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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作靶點(diǎn): HDAC; Autophagy作通路: Cell Cycle/DNA Damage; Epigenetics; Autophagy儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1
2、month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 150 mg/mL (459.63 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液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請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度,選擇合適的溶劑配制儲(chǔ)備液,并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性
3、 Scriptaid種組蛋去?;?(HDAC) 抑制劑,可于癌癥研究。IC50 & Target HDAC體外研究Scriptaid (1 g/mL) treatment inhibits cell growth in breast cancer cell lines, results in increased accumulation1/2 Master of Small Molecules 您邊的抑制劑師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.體內(nèi)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.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) 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 您邊的抑制劑師www.MedChemECa
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