesperetin purchased from MedChemExpress. Usage Cited in: Nutr Cancer. 2020;72(3):538-545.  [Abstract]

    U-251 cells are cultured with indicated concentration of Hesperetin for 24 h. Then the cells are stained with DAPI and observed under a fluorescence microscope.

    Hesperetin purchased from MedChemExpress. Usage Cited in: Nutr Cancer. 2020;72(3):538-545.  [Abstract]

    The expression of Bax and Bcl-2 was examined by western blotting. GAPDH was served as a loading control.

    Hesperetin purchased from MedChemExpress. Usage Cited in: Nutr Cancer. 2020;72(3):538-545.  [Abstract]

    p38 MAPK activation is involved in Hesperetin-induced apoptosis. The phosphorylation of p38 MAPK, JNK, and ERK in U-21 cells treated with hesperetin is analyzed by western blotting.

    Hesperetin purchased from MedChemExpress. Usage Cited in: Nutr Cancer. 2020;72(3):538-545.  [Abstract]

    Hesperetin induced G2/M arrest in GBM cell. Cells are treated with vehicle or various doses of hesperetin for 24 h. Whole cell lysates are immunoblotted with indicated antibodies. The protein levels of p21, CDK1, and cyclin B1 are measured by western blotting.

    View All p38 MAPK Isoform Specific Products:

    View All Isoforms
    p38 MAPK p38α p38β MAPK13 p38δ p38γ

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Hesperetin is a natural flavanone, and acts as a potent and broad-spectrum inhibitor against human UGT activity. Hesperetin regulates apoptosis.

    Cellular Effect
    Cell Line Type Value Description References
    BJ EC50
    > 10 μM
    Compound: 3
    Cytotoxicity against human BJ cells assessed as viable cells after 72 hrs by calcein AM assay
    Cytotoxicity against human BJ cells assessed as viable cells after 72 hrs by calcein AM assay
    		[PMID: 20192247]
    Caco-2 IC50
    66.67 μM
    Compound: 28
    Cytotoxicity in human Caco2 cells after 72 hrs by MTT assay
    Cytotoxicity in human Caco2 cells after 72 hrs by MTT assay
    		[PMID: 28793973]
    CCRF-CEM EC50
    > 10 μM
    Compound: 3
    Cytotoxicity against human CEM cells assessed as viable cells after 72 hrs by calcein AM assay
    Cytotoxicity against human CEM cells assessed as viable cells after 72 hrs by calcein AM assay
    		[PMID: 20192247]
    HCT-116 GI50
    36.1 μM
    Compound: Hesperetin
    Anticlonogenic activity in human HCT116 cells after 6 days by crystal violet staining based assay
    Anticlonogenic activity in human HCT116 cells after 6 days by crystal violet staining based assay
    		[PMID: 27840137]
    HeLa EC50
    > 10 μM
    Compound: 3
    Cytotoxicity against human HeLa cells assessed as viable cells after 72 hrs by calcein AM assay
    Cytotoxicity against human HeLa cells assessed as viable cells after 72 hrs by calcein AM assay
    		[PMID: 20192247]
    MCF7 EC50
    > 10 μM
    Compound: 3
    Cytotoxicity against human MCF7 cells assessed as viable cells after 72 hrs by calcein AM assay
    Cytotoxicity against human MCF7 cells assessed as viable cells after 72 hrs by calcein AM assay
    		[PMID: 20192247]
    Monocyte IC50
    2.1 μM
    Compound: hesperetin
    Inhibition of procoagulant activity in monocyte from human blood assessed as counteraction of IL1-induced tissue factor expression after 18 hrs
    Inhibition of procoagulant activity in monocyte from human blood assessed as counteraction of IL1-induced tissue factor expression after 18 hrs
    		[PMID: 8882428]
    PC-3 IC50
    40 μM
    Compound: Hesperetin
    Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay
    Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay
    		[PMID: 31398616]
    PC-3 IC50
    90 μM
    Compound: Hesperetin
    Antiproliferative activity against human PC3 cells after 24 hrs by MTT assay
    Antiproliferative activity against human PC3 cells after 24 hrs by MTT assay
    		[PMID: 31398616]
    RAW264.7 CC50
    > 100 μM
    Compound: 16
    Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
    Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
    		[PMID: 33667099]
    RAW264.7 IC50
    31.2 μM
    Compound: 16
    Inhibition of LPS induced NO production in mouse RAW264.7 cells measured after 24 hrs by Griess reagent based assay
    Inhibition of LPS induced NO production in mouse RAW264.7 cells measured after 24 hrs by Griess reagent based assay
    		[PMID: 33667099]
    RAW264.7 IC50
    48.59 μM
    Compound: 1; Hes
    Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production preincubated for 2 hrs followed by LPS stimulation and measured after 24 hrs by Griess method
    Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production preincubated for 2 hrs followed by LPS stimulation and measured after 24 hrs by Griess method
    		[PMID: 33493826]
    RPMI-8226 EC50
    > 10 μM
    Compound: 3
    Cytotoxicity against human RPMI8226 cells assessed as viable cells after 72 hrs by calcein AM assay
    Cytotoxicity against human RPMI8226 cells assessed as viable cells after 72 hrs by calcein AM assay
    		[PMID: 20192247]
    THP-1 EC50
    > 10 μM
    Compound: 3
    Cytotoxicity against human THP1 cells after 72 hrs by erythosin B staining method
    Cytotoxicity against human THP1 cells after 72 hrs by erythosin B staining method
    		[PMID: 20192247]
    U-266 EC50
    > 10 μM
    Compound: 3
    Cytotoxicity against human U266 cells assessed as viable cells after 72 hrs by calcein AM assay
    Cytotoxicity against human U266 cells assessed as viable cells after 72 hrs by calcein AM assay
    		[PMID: 20192247]
    Vero IC50
    8.3 μM
    Compound: Hesperetin
    Inhibition of SARS coronavirus 3C-like protease cis-cleavage activity transfected in african green monkey Vero cells by luciferase reporter gene assay
    Inhibition of SARS coronavirus 3C-like protease cis-cleavage activity transfected in african green monkey Vero cells by luciferase reporter gene assay
    		[PMID: 23647823]
    In Vitro

