2. Membrane Transporter/Ion Channel Metabolic Enzyme/Protease NF-κB Apoptosis Anti-infection Immunology/Inflammation
  3. Chloride Channel Pyruvate Kinase NF-κB TNF Receptor HIV AIM2
  4. Shikonin

Shikonin  (Synonyms: C.I. 75535; Isoarnebin 4)

Cat. No.: HY-N0822 Purity: 99.79%
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Shikonin is a major component of a Chinese herbal medicine named zicao. Shikonin is a potent TMEM16A chloride channel inhibitor with an IC50 of 6.5 μM. Shikonin is a specific pyruvate kinase M2 (PKM2) inhibitor and can also inhibit TNF-α and NF-κB pathway. Shikonin decreases exosome secretion through the inhibition of glycolysis. Shikonin inhibits AIM2 inflammasome activation.

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

Shikonin Chemical Structure

Shikonin Chemical Structure

CAS No. : 517-89-5

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Solid + Solvent
10 mM * 1 mL in DMSO
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 USD 61 In-stock
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10 mM * 1 mL in DMSO USD 61 In-stock
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5 mg USD 35 In-stock
10 mg USD 55 In-stock
25 mg USD 110 In-stock
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Based on 32 publication(s) in Google Scholar

Other Forms of Shikonin:

Shikonin Related Antibodies

Top Publications Citing Use of Products

31 Publications Citing Use of MCE Shikonin

IF

    Shikonin purchased from MedChemExpress. Usage Cited in: Int J Biochem Cell Biol. 2018 Mar;96:9-19.  [Abstract]

    Hep3B cells are treated with 2 μmol Shikonin, 5-FU, BSNQ or OSNQ for different times (3, 6, 12 and 24 h), and stained with Annexin V and PI. The apoptotic cells are detected by fluorescence microscopy and quantified as percentages.

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Shikonin is a major component of a Chinese herbal medicine named zicao. Shikonin is a potent TMEM16A chloride channel inhibitor with an IC50 of 6.5 μM[1]. Shikonin is a specific pyruvate kinase M2 (PKM2) inhibitor[2] and can also inhibit TNF-α and NF-κB pathway[3]. Shikonin decreases exosome secretion through the inhibition of glycolysis[4]. Shikonin inhibits AIM2 inflammasome activation[7].

    IC50 & Target[1][2][3]

    TMEM16A chloride channel

    6.5 μM (IC50)

    PKM2

     

    NF-κB

     

    In Vitro

    Shikonin is an inhibitor of TMEM16A chloride channel with an IC50 of 6.5 μM[1]. Shikonin is also a specific inhibitor of PKM2[2] and can also inhibit tumor necrosis factor-α (TNF-α) and prevent activation of nuclear factor-κB (NF-κB) pathway. Shikonin at concentrations higher than 50 μM significantly inhibits ormal human keratinocytes (NHKs) viability, compare with that of control (P<0.05). Pretreatment with Shikonin for 2 h attenuates TNF-α-induced NF-κB p65 nuclear translocation[3]. Treatments of Shikonin at 5 and 7.5 μM significantly inhibit the cell viability starting from 12 h and the inhibitory effects are presented in time-dependent patterns compare with the 0 h group in both cell lines. It is found that 5 μM Shikonin displays greater inhibition compare to 2.5 μM at the time points from 24 to 48 h. The invasiveness of U87 and U251 cells is significantly attenuated when treated with Shikonin at 2.5, 5, and 7.5 μM compare with the control group at 24 and 48 h (p<0.01)[4].

