CAS:2275619-53-7Methyl 2-(N-(5-bromo-4-fluoro-2-methylphenyl)sulfamoyl)-5-(3,5-dichlorophenylsulfonamido)benzoate

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Synonyms: Methyl 2-(N-(5-bromo-4-fluoro-2-methylphenyl)sulfamoyl)-5-(3,5-dichlorophenylsulfonamido)benzoate

DL-800 is an allosteric and selective SIRT6 activator with EC50 of 10.3μM.

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18817579266

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实验数据

技术信息

CAS号

2275619-53-7

储存条件

分子式

C21H16BrCl2FN2O6S2

运输

蓝冰

分子量

626.30

别名

Methyl 2-(N-(5-bromo-4-fluoro-2-methylphenyl)sulfamoyl)-5-(3,5-dichlorophenylsulfonamido)benzoate

溶解度

DMSO	125.0 mg/mL (199.6 mM)
Water	insoluble

动物实验配方

生物活性

描述SIRT6, responsible for deacetylation of histone H3 N^ε-acetyl-lysines 9 (H3K9ac) and 56 (H3K56ac), is a tumor suppressor which has frequently been found to have low expression in various cancers. MDL-800 is a selective SIRT6 activator. It increased the deacetylase activity of SIRT6 by up to 22-fold and led to a global decrease in H3K9ac and H3K56ac levels in human hepatocellular carcinoma (HCC) cells. Also, it inhibited the proliferation of HCC cells via SIRT6-driven cell-cycle arrest and was effective in a tumor xenograft model.
作用机制MDL-800 can bind to an allosteric site of SIRT6 to increase its activity.
动物研究
剂量
Mice: 50 mg/kg - 150 mg/kg^[1] (i.p.)

给药途径
i.p.