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Shikonin

Catalog No. T1125 CAS 517-89-5

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

Shikonin is an TMEM16A chloride channel inhibitor (IC50: 6.5 μM). Shikonin is also a selective PKM2 inhibitor and can also suppress activation of the NF-κB pathway and inhibit TNF-α. Shikonin decreases exosome secretion through the inhibition of glycolysis

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Shikonin, CAS 517-89-5

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Purity: 98%

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Storage & Solubility Information

Description	Shikonin is an TMEM16A chloride channel inhibitor (IC50: 6.5 μM). Shikonin is also a selective PKM2 inhibitor and can also suppress activation of the NF-κB pathway and inhibit TNF-α. Shikonin decreases exosome secretion through the inhibition of glycolysis
Targets&IC50	TMEM16A chloride channel:6.5 μM, PKM2 (FBP presence):0.8 μM, PKM2 (FBP absence):0.3 μM
In vitro	Shikonin (>50 μM) markedly inhibits normal 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]. Shikonin (5/7.5 μM) markedly inhibits 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 (2.5/5/7.5 μM) compare with the control group at 24 and 48 h (p<0.01)[4].
In vivo	Shikonin markedly inhibits the increase in TNF-α and IL-1β expression levels in the rat model of osteoarthritis, compared 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 compared 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, compared with that in the osteoarthritis group (P<0.01)[5].
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	Isoarnebin 4, Anchusa acid, NSC 252844, 紫草素, Alkanna Red, (+)-Shikonin, C.I. 75535
Molecular Weight	288.299
Formula	C16H16O5
CAS No.	517-89-5

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 57 mg/mL

H2O: Insoluble

Ethanol: 13 mg/mL(45.1 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Jiang Y, Yu B, Yang H, et al. Shikonin Inhibits Intestinal Calcium-Activated Chloride Channels and Prevents Rotaviral Diarrhea[J]. Frontiers in pharmacology, 2016, 7: 270. 2. Li W, Zhang C, Ren A, et al. Shikonin suppresses skin carcinogenesis via inhibiting cell proliferation[J]. PloS one, 2015, 10(5): e20126459. 3. Yan Y, Furumura M, Gouya T, et al. Shikonin promotes skin cell proliferation and inhibits nuclear factor-κB translocation via proteasome inhibition in vitro[J]. Chinese medical journal, 2015, 128(16): 2228. 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：

Anti-Cancer Compound Library HIF-1 Signaling Pathway Compound Library Phosphatase Inhibitor Library Glycometabolism Compound Library Anti-Cancer Metabolism Compound Library Traditional Chinese Medicine Monomer Library Tibetan medicine Compound Library Anti-Obesity Compound Library Lipid Metabolism Compound Library Glutamine Metabolism Compound Library

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Keywords

Shikonin 517-89-5 NF-Kb信号通路代谢蛋白酶体凋亡离子通道微生物学 Chloride channel HIV Protease NF-κB PKM TNF Inhibitor Nuclear factor-kappaB inhibit TNFR Human immunodeficiency virus HIV C.I. 75535 Cl? Channels Isoarnebin-4 TNF Receptor Pyruvate Kinase Isoarnebin4 Tumor Necrosis Factor Receptor Nuclear factor-κB Chloride Channel (+)-Shikonin Alkanna Red NSC 252844 Anchusa acid Isoarnebin 4 inhibitor

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