Phosphatase of regenerating liver 3 (PRL-3; also known as PTP4A3) plays critical roles in cell proliferation, motility, and invasion, and thus contributes to cancer metastasis. PRL-3 inhibitor is a cell-permeable benzylidene rhodamine that inhibits PRL-3 (IC50 = 900 nM for human PRL-3 in vitro), with minimal activity against other phosphatases. It reduces the invasion of mouse melanoma B16F10 cells in a cell-based assay. PRL-3 inhibitor has been used to elucidate the actions of this enzyme, demonstrating that it dephosphorylates Tyr783 on integrin β1 and modulates VEGF-mediated endothelial cell migration. It dose-dependently inhibits the growth and triggers apoptosis in cancer cell lines.
