生物活性 | |||
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描述 | SIRT6, responsible for deacetylation of histone H3 Nε-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. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.60mL 0.32mL 0.16mL |
7.98mL 1.60mL 0.80mL |
15.97mL 3.19mL 1.60mL |
参考文献 |
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