2. Autophagy Metabolic Enzyme/Protease
  3. Autophagy Cytochrome P450 Endogenous Metabolite
  4. Apigenin

Apigenin  (Synonyms: 4',5,7-Trihydroxyflavone; Apigenol; C.I. Natural Yellow 1)

Cat. No.: HY-N1201 Purity: 99.58%
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Apigenin (4',5,7-Trihydroxyflavone) is a competitive CYP2C9 inhibitor with a Ki of 2 μM.

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

Apigenin Chemical Structure

Apigenin Chemical Structure

CAS No. : 520-36-5

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 61 In-stock
Solution
10 mM * 1 mL in DMSO USD 61 In-stock
Solid
5 mg USD 35 In-stock
10 mg USD 55 In-stock
50 mg USD 72 In-stock
100 mg USD 121 In-stock
200 mg USD 176 In-stock
500 mg USD 264 In-stock
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Based on 31 publication(s) in Google Scholar

Other Forms of Apigenin:

Apigenin Related Antibodies

Top Publications Citing Use of Products

    Apigenin purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Oct 29;37(1):261.   [Abstract]

    The protein expression levels of cleaved PARP are detected from Curcumin and Apigenin-treated A375, A2058, and RPMI-7951 cell lysates compared to control samples using Western blotting analyses.

    Apigenin purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Oct 29;37(1):261.   [Abstract]

    A375 cells are incubated with DMSO, curcumin (25 μM), or apigenin (30 μM) for 4 h and then treated with IFN-γ (10 ng/mL) for indicated times. The levels of STAT1 phosphorylation at Tyr701 and total STAT1 are detected by Western blot analysis.

    Apigenin purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Oct 29;37(1):261.   [Abstract]

    A375, A2058, and RPMI-7951 cells were treated with DMSO (control), Curcumin (25 μM), or Apigenin (30 μM) for 24 h. Apigenin and Curcumin induce apoptosis in melanoma cells.

    Apigenin purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Oct 29;37(1):261.   [Abstract]

    Western analysis of PD-L1 expression in A375, A2058, and RPMI-7951 cells treated with IFN-γ, curcumin, or apigenin.

    Apigenin purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Oct 29;37(1):261.   [Abstract]

    A375 cells are incubated with DMSO, curcumin (25 μM), or apigenin (30 μM) for 4 h and then treated with IFN-γ (10 ng/mL) for indicated times. The levels of STAT1 phosphorylation at Tyr701 and total STAT1 are detected by Western blot analysis.

    Apigenin purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Oct 29;37(1):261.   [Abstract]

    A375 cells are incubated with DMSO, curcumin (25 μM), or apigenin (30 μM) for 4 h and then treated with IFN-γ (10 ng/mL) for indicated times. The levels of STAT1 phosphorylation at Tyr701 and total STAT1 are detected by Western blot analysis.

    View All Cytochrome P450 Isoform Specific Products:

    View All Isoforms
    CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Apigenin (4',5,7-Trihydroxyflavone) is a competitive CYP2C9 inhibitor with a Ki of 2 μM.

    IC50 & Target

    CYP2

     

    In Vitro

    Apigenin (4',5,7-Trihydroxyflavone) inhibits cytochrome P450 2C9 (CYP2C9) with a Ki of 2 μM in the CYP2C9 RECO system (a purified, reconstituted enzyme system containing recombinant human CYP2C9, P450 reductase, cytochrome b5, and liposomes)[1]. Apigenin inhibits cell proliferation. The growth inhibition rate (IR) of 20, 40, and 80 μM of Apigenin is 38%, 71%, and 99% respectively on the 7thd. after exposure to Apigenin for 24 or 48 h, the clone formation of SGC-7901 cells is suppressed in a dose- and time-dependent manner. The cloning efficiency in 80 μM is 9.8% and 5% after treatment with Apigenin for 24 and 48 h, while in the control group, it is 40.4% and 43.4%[2].

