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A high-throughput screening identifies histone deacetylase inhibitors as therapeutic agents against medulloblastoma

机译:高通量筛选将组蛋白脱乙酰基酶抑制剂鉴定为抗髓母细胞瘤的治疗剂

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摘要

High-throughput screen identifies dacinostat and quisinostat that reduce cell viability of Daoy and D283 cells. 125 compounds were assayed for their IC values after the screening of 12,800 compounds. Blue bars represent the concentration range interrogated and black points indicate the IC value derived from the curve fit. The red line represents the 1 μM IC cutoff used to identify the 46 most potent compounds. Compounds having names too long to fit on the plot axis are identified by their compound identifier; their names are as follows: SJ000831486-1 = BML285 (diaminoquinazoline); SJ000287267-1 = cephaeline dihydrochloride heptahydrate; SJ000311301-2 = NA; SJ000312176-2 = aurora kinase/CDK inhibitor; SJ000287062-3 = 1-benzyloxycarbonylaminophenethyl chloromethyl ketone; SJ000287130-1 = lysyltryptophanyl-lysine acetate. Cmpd Conc, compound concentration. , The dose response curves (based on MTT assays) for cell viability of Daoy and D283 cells after treated with dacinostat and quisinostat for 48 h at the indicated concentrations
机译:高通量屏幕可识别达西诺司他和拟西斯达司特,它们可降低Daoy和D283细胞的细胞活力。在筛选出12,800种化合物后,对125种化合物的IC值进行了测定。蓝色条表示所查询的浓度范围,黑点表示从曲线拟合得出的IC值。红线代表用于识别46种最有效化合物的1μMIC截止值。名称过长而无法在绘图轴上显示的化合物由其化合物标识符标识;其名称如下:SJ000831486-1 = BML285(二氨基喹唑啉); SJ000287267-1 =头孢菌灵二盐酸盐七水合物; SJ000311301-2 = NA; SJ000312176-2 =α极光激酶/ CDK抑制剂; SJ000287062-3 = 1-苄氧基羰基氨基苯乙基氯甲基酮; SJ000287130-1 =赖氨酸隐氨酰-赖氨酸乙酸酯。 Cmpd Conc,化合物浓度。 ,在指定浓度下用达西司他和喹诺司他处理48小时后,Daoy和D283细胞的细胞存活率的剂量响应曲线(基于MTT分析)

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