| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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Shikonin (C.I. 75535; Isoarnebin 4) is a natural product and major component of the Chinese medicin 'zicao' with various biological activities such as anti-inflammatory activity by inhibition of TNF-α, NF-κB, HIV-1. It acts as a TMEM16A chloride channel inhibitor (IC50 = 6.5 μM), also a pyruvate kinase M2 (PKM2) inhibitor. Shikonin can also inhibit AIM2 inflammasome activation.
| ln Vitro |
Shikonin, an inhibitor of the TMEM16A chloride channel, with an IC50 of 6.5 μM[1]. Additionally, shikokinin inhibits PKM2 specifically [2]. Additionally, it can stop the nuclear factor-κB (NF-κB) pathway from being activated and inhibit tumor necrosis factor-α (TNF-α). Normal human keratinocytes (NHK) were shown to be considerably less viable (P<0.05) when exposed to shikonin at concentrations greater than 50 μM in comparison to the control. TNF-α-induced NF-κB p65 nuclear translocation was inhibited by shikonin pretreatment for two hours [3]. Cell viability was considerably reduced after 12 hours of treatment with 5 and 7.5 μM shikonin. Both cell lines' inhibitory effects also displayed a time-dependent pattern as compared to the 0 hour group. It was discovered that at the 24- to 48-hour time period, 5 μM shikonin had a stronger inhibitory impact than 2.5 μM shikonin. When U87 and U251 cells were treated with shikonin at 2.5, 5 and 7.5 μM for 24 and 48 hours (p<0.01), their invasiveness was much lower than that of the control group [4].
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| ln Vivo |
When compared to the osteoarthritis group, shikonin significantly prevented the increase in IL-1β and TNF-α expression levels in the osteoarthritis rat model (P<0.01). In the rat model of osteoarthritis, shikonin dramatically reduced the amount of NF-κB protein expression when compared to the osteoarthritis group (P<0.01). In the rat osteoarthritis model treated with shikonin, the induction of iNOS levels was reduced (P<0.01) in comparison to the osteoarthritis group. Shikonin treatment dramatically reduced the increase of COX-2 protein expression in the osteoarthritis rat model when compared to the osteoarthritis group (P<0.01). The increase in caspase-3 activity was much lower in the shikonin-treated osteoarthritis rat model than in the osteoarthritis group (P<0.01). After receiving shikonin treatment, the osteoarthritis group's Akt phosphorylation was dramatically recovered in the rat model of osteoarthritis (P<0.01) [5].
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| References |
[1]. Jiang Y et al. Shikonin Inhibits Intestinal Calcium-Activated Chloride Channels and Prevents Rotaviral Diarrhea. Front Pharmacol. 2016 Aug 23;7:270.
[2]. Li W, et al. Shikonin Suppresses Skin Carcinogenesis via Inhibiting Cell Proliferation. PLoS One. 2015 May 11;10(5):e0126459. [3]. Yan Y, et al. Shikonin Promotes Skin Cell Proliferation and Inhibits Nuclear Factor-κB Translocation via Proteasome Inhibition In Vitro. Chin Med J (Engl). 2015 Aug 20;128(16):2228-33. [4]. Zhang FY, et al. Shikonin Inhibits the Migration and Invasion of Human Glioblastoma Cells by Targeting Phosphorylated β-Catenin and Phosphorylated PI3K/Akt: A Potential Mechanism for the Anti-Glioma Efficacy of a Traditional Chinese Herbal Medicine. Int J Mol Sci. 2015 Oct 9;16(10):23823-48. [5]. Fu D, et al. Shikonin inhibits inflammation and chondrocyte apoptosis by regulation of the PI3K/Akt signaling pathway in a rat model of osteoarthritis. Exp Ther Med. 2016 Oct;12(4):2735-2740. [6]. Kathleen M McAndrews, et al. Mechanisms associated with biogenesis of exosomes in cancer. Mol Cancer. 2019 Mar 30;18(1):52. [7]. Jernej Zorman, et al. Shikonin Suppresses NLRP3 and AIM2 Inflammasomes by Direct Inhibition of Caspase-1. PLoS One. 2016 Jul 28;11(7):e0159826 |
| Molecular Formula |
C16H16O5
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|---|---|
| Molecular Weight |
288.3
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| Exact Mass |
288.0998
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| CAS # |
517-89-5
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| Related CAS # |
(-)-Alkannin;517-88-4;Alkannin;23444-65-7;(Rac)-Shikonin;54952-43-1
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| SMILES |
O([H])[C@]([H])(C([H])([H])/C(/[H])=C(\C([H])([H])[H])/C([H])([H])[H])C1=C([H])C(C2=C(C([H])=C([H])C(=C2C1=O)O[H])O[H])=O
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| Synonyms |
Tokyo Violet Shikonin
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~433.58 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.21 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (7.21 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (7.21 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 30 mg/mL (104.06 mM) in 0.5% CMC-Na/saline water (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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