1. JAK/STAT Signaling
  2. Pim
  3. Hispidulin

Hispidulin is a natural flavone with a broad spectrum of biological activities. Hispidulin is a Pim-1 inhibitor with an IC50 of 2.71 μM.

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

CAS No. : 1447-88-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of Hispidulin:

Top Publications Citing Use of Products

    Hispidulin purchased from MedChemExpress. Usage Cited in: J Transl Med. 2025 Oct 7;23(1):1062.  [Abstract]

    Human osteosarcoma MG63 and 143B cells treated with various concentrations (20–60 µM) of HIS (Hispidulin) for 24, 48, and 72 h, as determined by the CCK-8 assay.

    Hispidulin purchased from MedChemExpress. Usage Cited in: J Transl Med. 2025 Oct 7;23(1):1062.  [Abstract]

    The effects of HIS (Hispidulin) (7.5-30 µM) on the migration and invasion abilities of MG63 and 143B cells were examined by Transwell assays.

    Hispidulin purchased from MedChemExpress. Usage Cited in: J Transl Med. 2025 Oct 7;23(1):1062.  [Abstract]

    Hispidulin (HIS) (7.5-15 µM; 48 h). Western blot analysis of the expression levels of G2/M phase-related proteins (CDK1, Cyclin B1), apoptosis-related protein (Bcl-2), and epithelial-mesenchymal transition (EMT)-related proteins (E-cadherin, N-cadherin, Vimentin) in MG63 and 143B cells. β-actin served as a loading control.

    Hispidulin purchased from MedChemExpress. Usage Cited in: J Transl Med. 2025 Oct 7;23(1):1062.  [Abstract]

    Apoptosis in MG63 and 143B cells after HIS (Hispidulin) (7.5-30 µM; 48 h) treatment was detected by Annexin V-FITC/PI double staining followed by flow cytometry.

    Hispidulin purchased from MedChemExpress. Usage Cited in: J Transl Med. 2025 Oct 7;23(1):1062.  [Abstract]

    Changes in intracellular free fatty acid (FFA) concentration and fatty acid synthase (FASN) activity in MG63 and 143B cells after HIS (Hispidulin) (15 µM; 48 h) treatment.

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    • Biological Activity

    • Protocol

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    • References

    • Customer Review

    Description

    Hispidulin is a natural flavone with a broad spectrum of biological activities. Hispidulin is a Pim-1 inhibitor with an IC50 of 2.71 μM.

    IC50 & Target

    IC50: 2.71 μM (Pim-1)[1]

