1. Membrane Transporter/Ion Channel
    Metabolic Enzyme/Protease
    NF-κB
    Apoptosis
  2. Chloride Channel
    Pyruvate Kinase
    NF-κB
    TNF Receptor

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

Cat. No.: HY-N0822 Purity: 99.64%
Handling Instructions

Shikonin is an inhibitor of TMEM16A chloride channel with an IC50 of 6.5 μM. Shikonin is also a specific inhibitor of PKM2 and can also inhibit tumor necrosis factor-α (TNF-α) and prevent activation of nuclear factor-κB (NF-κB) pathway.

For research use only. We do not sell to patients.
Shikonin Chemical Structure

Shikonin Chemical Structure

CAS No. : 517-89-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 66 In-stock
10 mg USD 60 In-stock
25 mg USD 132 In-stock
50 mg USD 192 In-stock
100 mg USD 312 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

    Shikonin purchased from MCE. Usage Cited in: Int J Biochem Cell Biol. 2018 Jan 8;96:9-19.

    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

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Shikonin is an inhibitor of TMEM16A chloride channel with an IC50 of 6.5 μM. Shikonin is also a specific inhibitor of PKM2 and can also inhibit tumor necrosis factor-α (TNF-α) and prevent activation of nuclear factor-κB (NF-κB) pathway.

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

    TMEM16A chloride channel

    6.5 μM (IC50)

    PKM2

     

    NF-κB

     

    TNF-α

     

    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].

    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].

    References
    Preparing Stock Solutions
    Concentration Volume 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.
    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
    Molecular Weight

    288.3

    Formula

    C₁₆H₁₆O₅

    CAS No.

    517-89-5

    SMILES

    O=C1C([[email protected]](O)C/C=C(C)/C)=CC(C2=C1C(O)=CC=C2O)=O

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 31 mg/mL

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    Purity: 99.64%

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    Product Name:
    Shikonin
    Cat. No.:
    HY-N0822
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