Abstract: Akt (PKB), a kind of serine/threonine protein kinase, is the downstream target of phosphatidyl inositol-3 kinase (PI3K), and it can promote cell growth, metabolism, apoptosis, angiogenesis, and other important process of cell biology by affecting phosphorylation of its downstream substrates. There exists the phenomenon of Akt overexpression or activity disorder in a variety of human malignant tumor. Research shows that it can effectively inhibit tumor cell proliferation by inhibiting the activity of Akt. Design and development of novel Akt inhibitors has been one of the hot spot of antitumor drug research. Akt inhibitor consists of PH structure domain inhibitors, ATP competitive inhibitors, allosteric inhibitors, etc., and currently, several small molecule Akt inhibitors have been into clinical stage. This paper reviews Akt inhibitory activity and feature of different Akt inhibitors for guiding the development of novel antitumor drugs.