    Cellular Effect
    Cell Line Type Value Description References
    A-431 ED50
    1.2 μg/mL
    Compound: hispidulin
    Cytotoxicity against human A431 cells
    Cytotoxicity against human A431 cells
    [PMID: 10579870]
    BC1 cell line ED50
    >20 μg/mL
    Compound: hispidulin
    Cytotoxicity against human BC1 cells
    Cytotoxicity against human BC1 cells
    [PMID: 10579870]
    BC1 cell line ED50
    19 μg/mL
    Compound: hispidulin
    Cytotoxicity against human BC1 cells
    Cytotoxicity against human BC1 cells
    [PMID: 7931367]
    Col2 ED50
    >20 μg/mL
    Compound: hispidulin
    Cytotoxicity against human Col2 cells
    Cytotoxicity against human Col2 cells
    [PMID: 10579870]
    Col2 ED50
    >20 μg/mL
    Compound: hispidulin
    Cytotoxicity against human Col2 cells
    Cytotoxicity against human Col2 cells
    [PMID: 7931367]
    HEK293 EC50
    7.3 μM
    Compound: 12
    Agonist activity at mouse PPARgamma expressed in HEK293 cells co-expressing with Gal4 reporter vector after 24 hrs by dual-luciferase reporter assay
    Agonist activity at mouse PPARgamma expressed in HEK293 cells co-expressing with Gal4 reporter vector after 24 hrs by dual-luciferase reporter assay
    [PMID: 24955889]
    HT ED50
    10.1 μg/mL
    Compound: hispidulin
    Cytotoxicity against human HT cells
    Cytotoxicity against human HT cells
    [PMID: 10579870]
    HT-1080 ED50
    5.2 μg/mL
    Compound: hispidulin
    Cytotoxicity against human HT1080 cells
    Cytotoxicity against human HT1080 cells
    [PMID: 7931367]
    Huh-7 CC50
    >50 μM
    Compound: 14
    Cytotoxicity against human Huh7.5.1 cells by MTT assay
    Cytotoxicity against human Huh7.5.1 cells by MTT assay
    [PMID: 22445328]
    Huh-7 EC50
    36.3 μM
    Compound: 14
    Antiviral activity against HCV JFH-1 J399EM infected in Human Huh7.5.1 cells assessed as suppression of viral replication after 72 hrs by EGFP assay
    Antiviral activity against HCV JFH-1 J399EM infected in Human Huh7.5.1 cells assessed as suppression of viral replication after 72 hrs by EGFP assay
    [PMID: 22445328]
    KB ED50
    18.8 μg/mL
    Compound: hispidulin
    Cytotoxicity against human KB cells
    Cytotoxicity against human KB cells
    [PMID: 10579870]
    KB ED50
    22 μg/mL
    Compound: NSC-122415
    Cytotoxicity against human KB cells
    Cytotoxicity against human KB cells
    [PMID: 469554]
    KB ED50
    5.6 μg/mL
    Compound: hispidulin
    Cytotoxicity against human KB cells
    Cytotoxicity against human KB cells
    [PMID: 7931367]
    KB ED50
    96 μg/mL
    Compound: 6
    Cytotoxicity against human KB cells
    Cytotoxicity against human KB cells
    10.1021/np50005a002
    KB-V1 ED50
    1.3 μg/mL
    Compound: hispidulin
    Cytotoxicity against human multidrug-resistant KB-V1+ cells in presence of vinblastine
    Cytotoxicity against human multidrug-resistant KB-V1+ cells in presence of vinblastine
    [PMID: 10579870]
    KB-V1 ED50
    2.8 μg/mL
    Compound: hispidulin
    Cytotoxicity against human KBV1 cells
    Cytotoxicity against human KBV1 cells
    [PMID: 7931367]
    KB-V1 ED50
    8.7 μg/mL
    Compound: hispidulin
    Cytotoxicity against human multidrug-resistant KBV1 cells in absence of vinblastine
    Cytotoxicity against human multidrug-resistant KBV1 cells in absence of vinblastine
    [PMID: 10579870]
    LNCaP ED50
    7.1 μg/mL
    Compound: hispidulin
    Cytotoxicity against hormone-dependent human LNCaP cells
    Cytotoxicity against hormone-dependent human LNCaP cells
    [PMID: 10579870]
    Lu1 ED50
    >20 μg/mL
    Compound: hispidulin
    Cytotoxicity against human Lu1 cells
    Cytotoxicity against human Lu1 cells
    [PMID: 10579870]
    Lu1 ED50
    17.6 μg/mL
    Compound: hispidulin
    Cytotoxicity against human Lu1 cells
    Cytotoxicity against human Lu1 cells
    [PMID: 7931367]
    MDCK CC50
    172.46 μM
    Compound: 3
    Cytotoxicity against MDCK cells by MTT assay
    Cytotoxicity against MDCK cells by MTT assay
    [PMID: 18640042]
    MOLM-13 IC50
    6.4 μM
    Compound: NSC122415
    Cytotoxicity against human MOLM-13 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against human MOLM-13 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 33026809]
    MOLM-13 IC50
    7 μM
    Compound: 40
    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: 40
    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]
    MV4-11 IC50
    8.2 μM
    Compound: NSC122415
    Cytotoxicity against human MV4-11 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against human MV4-11 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 33026809]
    P388 ED50
    0.8 μg/mL
    Compound: hispidulin
    Cytotoxicity against mouse P388 cells
    Cytotoxicity against mouse P388 cells
    [PMID: 7931367]
    SK-MEL-2 ED50
    11.5 μg/mL
    Compound: hispidulin
    Cytotoxicity against human SK-MEL-2 cells
    Cytotoxicity against human SK-MEL-2 cells
    [PMID: 7931367]
    U-373MG ATCC ED50
    8.8 μg/mL
    Compound: hispidulin
    Cytotoxicity against human U373 cells
    Cytotoxicity against human U373 cells
    [PMID: 10579870]
    ZR-75-1 ED50
    1.2 μg/mL
    Compound: hispidulin
    Cytotoxicity against hormone-dependent human ZR751 cells
    Cytotoxicity against hormone-dependent human ZR751 cells
    [PMID: 10579870]
    In Vitro

