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  3. Acacetin

Acacetin  (Synonyms: 5,7-Dihydroxy-4'-methoxyflavone)

Cat. No.: HY-N0451 Purity: 99.71%
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Acacetin (5,7-Dihydroxy-4'-methoxyflavone) is an orally active flavonoid derived from Dendranthema morifolium. Acacetin docks in the ATP binding pocket of PI3Kγ. Acacetin causes cell cycle arrest and induces apoptosis and autophagy in cancer cells. Acacetin has potent anti-cancer and anti-inflammatory activity and has the potential for pain-related diseases research.

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

CAS No. : 480-44-4

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10 mM * 1 mL in DMSO
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Customer Review

Based on 13 publication(s) in Google Scholar

Other Forms of Acacetin:

Top Publications Citing Use of Products

    Acacetin purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2025 Oct 15:148:157405.  [Abstract]

    Acacetin (ACA) (10 μM; 24 h) significantly alleviated TBHP-induced pyroptotic alterations in NPCs.

    Acacetin purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2025 Oct 15:148:157405.  [Abstract]

    Acacetin (ACA) (10 μM; 24 h) significantly inhibited TBHP-induced NPC programmed cell death.

    Acacetin purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2025 Oct 15:148:157405.  [Abstract]

    Acacetin (ACA) (10 μM; 24 h) significantly reduced ROS production in NPCs exposed to TBHP.

    Acacetin purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2025 Oct 15:148:157405.  [Abstract]

    Acacetin (ACA) (10 μM; 24 h) downregulated the expression of pyroptosis-related proteins in NPCs exposed to TBHP.

    Acacetin purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2025 Oct 15:148:157405.  [Abstract]

    Acacetin (ACA) (10 μM; 24 h) effectively restored the reduced mitochondrial membrane potential in NPCs induced by TBHP.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Acacetin (5,7-Dihydroxy-4'-methoxyflavone) is an orally active flavonoid derived from Dendranthema morifolium. Acacetin docks in the ATP binding pocket of PI3Kγ. Acacetin causes cell cycle arrest and induces apoptosis and autophagy in cancer cells. Acacetin has potent anti-cancer and anti-inflammatory activity and has the potential for pain-related diseases research[1][2].

    Cellular Effect
    Cell Line Type Value Description References
    A-431 IC50
    4 x 10-1 μg/mL
    Compound: 39
    Inhibition of EGFR in human A431 cells
    Inhibition of EGFR in human A431 cells
    [PMID: 1479375]
    A549 IC50
    0.4 μg/mL
    Compound: Acacetin
    Cytotoxicity against human A549 cells by SRB assay
    Cytotoxicity against human A549 cells by SRB assay
    [PMID: 31784199]
    HCT-15 IC50
    0.4 μg/mL
    Compound: Acacetin
    Cytotoxicity against human HCT15 cells by SRB assay
    Cytotoxicity against human HCT15 cells by SRB assay
    [PMID: 31784199]
    KB ED50
    > 100 μg/mL
    Compound: NSC-76061
    Cytotoxicity against human KB cells
    Cytotoxicity against human KB cells
    [PMID: 469554]
    MOLM-13 IC50
    9.1 μM
    Compound: 28
    Cytotoxicity against human MOLM-13 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
    Cytotoxicity against human MOLM-13 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
    [PMID: 33393294]
    MV4-11 IC50
    6.8 μM
    Compound: 28
    Cytotoxicity against human MV4-11 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
    Cytotoxicity against human MV4-11 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
    [PMID: 33393294]
    Monocyte IC50
    22 μM
    Compound: Acacetin
    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]
    Neutrophil IC50
    7 μM
    Compound: 4d
    Inhibition of oxidative burst in PMA-stimulated human neutrophils assessed as inhibition of superoxide anion radical-induced lucigenin oxidation incubated for 5 mins prior to PMA challenge by chemiluminescence assay
    Inhibition of oxidative burst in PMA-stimulated human neutrophils assessed as inhibition of superoxide anion radical-induced lucigenin oxidation incubated for 5 mins prior to PMA challenge by chemiluminescence assay
    [PMID: 23871908]
    RAW264.7 CC50
    60.9 μM
    Compound: 17
    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
    27.7 μM
    Compound: 27
    Inhibition of LPS-stimulated nitric oxide production in mouse RAW264.7 cells by Greiss method
    Inhibition of LPS-stimulated nitric oxide production in mouse RAW264.7 cells by Greiss method
    [PMID: 27955927]
    RAW264.7 IC50
    5.9 μM
    Compound: 17
    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
    53.7 μM
    Compound: 27
    Inhibition of LPS/INF-gamma-stimulated nitric oxide production in mouse RAW264.7 cells by Greiss method
    Inhibition of LPS/INF-gamma-stimulated nitric oxide production in mouse RAW264.7 cells by Greiss method
    [PMID: 27955927]
    RAW264.7 IC50
    6.2 μM
    Compound: 11
    Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as decrease in PGE2 production preincubated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA
    Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as decrease in PGE2 production preincubated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA
    [PMID: 31747281]
    SK-MEL-2 IC50
    0.4 μg/mL
    Compound: Acacetin
    Cytotoxicity against human SK-MEL-2 cells by SRB assay
    Cytotoxicity against human SK-MEL-2 cells by SRB assay
    [PMID: 31784199]
    SK-OV-3 IC50
    0.4 μg/mL
    Compound: Acacetin
    Cytotoxicity against human SKOV3 cells by SRB assay
    Cytotoxicity against human SKOV3 cells by SRB assay
    [PMID: 31784199]
    XF498 IC50
    0.4 μg/mL
    Compound: Acacetin
    Cytotoxicity against human XF498 cells by SRB assay
    Cytotoxicity against human XF498 cells by SRB assay
    [PMID: 31784199]
    In Vitro

