Locostatin is primarily recognized for its role as a selective inhibitor of cell migration, making it a valuable tool in research related to cancer and inflammatory diseases. It does not prevent cell proliferation but specifically interferes with the movement of cells, which is critical in processes like tumor metastasis and immune cell trafficking. This unique property allows scientists to study the mechanisms behind cell motility without disrupting overall cell growth.

It has been used in experimental models to probe signaling pathways involved in cytoskeletal reorganization, particularly those linked to the Rho family of GTPases, which regulate cell shape and movement. Due to its ability to suppress directed cell migration, locostatin is investigated for potential therapeutic applications in preventing cancer spread and modulating immune responses. However, it remains mainly a research compound and is not used clinically. Its application is largely confined to in vitro studies and preclinical research settings.