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NSC 146109 is an activator of the tumor suppressor p53 that increases expression of p53 and the p53 target DR5 in wild-type and p53-knockout HCT116 colon adenocarcinoma cells.1 It is selective for p53, having no effect on p73 expression in HCT116 cells at a concentration of 2 μM. NSC 146109 activates p53, which induces cell accumulation in the sub-G0/G1 phase and apoptosis in MCF-7 breast cancer cells.2 It increases p53 expression, decreases expression of the p53 suppressor MDMX, and reduces viability in a panel of breast cancer cell lines when used at a concentration of 0.5 μM. NSC 146109 also reduces growth of AMC-HN9 head and neck carcinoma (HNC) cells in vitro and in vivo when administered alone or in combination with cisplatin (Item No. 13119) in a mouse xenograft model at a dose of 70 mg/kg.3
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