p53 Activator 2 (compound 10ah) intercalats into DNA and results in significant DNA double-strand break.p53 Activator 2 increases the expression of p53 , p-p53, CDK4 , p21 to cause cell cycle arrest at G2/M phase.p53 Activator 2 induce apoptosis and significantly down-regulates the anti-apoptosis proteins Bcl-2 , Bcl-xL and the levels of cyclin B1.p53 Activator 2 has anti-proliferation activity against MGC-803 cells, with an IC 50 of 1.73 µM. p53 Activator 2 displays potent anticancer efficiency against MGC-803 xenograft tumors models.