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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemELucanthoneCat. No.: HY-B2098CAS No.: 479-50-5分式: CHNOS分量: 340.48作靶点: Autophagy作通路: Autophagy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 : 25 mg/mL (73.43 mM; Need ultrasonic)Mass Solvent1
2、 mg 5 mg 10 mg Concentration制备储备液1 mM 2.9370 mL 14.6852 mL 29.3703 mL5 mM 0.5874 mL 2.9370 mL 5.8741 mL10 mM 0.2937 mL 1.4685 mL 2.9370 mL请根据产品在不同溶剂中的溶解度,选择合适的溶剂配制储备液,并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Lucanthone是Apurinic 内切核酸酶-1 (APE-1) 的内切核酸酶抑制剂。IC50 & Target APE-1 1体外研究Lucanthone is a novel in
3、hibitor of autophagy that induces cathepsin D-mediated apoptosis. To investigate theanticancer activity of Lucanthone, cell viability is measured by MTT assay. Lucanthone reduces cell viabilityto a similar extent in a panel of seven breast cancer cell lines. In addition, a direct comparison reveals
4、that1/2 Master of Small Molecules 您边的抑制剂师www.MedChemELucanthone is significantly more potent than Chloroquine (CQ) at reducing breast cancer cell viability with amean IC50 of 7.2 M versus 66 M for CQ. Measurement of cell viability in two representative cell lines(MDA-MB-231 and BT-20) by ATPlite ass
5、ay and trypan blue exclusion reveals comparable results 2.PROTOCOLCell Assay 2 Cell viability is assessed by MTT assay. Cells are seeded into 96-well microculture plates at 10,000 cells perwell and allowed to attach for 24 h. Cells are then treated with Lucanthone (0, 0.5, 1, 5, 10, 20 and 40 M),Chl
6、oroquine, Vorinostat, or combinations for 72 h. Following drug treatment, MTT is added and cell viability isquantified using a BioTek microplate reader. Effects on cell viability are also determined by measuring ATPlevels using the ATPlite assay system and by trypan blue exclusion. Pro-apoptotic eff
7、ects following in vitrodrug exposure are quantified by propidium iodide (PI) staining and fluorescence-activated cell sorting (FACS)analysis of sub-G0/G1 DNA content 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Chowdhury SM, et al. Gra
8、phene nanoribbons as a drug delivery agent for lucanthone mediated therapy of glioblastoma multiforme.Nanomedicine. 2015 Jan;11(1):109-18.2. Carew JS, et al. Lucanthone is a novel inhibitor of autophagy that induces cathepsin D-mediated apoptosis. J Biol Chem. 2011 Feb25;286(8):6602-13.McePdfHeightCaution: Product has not been fully validated for medical applications.
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