    Acacetin (5,7-Dihydroxy-4'-methoxyflavone; 10-200 μM; 24 hours) decreases cell viabilities in a dose-dependent manner. Acacetin has little effect on human normal glial cell line HEB and non-tumorigenic epithelial cell line MCF-10A[1].
    Acacetin (50-150 μM; 24 hours) causes G2/M cell cycle arrest and induces apoptosis and autophagy[1].
    Acacetin (50-150 μM; 24 hours) leads to decreases in levels of PI3Kγ-p110, p-AKT, p-mTOR, p-p70S6K, and p-ULK in a dose-dependent manner[1].

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

    Cell Viability Assay[1]

    Cell Line: Breast cancer MCF-7 cells, hepatocellular carcinoma SMMC-7721 cells, lung adenocarcinoma A549 cells, esophageal carcinoma Eca109 cells
    Concentration: 10, 20, 40, 60, 80, 100, 150, 200 μM
    Incubation Time: 24 hours
    Result: Decreased cancer cell viabilities in a dose-dependent manner.
    Had IC50 values of 82.75 μM, 103.9 μM, 157.4 μM, 54.7 μM in MDA-MB-231, MCF-7, A549, Eca109 cells, respectively.

    Cell Cycle Analysis[1]

    Cell Line: MDA-MB-231 cells
    Concentration: 50, 100, 150 μM
    Incubation Time: 24 hours
    Result: Resulted in increase in percentage of cells at G2/M phase and decrease in percentage of cells at G1 and S phase in a dose-dependent manner.

    Apoptosis Analysis[1]

    Cell Line: MDA-MB-231 cells
    Concentration: 50, 100, 150 μM
    Incubation Time: 24 hours
    Result: Induced apoptosis.

    Cell Autophagy Assay[1]

    Cell Line: MDA-MB-231 cells
    Concentration: 50, 100, 150 μM
    Incubation Time: 24 hours
    Result: Induced autophagy.
    Resulted in marked increases in EGFP-LC3 puncta formation and a dose-dependent accumulation of LC3-II.

    Western Blot Analysis[1]

    Cell Line: MDA-MB-231 cells
    Concentration: 50, 100, 150 μM
    Incubation Time: 24 hours
    Result: Resulted in decrease in levels of Bcl-2 and Bcl-xL and increase in levels of p53.
    Led to decreases in levels of PI3Kγ-p110, p-AKT, p-mTOR, p-p70S6K, and p-ULK in a dose-dependent manner.
    Had little or no effect on expression of PI3Kα, PI3Kβ, PI3Kδ, p-ERK, p-p38, and p-JNK.
    In Vivo

    Acacetin (5,7-Dihydroxy-4'-methoxyflavone; 5, 20 mg/kg/day; orally; for 3 days) significantly suppresses microglial activation in an LPS-induced neuroinflammation mouse model[2].
    Acacetin (25 mg/kg/day; orally; for 3 days) reduces neuronal cell death in an animal model of ischemia[2].
    Acacetin (1.8-56.2 mg/kg/day; ip; single dose) decreases visceral and inflammatory nociception and prevented the formalin-induced oedema[3].

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

    Animal Model: Male C57BL/6 mice, 7 weeks of age[2]
    Dosage: 5, 20 mg/kg
    Administration: Orally; once a day for 3 days
    Result: Significantly suppressed microglial activation in an LPS-induced (ip; 5mg/kg) neuroinflammation mouse model.
    Molecular Weight

    284.26

    Formula

    C16H12O5

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C1C=C(C2=CC=C(OC)C=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 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 125 mg/mL (439.74 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 3.5179 mL 17.5895 mL 35.1791 mL
    5 mM 0.7036 mL 3.5179 mL 7.0358 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.

    • 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    90% Corn Oil

      Solubility: ≥ 2.08 mg/mL (7.32 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

    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:  50% PEG300    50% Saline

      Solubility: 5 mg/mL (17.59 mM); Suspended solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  0.5% CMC-Na/saline water

      Solubility: 10 mg/mL (35.18 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: 99.71%

    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
    DMSO 1 mM 3.5179 mL 17.5895 mL 35.1791 mL 87.9477 mL
    5 mM 0.7036 mL 3.5179 mL 7.0358 mL 17.5895 mL
    10 mM 0.3518 mL 1.7590 mL 3.5179 mL 8.7948 mL
    15 mM 0.2345 mL 1.1726 mL 2.3453 mL 5.8632 mL
    20 mM 0.1759 mL 0.8795 mL 1.7590 mL 4.3974 mL
    25 mM 0.1407 mL 0.7036 mL 1.4072 mL 3.5179 mL
    30 mM 0.1173 mL 0.5863 mL 1.1726 mL 2.9316 mL
    40 mM 0.0879 mL 0.4397 mL 0.8795 mL 2.1987 mL
    50 mM 0.0704 mL 0.3518 mL 0.7036 mL 1.7590 mL
    60 mM 0.0586 mL 0.2932 mL 0.5863 mL 1.4658 mL
    80 mM 0.0440 mL 0.2199 mL 0.4397 mL 1.0993 mL
    100 mM 0.0352 mL 0.1759 mL 0.3518 mL 0.8795 mL
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      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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