PRL-3 INHIBITOR I

P0108 (893449-38-2) is a potent inhibitor of phosphatase of regenerating liver-3 (PRL-3), IC50=0.9 μM.1? Reduces the invasive properties of mouse melanoma B16F10 cells in a cellular model.2 Sensitizes PRL-3-expressing cancer cells to chemotherapeutics.3 Inhibits dephosphorylation of tyrosine-783 of integrin β1 in BGC823 and SW480 cells.4

5-[[5-Bromo-2-[(2-bromophenyl)methoxy]phenyl]methylene]-2-thioxo-4-thiazolidinone is a a cell-permeable benzylidene rhodamine that inhibits Phosphatase of regenerating liver 3 (PRL-3).

ChEBI: 5-[[5-bromo-2-[(2-bromophenyl)methoxy]phenyl]methylidene]-2-sulfanylidene-1,3-thiazolidin-4-one is an aromatic ether.

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].

900 nm: blocks human phosphatase of regenerating liver 3 (prl-3) in vitro.

[1] JOONG-KWON CHOI  et al. et al. Synthesis and Biological Evaluation of Rhodanine Derivatives as PRL-3 Inhibitors.[J]. ChemInform, 2006, 37 34. DOI:10.1002/chin.200634126
[2] GARAM MIN . Rhodanine-based PRL-3 inhibitors blocked the migration and invasion of metastatic cancer cells[J]. Bioorganic & Medicinal Chemistry Letters, 2013, 23 13: Pages 3769-3774. DOI:10.1016/j.bmcl.2013.04.092
[3] JIANBIAO ZHOU. PRL-3, a metastasis associated tyrosine phosphatase, is involved in FLT3-ITD signaling and implicated in anti-AML therapy.[J]. PLoS ONE, 2011: e19798. DOI:10.1371/journal.pone.0019798
[4] WEI TIAN. Phosphatase of regenerating liver-3 directly interacts with integrin β1 and regulates its phosphorylation at tyrosine 783.[J]. BMC Biochemistry, 2012, 13: 22. DOI:10.1186/1471-2091-13-22