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

    Shikonin Related Antibodies
    In Vivo

    Shikonin significantly inhibits the increase in IL-1β and TNF-α expression levels in the rat model of osteoarthritis, compare with those in the osteoarthritis group (P<0.01). The NF-κB protein expression level is significantly suppressed by Shikonin in the rat model of osteoarthritis, compare with that in the osteoarthritis group (P<0.01). The induction of the iNOS level is suppressed by treatment with Shikonin in the rat model of osteoarthritis, compare with that in the osteoarthritis group (P<0.01). The administration of Shikonin markedly weakens the up-regulation of COX-2 protein expression in the rat model of osteoarthritis, as compare with that in the osteoarthritis group (P<0.01). The elevation of caspase-3 activity is significantly reduced by Shikonin treatment in the rat model of osteoarthritis, compare with that in the osteoarthritis group (P<0.01). The downregulation of Akt phosphorylation is also significantly recovered by treatment with Shikonin in the rat model of osteoarthritis, compare with that in the osteoarthritis group (P<0.01)[5].

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

    288.30

    Formula

    C16H16O5
    CAS No.
    Appearance

    Solid

    Color

    Brown to reddish brown

    SMILES

    O=C1C([C@H](O)C/C=C(C)/C)=CC(C2=C1C(O)=CC=C2O)=O
    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 (433.58 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 3.4686 mL 17.3430 mL 34.6861 mL
    5 mM 0.6937 mL 3.4686 mL 6.9372 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)

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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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    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 (7.21 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 (7.21 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: 30 mg/mL (104.06 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)

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    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: 99.80%

    COA (250 KB) HNMR (206 KB) LCMS (123 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [4]

    U87 and U251 cells are seeded into 96-well plates at a density of 1×104 cells per well in standard DMEM and incubated for 24 h under standard conditions (37°C and 5% CO2). Then the medium is replaced with either blank, serum-free DMEM or DMEM containing Shikonin at concentrations of 2.5, 5, and 7.5 μM. The total volume in each well is 200 μL. Finally, the plates are shaken softly and the optical density is recorded at 570 nm (OD570) using a plate reader. At least three independent experiments are performed[4].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [5]

    Healthy male Sprague-Dawley rats (n=30; 8 to 10-weeks old, 250 to 300 g) are used in this study. Rats are randomly assigned to three groups: Sham-operated group (n=10), osteoarthritis model group (n=10) and Shikonin-treated group (n=10). In the sham-operated group, the right knee joint of the anesthetized rat is only exposed under sterile conditions, and the rats are treated with 0.1 ml/100 g physiological saline (i.p.). In the osteoarthritis model group, osteoarthritis model rats were treated with 0.1 ml/100 g physiological saline (i.p.). In the Shikonin-treated group, osteoarthritis model rats are treated with 10 mg/kg Shikonin (i.p.) once daily for 4 days after osteoarthritis modeling[5].

    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 3.4686 mL 17.3430 mL 34.6861 mL 86.7152 mL
    5 mM 0.6937 mL 3.4686 mL 6.9372 mL 17.3430 mL
    10 mM 0.3469 mL 1.7343 mL 3.4686 mL 8.6715 mL
    15 mM 0.2312 mL 1.1562 mL 2.3124 mL 5.7810 mL
    20 mM 0.1734 mL 0.8672 mL 1.7343 mL 4.3358 mL
    25 mM 0.1387 mL 0.6937 mL 1.3874 mL 3.4686 mL
    30 mM 0.1156 mL 0.5781 mL 1.1562 mL 2.8905 mL
    40 mM 0.0867 mL 0.4336 mL 0.8672 mL 2.1679 mL
    50 mM 0.0694 mL 0.3469 mL 0.6937 mL 1.7343 mL
    60 mM 0.0578 mL 0.2891 mL 0.5781 mL 1.4453 mL
    80 mM 0.0434 mL 0.2168 mL 0.4336 mL 1.0839 mL
    100 mM 0.0347 mL 0.1734 mL 0.3469 mL 0.8672 mL
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    Shikonin 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:

    Shikonin517-89-5C.I. 75535 Isoarnebin 4Isoarnebin4Isoarnebin 4Isoarnebin-4Chloride ChannelPyruvate KinaseNF-κBTNF ReceptorHIVAIM2Cl− Channels Nuclear factor-κBNuclear factor-kappaBTumor Necrosis Factor ReceptorTNFRHuman immunodeficiency virusAbsent in melanoma 2Interferon-inducible protein AIM2PYHINInhibitorinhibitorinhibit

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