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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEScriptaidCat. No.: HY-15489CAS No.: 287383-59-9Synonyms: Scriptide; GCK1026分式: CHNO分量: 326.35作靶点: HDAC; Autophagy作通路: Cell Cycle/DNA Damage; Epigenetics; Autophagy储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1

2、month溶解性数据体外实验 DMSO : 150 mg/mL (459.63 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.0642 mL 15.3210 mL 30.6419 mL5 mM 0.6128 mL 3.0642 mL 6.1284 mL10 mM 0.3064 mL 1.5321 mL 3.0642 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

3、 Scriptaid种组蛋去酰化酶 (HDAC) 抑制剂,可于癌症研究。IC50 & Target HDAC体外研究Scriptaid (1 g/mL) treatment inhibits cell growth in breast cancer cell lines, results in increased accumulation1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEof both acetyl H3 and acetyl H4 proteins in MDA-MB-231, MDA-MB-435, and Hs578t ce

4、lls. Scriptaid alsoinhibits cell growth of MDA-MB-231, MDA-MB-435, and Hs578t cell lines, with IC50s of 0.5-1.0 g/mL.Scriptaid (0.1-1.0 g/mL) induces ER and PR mRNA expression in a dose dependent manner; when it iscombined with AZA, they enhance ER expression and induce a functional ER protein 1. Sc

5、riptaid and SAHApreferentially inhibit the Class I histone deacetylases, hdac1, 2, and 3. Scriptaid is a potent anti-T. gondiicompound with low cytotoxicity, and the IC50 is 39 nM. Scriptaid has atypical effects in T. gondiiinfectedHS68 cells 2. Scriptaid inhibits the growth of HeLa cells with IC50

6、of 2 M at 48 h in a dose-dependentmanner. Scriptaid also affects cell-cycle and apoptosis 3.体内研究 Scriptaid (3.5 g/g mouse, i.p.) clearly inhibits tumor growth in a xenograft mouse model 1.PROTOCOLCell Assay 1 IC50 concentrations of Scriptaid are determined in MDA-MB-231, MDA-MB-435 and Hs578t cells

7、by MTTassay. For cell growth assays, MDA-MB-231, MDA-MB-435, and Hs578t cells are plated at a cell density of5000 cells/well in 12 well plates and treated with 1.0 g/mL Scriptaid for up to 3 days. Cells are counted dailyusing a Coulter counter. Percent growth inhibition is determined by comparison o

8、f treated and untreated cells1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Four to six week old athymic female nude mice are housed under laminar flow hoods in an environmentallyAdministration 1 controlled pathogen free animal facility for th

9、e duration of experiments. Mice are injected with 2106 MDA-MB-231 human breast cancer cells into each flank. Tumors are allowed to grow to approximately 0.1 cm3 indiameter before treatment. Mice are then treated with Scriptaid (3.5 g/g mouse), TSA (0.5 g/g mouse), orDMSO vehicle intraperitoneally fo

10、r five consecutive days with 2 days rest each week for a total of 4 weeks.Individual tumor measurements are recorded from each flank weekly 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Proc Natl Acad Sci U S A. 2019 Feb 19;116(8):2961-2

11、966.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Keen JC, et al. A novel histone deacetylase inhibitor, scriptaid, enhances expression of functional estrogen receptor alpha (ER) in ERnegative human breast cancer cells in combination with 5-aza 2-deoxycytidine. Breast Cancer

12、Res Treat. 2003 Oct;81(3):177-86.2. Strobl JS, et al. Scriptaid and suberoylanilide hydroxamic acid are histone deacetylase inhibitors with potent anti-Toxoplasma gondiiactivity in vitro. J Parasitol. 2007 Jun;93(3):694-700.3. Janaki Ramaiah M, et al. Scriptaid cause histone deacetylase inhibition and cell cycle arrest in HeLa cancer cells: A study on structuraland functional aspects. Gene. 2017 Sep 5;627:379-386.McePdfHeight2/2 Master of Small Molecules 您边的抑制剂师www.MedChemECa

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