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  3. Scutellarin

Scutellarin, an active flavone isolated from Scutellaria baicalensis, can down-regulates the STAT3/Girdin/Akt signaling in HCC cells, and inhibits RANKL-mediated MAPK and NF-κB signaling pathway in osteoclasts. Scutellarin is active against HIV-1IIIB, HIV-1(74V) and HIV-1KM018 with EC50s of 26 μM, 253 μM and 136 μM, respectively.

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Scutellarin Chemical Structure

Scutellarin Chemical Structure

CAS No. : 27740-01-8

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10 mM * 1 mL in DMSO
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Customer Review

Based on 10 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Scutellarin purchased from MedChemExpress. Usage Cited in: Thorac Cancer. 2019 Mar;10(3):492-500.  [Abstract]

    A549 cells are treated with scutellarin (SCU) (0, 200, 400, 600 μM) for 24 hours. Western blotting analyses are used to detect the expression of proteins in the STAT3 pathways, cyclin D1, and cyclin E.

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Scutellarin, an active flavone isolated from Scutellaria baicalensis, can down-regulates the STAT3/Girdin/Akt signaling in HCC cells, and inhibits RANKL-mediated MAPK and NF-κB signaling pathway in osteoclasts. Scutellarin is active against HIV-1IIIB, HIV-1(74V) and HIV-1KM018 with EC50s of 26 μM, 253 μM and 136 μM, respectively.

    IC50 & Target[1]

    STAT3

     

    HIV-1

     

    In Vitro

    Scutellarin treatment significantly reduces HepG2 cell viability in a dose-dependent manner, and inhibits migration and invasion of HCC cells in vitro. Scutellarin treatment significantly reduces STAT3 and Girders of actin filaments (Girdin) expression, STAT3 and Akt phosphorylation in HCC cells. Introduction of STAT3 overexpression restores the scutellarin-downregulated Girdin expression, Akt activation, migration and invasion of HCC cells. Furthermore, induction of Girdin overexpression completely abrogates the inhibition of scutellarin on the Akt phosphorylation, migration and invasion of HCC cells. Scutellarin can inhibit HCC cell metastasis in vivo, and migration and invasion in vitro by down-regulating the STAT3/Girdin/Akt signaling[1]. Scutellarin selectively enhances Akt phosphorylation[2]. Scutellarin is a putative therapeutic agent as it has been found to not only suppress microglial activation thus ameliorating neuroinflammation, but also enhance astrocytic reaction. Acutellarin amplifies the astrocytic reaction by upregulating the expression of neurotrophic factors among others thus indicating its neuroprotective role. Remarkably, the effects of scutellarin on reactive astrocytes are mediated by activated microglia supporting a functional "cross-talk" between the two glial types[3]. Scutellarin can suppress RANKL-mediated osteoclastogenesis, the function of osteoclast bone resorption, and the expression levels of osteoclast-specific genes (tartrate-resistant acid phosphatase (TRAP), cathepsin K, c-Fos, NFATc1). Further investigation indicates that Scutellarin can inhibit RANKL-mediated MAPK and NF-κB signaling pathway, including JNK1/2, p38, ERK1/2, and IκBα phosphorylation[5].

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

    In Vivo

    Scutellarin (50 mg/kg/day) significantly mitigates the lung and intrahepatic metastasis of HCC tumors in vivo. The numbers of the lung and intrahepatic metastatic tumors in the scutellarin-treated group are significantly less than that in the controls[1]. The rats treated with Scutellarin display a significant alleviation in neurobehavioral deficits compared to the SAH group. Scutellarin enhanced eNOS expression compared with SAH rats[4].

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

    Molecular Weight

    462.36

    Formula

    C21H18O12

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to green yellow

    SMILES

    O=C(C=C(C1=CC=C(O)C=C1)OC2=CC(O[C@@H]([C@@H]([C@@H](O)[C@@H]3O)O)O[C@@H]3C(O)=O)=C4O)C2=C4O

    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 : 100 mg/mL (216.28 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 2.1628 mL 10.8141 mL 21.6282 mL
    5 mM 0.4326 mL 2.1628 mL 4.3256 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.

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

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    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:  15% Cremophor EL    85% Saline

      Solubility: 5 mg/mL (10.81 mM); Suspended solution; Need ultrasonic

    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 (21.63 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
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    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
    Cell Assay
    [1]

    HepG2 cells (1×105/well) are cultured in 96-well plates and treated in triplicate with scutellarin at concentrations of 5, 10, 20, 30, and 100 μM or vehicle alone for 24 h. The cellular viability is tested by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, and is expressed as a percentage of proliferation versus controls.

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

    Animal Administration
    [1]

    To establish an orthotopic liver xenograft model, individual mice are anesthetized with isoflurane and a small incision is made in their abdomen. Individual mice are injected with 2×106 SK-Hep1 cells in 30 μL Matrigel into their left lobe of the liver. Twenty-four hours after orthotopic liver implantation, the mice are randomized and injected intraperitoneally with scutellarin (50 mg/kg/day) or vehicle (0.9% NaCl, normal saline) daily for 35 consecutive days (n=10 per group). Subsequently, the mice are sacrificed, and their lungs and livers are excised, fixed in 10% buffered formalin and paraffin-embedded for hematoxylin and eosin staining.

    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 2.1628 mL 10.8141 mL 21.6282 mL 54.0704 mL
    5 mM 0.4326 mL 2.1628 mL 4.3256 mL 10.8141 mL
    10 mM 0.2163 mL 1.0814 mL 2.1628 mL 5.4070 mL
    15 mM 0.1442 mL 0.7209 mL 1.4419 mL 3.6047 mL
    20 mM 0.1081 mL 0.5407 mL 1.0814 mL 2.7035 mL
    25 mM 0.0865 mL 0.4326 mL 0.8651 mL 2.1628 mL
    30 mM 0.0721 mL 0.3605 mL 0.7209 mL 1.8023 mL
    40 mM 0.0541 mL 0.2704 mL 0.5407 mL 1.3518 mL
    50 mM 0.0433 mL 0.2163 mL 0.4326 mL 1.0814 mL
    60 mM 0.0360 mL 0.1802 mL 0.3605 mL 0.9012 mL
    80 mM 0.0270 mL 0.1352 mL 0.2704 mL 0.6759 mL
    100 mM 0.0216 mL 0.1081 mL 0.2163 mL 0.5407 mL
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