4-(4-甲基-1-哌嗪基)-7-硝基-2,1,3-苯并二唑 3-氧化物-abs813939

NSC-207895 (XI-006) is a derivative of nitrobenzofuroxan and an anticancer agent with an EC50 of 1 μM. NSC-207895 (XI-006) is a highly electrophilic compound known to have both antitumor and mutagenic activities. NSC-207895 (XI-006) may lead to the damage of DNA that inhibits the growth of tumors. NSC-207895 (XI-006) strikingly prevented the expression of MDMX which is a p53-binding protein and modulate the activities and stabilities of p53. NSC-207895 (XI-006) is less toxic and reduced the activities of MDMX promoter in a dose-dependent manner. Moreover,NSC-207895 (XI-006)  possibly decreased the expression of MDMX via suppressing MDMX transcription. However, NSC-207895 (XI-006) induced the expression of MDM2 which is also a p53 downstream gene, despite to a less extent. In addition, NSC-207895 (XI-006) also upregulated the expression of p53 in MCF-7 cells that led to increased expression of proapoptotic genes including PUMA, BAX, as well as PIG3. Notably, NSC-207895 (XI-006), also called a small-molecule p53 activator, gives rise to MCF-7 cells to experience apoptosis and decrease the viability of cancer cells along with nutlin-3a, which dissociated the MDM2-p53 complex.