Abstract: With various clinical trials being conducted of more than ten small Akt inhibitors in these years, the potential of Akt as a promising anti-cancer drug target has been validated. In this review, the structure and function of Akt as well as some promising small Akt inhibitors such as Perifosine, MK-2206 and GSK2110183 are going to be introduced. Additionally, the preclinical and clinical research will be illustrated in detail.