HIV-1 inhibitor-53 is a dual HIV-1 protease and reverse transcriptase inhibitor. HIV-1 inhibitor-53 inhibits HIV-1 protease (PR) and reverse transcriptase (RT) activity with IC 50 values of 1.93 nM and 2.35 μM, respectively. HIV-1 inhibitor-53 can be used for the research of acquired immune deficiency syndrome (AIDS).