    Hispidulin induces cell death in a dose- and time-dependent manner in HepG2 cells. Hispidulin induces apoptosis through mitochondrial dysfunction, which is characterized by decreased Bcl-2/Bax ratio, disrupted mitochondrial membrane potential and increased release of cytochrome C and activated capase-3[2].

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

    In Vivo

    Hispidulin shows significant inhibitory effect on mice tumor size[2].
    Hispidulin treatment effectively prevents ovariectomy-induced body weight loss and attenuates ovariectomy-induced bone loss. Hispidulin treatment also decreases trabecular spacing in ovariectomy mice[3].
    Intraperitoneally administering hispidulin(10 or 50mg/ kg) to rats 30 min before intraperitoneally injecting kainic acid (15mg/kg) increases seizure latency and decreases seizure score. In addition, hispidulin substantially attenuates kainic acid-induced hippocampal neuronal cell death, and this protective effect is accompanied by the suppression of microglial activation and the production of proinflammatory cytokines such as interleukin-1β, interleukin-6, and tumor necrosis factor-α in the hippocampus[4].

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

    Molecular Weight

    300.26

    Formula

    C16H12O6

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C1C=C(C2=CC=C(O)C=C2)OC3=CC(O)=C(OC)C(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 : 62.5 mg/mL (208.15 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 3.3304 mL 16.6522 mL 33.3045 mL
    5 mM 0.6661 mL 3.3304 mL 6.6609 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    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (6.93 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 (6.93 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:  50% PEG300    50% Saline

      Solubility: 10 mg/mL (33.30 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: 99.74%

    References
    Cell Assay
    [2]

    HepG2 cells are treated with different concentrations of hispidulin (50, 100, 200 μM) for 24, 48 and 72 h. Following treatment, cells are further incubated with MTT reagents at 37°C for 4 h before DMSO is added, to dissolve farmazan crystals, and absorbance is measured at 570 nm in a microplate reader[2].

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

    Animal Administration
    [2]

    Mice: Tumor are established in mice. Mice are treated with DMSO or Hispidulin at a dosage of 10, 20 or 40 mg/kg/day for 35 days. The body weight of tumour-bearing mice is recorded every week and tumour volume is calculated [2].

    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, 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 3.3304 mL 16.6522 mL 33.3045 mL 83.2612 mL
    5 mM 0.6661 mL 3.3304 mL 6.6609 mL 16.6522 mL
    10 mM 0.3330 mL 1.6652 mL 3.3304 mL 8.3261 mL
    15 mM 0.2220 mL 1.1101 mL 2.2203 mL 5.5507 mL
    20 mM 0.1665 mL 0.8326 mL 1.6652 mL 4.1631 mL
    25 mM 0.1332 mL 0.6661 mL 1.3322 mL 3.3304 mL
    30 mM 0.1110 mL 0.5551 mL 1.1101 mL 2.7754 mL
    40 mM 0.0833 mL 0.4163 mL 0.8326 mL 2.0815 mL
    50 mM 0.0666 mL 0.3330 mL 0.6661 mL 1.6652 mL
    60 mM 0.0555 mL 0.2775 mL 0.5551 mL 1.3877 mL
    80 mM 0.0416 mL 0.2082 mL 0.4163 mL 1.0408 mL
    100 mM 0.0333 mL 0.1665 mL 0.3330 mL 0.8326 mL
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    • 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.

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    Product Name:
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    Cat. No.:
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