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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemECurcuminCat. No.: HY-N0005CAS No.: 458-37-7Synonyms: Turmeric yellow; Natural Yellow 3; Diferuloylmethane分式: CHO分量: 368.38作靶点: Keap1-Nrf2; Autophagy; Histone Acetyltransferase; EpigeneticReader Domain; Mitophagy作通路: NF-B; Autoph

2、agy; Epigenetics储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (271.46 mM)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 3 mg/mL (8.14 mM); Clear solution1/3 Master of Small Molecules 您边的抑制剂师www.MedChemE2. 请依序添加每种溶剂: 10% DMSO 90% (20% SBE-CD in s

3、aline)Solubility: 3 mg/mL (8.14 mM); Suspended solution; Need ultrasonic3. 请依序添加每种溶剂: 10% DMSO 90% corn oilSolubility: 3 mg/mL (8.14 mM); Precipitated solutionBIOLOGICAL ACTIVITY物活性 Curcumin (Turmeric yellow)种天然酚类化合物,具有抗炎,抗氧化,抗增殖和抗管成等多种活性。Curcuminp300组蛋酰转移酶 (HATs) 抑制剂,也显对 NF-B 和MAPKs 的抑制作。IC50 & Tar

4、get Keap1-Nrf2 1, Histone acetyltransferase 6体外研究 Curcumin exerts its chemopreventive effects partly through the activation of nuclear factor (erythroid-2related) factor 2 (Nrf2) and its antioxidant and phase II detoxifying enzymes 1. Curcumin inhibits T47D cellsgrowth, with IC50s of 25, 19 and 17.5

5、 M for 24, 48 and 72 h MTT assays respectively. IC50s of curcuminand silibinin mixture against T47D cells, are 17.5, 15, and 12 M for 24, 48, and 72 h exposure times,respectively 2. Curcumin (2.5-80 M) induces apoptotic cell death in AGS and HT-29 cell lines, and theIC50 is 21.90.1, 40.70.5 M, respe

6、ctively, in both AGS and HT-29 cell lines. Curcumin-induced apoptosisrequires caspase activities in AGS and HT-29 cells. Curcumin induces ER Ca2+ decline and mitochondrialCa2+ overloading 3. Curcumin induces the G2/M cell cycle arrest of LNCaP and PC-3 cells in a dosedependent manner. Curcumin upreg

7、ulates the protein level of NF-kappaB inhibitor IkappaBalpha anddownregulates protein levels of c-Jun and AR 5.体内研究 Curcumin (10 mg/kg, p.o.) significantly prevents decrease in the percentage of sucrose consumption, ascompared to the CMS-exposed rats. Curcumin treatment results in significant preven

8、tion of increase in TNF- and IL-6 levels in stressed rats 4. Curcumin decreases binding of p300/CREB-binding protein (CBP) atthe brain-derived neurotrophic factor (BDNF) promoter at 20 mg/kg (i.p.), reduces binding of P300/CBP at theBDNF promoter at 40 mg/kg, and decreases binding all the four prote

9、ins of p300/CBP and H3K9ac/H4K5acat the BDNF promoter at 60 mg/kg in chronic constriction injury (CCI) rats 6.PROTOCOLCell Assay 2 T47D breast cancer cell line is grown in RPMI 1640 supplemented with 10% FBS, 2 mg/mL sodiumbicarbonate, 0.05 mg/mL penicillin G, 0.08 mg/mL streptomycin. Culture is mai

10、ntained on plastic flask andincubated at 37C in 5% CO2. After growing sufficient amount of cells, cytotoxic effect of silibinin andcurcumin is studied by 24, 48 and 72 h MTT assays in which 1000 cell/well are cultivated in a 96 well plate.After 24 h incubation in 37C with humidified atmosphere conta

11、ining 5% CO2, the cells are treated with serialconcentrations of curcumin (5, 10, 20, 30, 40, 50, 60, 80, 100 M), silibinin (20, 40, 60, 80, 100, 120, 140,180, 200 M), and curcumin-silibinin mixture (each of them 5, 10, 20, 30, 40, 50, 60, 80, 100 M) for 24, 48and 72 h in the quadruplicate manner, i

12、n addition to cells with 200 L culture medium containing 10% DMSOfor control. After incubation, the medium of all wells of the plate are exchanged with fresh medium and thecells are leaved for 24 h in incubator. Then, medium of all wells are removed carefully and 50 L of 2 mg/mL2/3 Master of Small M

13、olecules 您边的抑制剂师www.MedChemEMTT dissolved in PBS is added to each wells and the plate is covered with aluminum foil and incubated for4.5 h again. After removing content of the wells, 200 L pure DMSO is added to the wells. Then, 25 LSorensens glycine buffer is added and immediately absorbance of each

14、 wells is read in 570 nm usingEL800 Microplate Absorbance Reader with reference wavelength of 630 nm.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Curcumin (10 mg/kg), freshly suspended in saline, is administrated by oral gavage once a day for

15、3 weeks.Administration 4 Forty rats are randomLy assigned to 4 groups (n=10/each group): group I receives saline and serves ascontrol, group II receives curcumin, group III is exposed to CMS andreceive saline and group IV aresubjected to CMS andreceive curcumin.MCE has not independently confirmed th

16、e accuracy of these methods. They are for reference only. Cell Syst. 2018 Apr 25;6(4):424-443.e7. J Exp Clin Cancer Res. 2018 Oct 29;37(1):261. FASEB J. 2017 Sep;31(9):3800-3815. Int J Mol Sci. 2018 Dec 21;20(1). pii: E28. J Cell Biochem. 2019 Apr;120(4):6718-6728.See more customer validations on HY

17、PERLINK / www.MedChemEREFERENCES1. Gao S, et al. Curcumin attenuates arsenic-induced hepatic injuries and oxidative stress in experimental mice through activation of Nrf2pathway, promotion of arsenic methylation and urinary excretion. Food Chem Toxicol. 2013 Jul 18. pii: S0278-6915(13)0042. Nasiri M

18、, et al. Curcumin and Silibinin Inhibit Telomerase Expression in T47D Human Breast Cancer Cells. Asian Pac J Cancer Prev.2013;14(6):3449-53.3. Cao A, et all. Curcumin induces apoptosis in human gastric carcinoma AGS cells and colon carcinoma HT-29 cells throughmitochondrial dysfunction and endoplasmic reticulum stress. Apoptosis. 2013 Jul 24. Epub ahead of print4. Jiang H, et al. Antidepressant-like effects of curcumin in chronic mild stress of rats: Involvement of its anti-inflammatory action. ProgNeuropsychopharmacol Biol Psychiatry. 2013 Jul 20. pii: S0

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