IC50: 900 nM: blocks human phosphatase of regenerating liver 3 (PRL-3) in vitro.

PRL-3 inhibitor, a cell-permeable benzylidene rhodamine compound, potently dampens PRL-3 and inhibits other phosphatases with minimal activity. It has been demonstrated that PRL-3 inhibitor can be used as therapeutics for the treatment of cancer. PRL-3 is a member of the regenerating liver family tyrosine phosphatases and plays vital roles in cell proliferation, migration, invasion, and motility, and thus leads to cancer metastasis.

In vitro: PRL-3 inhibitor, in a dose-dependent fashion, blocked the dephosphorylation of DiFMUP by PRL-3 and strongly suppressed the activity of PRL-3 phosphatase in PRL-3 overexpressing DLD-1 colon tumor cells [DLD-1 (PRL-3)]. Also, PRL-3 inhibitor dose-dependently blocked the migration of DLD-1 (PRL-3) cells, however, it did not inhibit the proliferation of DLD-1(PRL-3) cells, suggesting that PRL-3 inhibitor significantly blocked cell immigration and invasion without cytotoxicity [1].

In vivo: Up to now, in vivo study of PRL-3 Inhibitor is still in the development stage.

Reference:
[1].  Min, G., Lee, S., Kim, H., Han, Y., Lee, R., & Jeong, D. et al. Rhodanine-based PRL-3 inhibitors blocked the migration and invasion of metastatic cancer cells. Bioorganic & Medicinal Chemistry Letters. 2013; 23(13): 3769-3774.