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

    Apigenin Related Antibodies
    In Vivo

    Apigenin (4',5,7-Trihydroxyflavone), a natural flavonoid, possesses a broad spectrum of biological properties, including antioxidative, anti-inflammatory, anticancer, and neuroprotective effects. Apigenin (125 mg/kg and 250 mg/kg) alleviates Adriamycin (ADR) (24 mg/kg)-induced myocardial injury. Apigenin inhibits serum aspartate amino transferase (AST) release. Apigenin reduces serum lactate dehydrogenase (LDH) release. Apigenin reduces serum creatine kinase (CK) contents[3].

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

    270.24

    Formula

    C15H10O5
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to green yellow

    SMILES

    OC1=C2C(OC(C3=CC=C(O)C=C3)=CC2=O)=CC(O)=C1
    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 : 83.33 mg/mL (308.36 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.7004 mL 18.5021 mL 37.0041 mL
    5 mM 0.7401 mL 3.7004 mL 7.4008 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    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (7.70 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 (7.70 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.

    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-Na/saline water

      Solubility: 10 mg/mL (37.00 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

    Purity: 99.58%

    COA (259 KB) HNMR (117 KB) LCMS (96 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [2]

    The effect of Apigenin on the viability of cells is determined by MTT assay. Near-confluent stock cultures of human gastric cancer SGC-7901 cells are harvested with 0.2% EDTA and plated at a density of 2.5×103/well in 96-well microtiter plates. After an overnight incubation to allow cell attachment, the medium is replaced by fresh medium containing different concentrations (0, 20, 40, and 80 μM) of Apigenin. Control wells receive DMSO (0.2%). Each concentration of Apigenin is repeated in four wells. After incubation for 24 h, one plate is assayed with a microplate reader at the wavelength of 570 nm. Before the assay, MTT (5 mg/mL in PBS) is added to each well and incubated for 4 h, then MTT solution is removed from the wells by aspiration. After careful removal of the medium, 0.1 mL of DMSO is added to each well, and the plate is shaken for 15 min. The data of 7 d are fed into the computer and the growth curve is drawn. The growth inhibition rate (IR) is calculated[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [3]

    Mice[3]
    Sixty healthy Kunming mice (26±2 g) are randomly assigned into two groups: a control group (n=15) and an ADR group (n=45). The ADR group is divided into three subgroups: ADR only without Apigenin (ADR, n=15), low-dose Apigenin (125 mg/kg/day, n=15), and high-dose Apigenin (250 mg/kg/day, n=15). All Apigenin-treated groups are treated daily via gastric gavage for seventeen days with a 125 or 250 mg/kg/day dose. ADR (3 mg/kg/day) is injected intraperitoneally into animals at an interval of 48 h (in total, eight times at a cumulative dose of 24 mg/kg). The mice in the control group receive injections of 0.9% sterile saline. On the 17th day after the first treatment, the mice are sacrificed, and blood samples are collected. A number of hearts are fixed with 2.5% glutaraldehyde fixative for electron microscopy analysis, and the others are stored at -80°C for western blot analysis.

    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, 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 3.7004 mL 18.5021 mL 37.0041 mL 92.5104 mL
    5 mM 0.7401 mL 3.7004 mL 7.4008 mL 18.5021 mL
    10 mM 0.3700 mL 1.8502 mL 3.7004 mL 9.2510 mL
    15 mM 0.2467 mL 1.2335 mL 2.4669 mL 6.1674 mL
    20 mM 0.1850 mL 0.9251 mL 1.8502 mL 4.6255 mL
    25 mM 0.1480 mL 0.7401 mL 1.4802 mL 3.7004 mL
    30 mM 0.1233 mL 0.6167 mL 1.2335 mL 3.0837 mL
    40 mM 0.0925 mL 0.4626 mL 0.9251 mL 2.3128 mL
    50 mM 0.0740 mL 0.3700 mL 0.7401 mL 1.8502 mL
    60 mM 0.0617 mL 0.3084 mL 0.6167 mL 1.5418 mL
    80 mM 0.0463 mL 0.2313 mL 0.4626 mL 1.1564 mL
    100 mM 0.0370 mL 0.1850 mL 0.3700 mL 0.9251 mL
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    Apigenin 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:

    Apigenin520-36-54',5,7-Trihydroxyflavone Apigenol C.I. Natural Yellow 1AutophagyCytochrome P450Endogenous MetaboliteCYPsInhibitorinhibitorinhibit

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