    Hesperetin has the retention of antioxidant potential in self nano-emulsifying drug delivery system[1]. Hesperetin and NGR display broad-spectrum inhibition against human UGTs. Besides, Hesperetin exhibits strong inhibitory effects on UGT1A1, 1A3 and 1A9 (both IC50 and Ki values lower than 10 μM) and moderately inhibits UGT1A4, UGT1A7, UGT1A8 (IC50 values 29.68-63.87 μM)[2]. Hesperetin interacts with different types of proteins involving hydrogen bonds, pi-pi effects, pi-cation bonding and pi-sigma interactions with varying binding energies. Hesperetin exhibits drug-like properties which projects its potential as a therapeutic option for CHIKV infection[3]. Hesperetin dose-dependently reduces GCDCA-induced caspase-3 activity in cultured primary rat hepatocytes. Hesperetin also dose-dependently reduces CM-induced Nos2 (iNOS) expression in hepatocytes. Interestingly, hesperetin-induced expression of the antioxidant gene haem oxygenase 1 (HO-1) about fourfold compared with cytokine mixture alone[5].

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

    Hesperetin Related Antibodies
    In Vivo

    Preadministration of Hesperetin (40 mg/kg b.w., oral) significantly attenuates the Cd-induced oxidative stress and mitochondrial dysfunction, restores the antioxidant and membrane-bound enzyme activities and decreases apoptosis in the brain of rats[4]. Hesperetin (200 mg/kg) attenuates Con A-induced hepatocyte apoptosis and hepatic Nos2 (iNOS) expression in mice. Hesperetin co-treatment also decreases the occurrence of apoptotic bodies, hydropic degeneration, nuclear fragments, autolysis and haemorrhage. The number of leukocytes infiltrated in liver tissue of mice with D-GalN/LPS-induced fulminant hepatitis are significantly decreased by hesperetin in a murine model[5].

