Shikonin-C-I-75535-DataSheet-生命科學試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEShikoninCat. No.: HY-N0822CAS No.: 517-89-5Synonyms: C.I. 75535; Isoarnebin 4分式: CHO分量: 288.3作靶點: Chloride Channel; Pyruvate Kinase; NF-B; TNF Receptor作通路: Membrane Transporter/Ion Channel; MetabolicEnzyme/Protease; NF-B; Apopto

2、sis儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數據體外實驗 DMSO : 31 mg/mL (107.53 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 3.4686 mL 17.3430 mL 34.6861 mL5 mM 0.6937 mL 3.4686 mL 6.9372 mL10 mM 0.3469 mL 1.7343 mL 3.4686 m

3、L請根據產品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內實驗請根據您的實驗動物和給藥式選擇適當的溶解案，配制前請先配制澄清的儲備液，再依次添加助溶劑(為保證實驗結果的可靠性，體內實驗的作液，建議您現現配，當天使；澄清的儲備液可以根據儲存條件，適當保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (7.21 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 9

4、0% corn oil1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.08 mg/mL (7.21 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Shikonin中草藥紫草的主 成分。 Shikonin顯出各種物活性，包括抑制TNF-，NF-B，HIV-1。IC50 & Target NF-B TNF- TMEM16A chloride PKM2channel6.5 M (IC50)體外研究 Shikonin is an inhibitor of TMEM16A chloride

5、 channel with an IC50 of 6.5 M 1. Shikonin is also a specificinhibitor of PKM2 2 and can also inhibit tumor necrosis factor- (TNF-) and prevent activation of nuclearfactor-B (NF-B) pathway. Shikonin at concentrations higher than 50 M significantly inhibits ormal humankeratinocytes (NHKs) viability,

6、compare with that of control (P 3. Treatments of Shikonin at 5 and 7.5 Msignificantly 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 M Shikonin displaysgreater inhibit

7、ion compare to 2.5 M at the time points from 24 to 48 h. The invasiveness of U87 and U251cells is significantly attenuated when treated with Shikonin at 2.5, 5, and 7.5 M compare with the controlgroup at 24 and 48 h (p 4.體內研究 Shikonin significantly inhibits the increase in IL-1 and TNF- expression l

8、evels in the rat model ofosteoarthritis, compare with those in the osteoarthritis group (P 5.PROTOCOLCell Assay 4 U87 and U251 cells are seeded into 96-well plates at a density of 1104 cells per well in standard DMEMand incubated for 24 h under standard conditions (37C and 5% CO2). Then the medium i

9、s replaced witheither blank, serum-free DMEM or DMEM containing Shikonin at concentrations of 2.5, 5, and 7.5 M. Thetotal volume in each well is 200 L. Finally, the plates are shaken softly and the optical density is recorded at570 nm (OD570) using a plate reader. At least three independent experime

10、nts are performed 4.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Healthy male Sprague-Dawley rats (n=30; 8 to 10-weeks old, 250 to 300 g) are used in this study. Rats areAdministration 5 randomly assigned to three groups: Sham-operated group (

11、n=10), osteoarthritis model group (n=10) andShikonin-treated group (n=10). In the sham-operated group, the right knee joint of the anesthetized rat is onlyexposed under sterile conditions, and the rats are treated with 0.1 ml/100 g physiological saline (i.p.). In theosteoarthritis model group, osteo

12、arthritis 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 for4 days after osteoarthritis modeling 5.MCE has not independently confirmed the accuracy of these methods. T

13、hey are for reference only.戶使本產品發(fā)表的科研獻2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE Int J Biochem Cell Biol. 2018 Mar;96:9-19. J Chemother. 2019 May.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Jiang Y et al. Shikonin Inhibits Intestinal Calcium-Activated Chloride Channe

14、ls and Prevents Rotaviral Diarrhea. Front Pharmacol. 2016Aug 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-B Translocation

15、 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 -Catenin andPhosphorylated PI3K/Akt: A Potential Mechanism for the Anti-Glioma Efficacy of a Traditional Chinese Herbal Medicine. Int J Mol Sci. 2015Oct 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 ofosteoarthritis. Ex