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Bestatin (Ubenimex) competitively inhibits many aminopeptidases, including B, N and leucine aminopeptidases. Ubenimex is a microbial metabolite and dipeptide with potential immunomodulatory and antitumor activities. Aminopeptidases has been implicated in the process of cell adhesion and invasion of tumor cells. Therefore, inhibiting aminopeptidases may partially attribute to the antitumor effect of ubenimex. This agent also activates T lymphocyte, macrophage, and bone marrow stem cell as well as stimulates the release of interleukin-1 and -2, thus further enhances its antitumor activity.

Bestatin hydrochloride (Ubenimex hydrochloride) is an inhibitor of aminopeptidase N (APN) CD13 and aminopeptidase B.

Bestatin trifluoroacetate (Ubenimex trifluoroacetate) is a CD13 (Aminopeptidase N)/APN and leukotriene A4 hydrolase inhibitor that is often used in cancer research.