4-(4-Methyl-1-piperazinyl)-7-nitrobenzofurazane 3-oxide

Описание

NSC 207895 is an inhibitor of the p53-binding protein MDMX. It decreases MDMX promoter activity in a reporter assay using HT-1080 cells in a concentration-dependent manner. NSC 207895 (5 μmol/L) decreases the expression and protein levels of MDMX and increases the expression of the p53 target gene CDKN1 (p21) in MCF-7 cells overexpressing MDMX. It also increases the expression of the pro-apoptotic genes PUMA, Bax, and PIG3. NSC 207895 (5 μmol/L) induces apoptosis and decreases cell viability in MCF-7 cells in a p53-dependent manner. It also induces p53-independent apoptosis in wild-type, mutated, and truncated p53 Ewing sarcoma cell lines (IC₅₀s = 98.9-1,613, 236-299, and 121-396 nM, respectively) selectively over wild-type and p53-null osteosarcoma cells (IC₅₀s = 3,690-5,416 and 2,143 nM, respectively).

Использование

NSC-207895 is an anticancer agent and p53 activator. This compound decreases the expression of MDMX but also induced the expression of MDM2. It can also be used in pharmacological activity and therapeutic use of reviving antibiotics in relation to prepared efflux pump inhibitors that interact with AcrA, membrane fusion protein of AcrAB-TolC multidrug efflux pump.