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%
COA Handling Instructions

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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10 mM * 1 mL in DMSO USD 61 In-stock
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10 mg USD 55 In-stock
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Customer Review

Based on 22 publication(s) in Google Scholar

Other Forms of Shikonin:

Shikonin Related Antibodies

Top Publications Citing Use of Products

    Shikonin purchased from MCE. 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.

    View All NF-κB Isoform Specific Products:

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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].

    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].

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

    288.30

    Appearance

    Solid

    Formula

    C16H16O5
    CAS No.
    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)

    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
    10 mM 0.3469 mL 1.7343 mL 3.4686 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

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

      Solubility: 30 mg/mL (104.06 mM); Suspended solution; Need ultrasonic

    • 2.

      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

    • 3.

      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

    • 4.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.08 mg/mL (7.21 mM); Clear solution

    *All of the co-solvents are available by MCE.
    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
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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.

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    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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