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Shikonin

Catalog No. T1125 CAS 517-89-5

Synonyms: NSC 252844, Isoarnebin 4, (+)-Shikonin, Alkanna Red, C.I. 75535, Anchusa acid

Shikonin (Anchusa acid) is a natural product, a TMEM16A chloride channel inhibitor (IC50=6.5 μM) and selective PKM2 inhibitor. Shikonin exhibits antitumor, anti-inflammatory and wound healing activities.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Shikonin, CAS 517-89-5

Pack Size	Availability	Price/USD
5 mg	In stock	$ 29.00
10 mg	In stock	$ 44.00
25 mg	In stock	$ 89.00
50 mg	In stock	$ 143.00
100 mg	In stock	$ 226.00
200 mg	In stock	$ 336.00
500 mg	In stock	$ 562.00
1 mL * 10 mM (in DMSO)	In stock	$ 48.00

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Purity: 99.9%

Purity: 99.11%

Purity: 98.54%

Purity: 98.14%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Shikonin (Anchusa acid) is a natural product, a TMEM16A chloride channel inhibitor (IC50=6.5 μM) and selective PKM2 inhibitor. Shikonin exhibits antitumor, anti-inflammatory and wound healing activities.
Targets&IC50	PKM2 (FBP absence):0.3 μM, PKM2 (FBP presence):0.8 μM, TMEM16A (Cl- channel):6.5 μM
In vitro	METHODS: Human glioma cells U87 and U251 were treated with Shikonin (2.5-7.5 μmol/L) for 12-72 h. Cell viability was measured by CCK-8. RESULTS: Shikonin inhibited the proliferation of U87 and U251 cells in a time- and dose-dependent manner. [1] METHODS: Macrophages RAW264.7 were pretreated with Shikonin (0.5-2 μM) for 1 h, then treated with LPS (250 ng/mL) and IFN-γ (100 ng/mL) for 24 h. Inflammatory factor levels were measured using RT-qPCR and ELISA. RESULTS: In LPS+IFN-γ-mimicked RAW264.7 cells, mRNA and protein expression of IL-1β, IL-6 and TNF-α were reduced. [2]
In vivo	METHODS: To investigate the efficacy against murine colitis, Shikonin (6.125-25 mg/kg) was administered by gavage to a DSS-induced Balb/c mouse model of colitis once daily for seven days. RESULTS: Shikonin attenuated the overall symptoms of DSS-induced colitis in mice and reduced colonic injury. [2] METHODS: To detect anti-tumor activity in vivo, Shikonin (0.1-10 mg/kg) was administered intraperitoneally to SCID mice bearing human melanoma B16 once daily for nine days. RESULTS: Shikonin treatment inhibited B16 cell growth in SCID mice in a dose-dependent manner. [3]
Cell Research	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].
Animal Research	Healthy male Sprague-Dawley rats (n=30; 8 to 10-weeks old, 250 to 300 g) are used in this study. Rats were 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].

Synonyms	NSC 252844, Isoarnebin 4, (+)-Shikonin, Alkanna Red, C.I. 75535, Anchusa acid
Molecular Weight	288.3
Formula	C16H16O5
CAS No.	517-89-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 57 mg/mL

H2O: Insoluble

Ethanol: 13 mg/mL(45.1 mM)

References and Literature

1. 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. 2. Huang B, et al. Shikonin ameliorated mice colitis by inhibiting dimerization and tetramerization of PKM2 in macrophages. Front Pharmacol. 2022 Aug 17;13:926945. 3. Zhao X, et al. Shikonin Inhibits Tumor Growth in Mice by Suppressing Pyruvate Kinase M2-mediated Aerobic Glycolysis. Sci Rep. 2018 Sep 28;8(1):14517. 4. Zhang F Y, Hu Y, Que Z Y, 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[J]. International journal of molecular sciences, 2015, 16(10): 23823-23848. 5. Fu D, Shang X, Ni Z, et al. Shikonin inhibits inflammation and chondrocyte apoptosis by regulation of the PI3K/Akt signaling pathway in a rat model of osteoarthritis[J]. Experimental and therapeutic medicine, 2016, 12(4): 2735-2740. 6. 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. 7. Jiang Y et al. Shikonin Inhibits Intestinal Calcium-Activated Chloride Channels and Prevents Rotaviral Diarrhea. Front Pharmacol. 2016 Aug 23;7:270.

Citations

1. Lu J, Liu S Y, Zhang J, et al. Inhibition of BAG3 enhances the anticancer effect of shikonin in hepatocellular carcinoma. American Journal of Cancer Research. 2021, 11(7): 3575.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Membrane Protein-targeted Compound Library Kinase Inhibitor Library Glycolysis Compound Library Anti-Cardiovascular Disease Compound Library Lipid Metabolism Compound Library Natural Product Library for HTS Target-Focused Phenotypic Screening Library Anti-Prostate Cancer Compound Library Anti-Tumor Natural Product Library

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Keywords

Shikonin 517-89-5 Apoptosis Membrane transporter/Ion channel Metabolism Microbiology/Virology NF-Κb Proteases/Proteasome NF-κB TNF HIV Protease PKM Chloride channel Inhibitor Nuclear factor-kappaB inhibit TNFR Human immunodeficiency virus HIV Cl? Channels Isoarnebin-4 NSC 252844 TNF Receptor Pyruvate Kinase Isoarnebin4 Tumor Necrosis Factor Receptor Nuclear factor-κB Isoarnebin 4 NSC-252844 Chloride Channel (+)-Shikonin NSC252844 Alkanna Red C.I. 75535 Anchusa acid inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.