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

    302.28

    Formula

    C16H14O6
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C1C[C@@H](C2=CC=C(OC)C(O)=C2)OC3=CC(O)=CC(O)=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 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 125 mg/mL (413.52 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 3.3082 mL 16.5410 mL 33.0819 mL
    5 mM 0.6616 mL 3.3082 mL 6.6164 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.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    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 (8.27 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 (8.27 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:  0.5% CMC/saline water

      Solubility: 20 mg/mL (66.16 mM); Suspended 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.
    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
    References
    Kinase Assay
    [4]

    First, 0.5 mL tissue homogenate is diluted with 1 mL water. Then, to this mixture, 2.5 mL ethanol and 1.5 mL chloroform (all reagents chilled) are added and shaken for 1 min at 4°C, then centrifuged. The enzyme activity in the supernatant is determined. The assay mixture contained 1.2 mL sodium pyrophosphate buffer (0.025 M, pH 8.3), 0.1 mL 186 mM phenazine methosulfate (PMS), 0.3 mL 30 mM Nitroblue tetrazolium (NBT), and 0.2 mL of nicotinamide adenine dinucleotide (NADH), and appropriately diluted enzyme preparation and water in a total volume of 3 mL. Reaction is initiated by the addition of NADH. After incubation at 30°C for 90 min, the reaction is stopped by the addition of 1 mL glacial acetic acid. The reaction mixture is stirred vigorously and shaken with 4 mL n-butanol. The intensity of the chromogen in the butanol layer is measured at 560 nm against a butanol blank. A system without enzyme served as control. One unit of enzyme activity is defined as 50% inhibition of NBT reduction in 1 min under the assay conditions.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [4]

    After 7 days of adjusting, the animals are randomly divided into 10 experimental groups. Control group (n=8): These animals are treated with the equivalent volume of PBS as used for the administration of Con A and D-GalN/LPS. Control hesperetin group (n=8): The mice are treated with hesperetin 400 mg/kg p.o. in 0.5% sodium carboxymethylcellulose (CMC-Na) solution for 10 days. Con A group (n=15): The animals are treated with the same volume of CMC-Na as used for administration of hesperetin for 10 days and are challenged with Con A (i.v.15 mg/kg). Con A + hesperetin groups: The animals receive various doses of hesperetin (100, 200, 400 mg/kg) p.o. for 10 days before Con A injection (each group n=15). D-GalN/LPS group (n=15): The animals are given CMC-Na for 10 days and injected i.p. with D-GalN (700 mg/kg)/LPS (5 μg/kg). D-GalN/LPS + hesperetin groups: Three doses of hesperetin (100, 200, 400 mg/kg) are given to mice once daily for 10 days. D-GalN (700 mg/kg)/LPS (5 μg/kg) are injected i.p. (each group n=15).

    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, 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
    DMSO 1 mM 3.3082 mL 16.5410 mL 33.0819 mL 82.7048 mL
    5 mM 0.6616 mL 3.3082 mL 6.6164 mL 16.5410 mL
    10 mM 0.3308 mL 1.6541 mL 3.3082 mL 8.2705 mL
    15 mM 0.2205 mL 1.1027 mL 2.2055 mL 5.5137 mL
    20 mM 0.1654 mL 0.8270 mL 1.6541 mL 4.1352 mL
    25 mM 0.1323 mL 0.6616 mL 1.3233 mL 3.3082 mL
    30 mM 0.1103 mL 0.5514 mL 1.1027 mL 2.7568 mL
    40 mM 0.0827 mL 0.4135 mL 0.8270 mL 2.0676 mL
    50 mM 0.0662 mL 0.3308 mL 0.6616 mL 1.6541 mL
    60 mM 0.0551 mL 0.2757 mL 0.5514 mL 1.3784 mL
    80 mM 0.0414 mL 0.2068 mL 0.4135 mL 1.0338 mL
    100 mM 0.0331 mL 0.1654 mL 0.3308 mL 0.8270 mL
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    Hesperetin 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:

    Hesperetin520-33-2p38 MAPKAutophagyApoptosisInhibitorinhibitorinhibit

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