Description
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
Uses
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).
Definition
ChEBI: 5-[[5-bromo-2-[(2-bromophenyl)methoxy]phenyl]methylidene]-2-sulfanylidene-1,3-thiazolidin-4-one is an aromatic ether.
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].
IC 50
900 nm: blocks human phosphatase of regenerating liver 3 (prl-3) in vitro.
References
1) Ahn et al. (2006), Synthesis and biological evaluation of rhodanine derivatives as PRL-3 inhibitors; Bioorg. Med. Chem. Lett., 16 2996
2) Min et al. (2013), Rhodanine-based PRL-3 inhibitors blocked the migration and invasion of metastatic cancer cells; Bioorg. Med. Chem. Lett., 23 3769
3) Zhao et al. (2011), PRL-3, a metastasis associated tyrosine phosphatase, is involved in FLT3-ITD signaling and implicated in anti-AML therapy; PLoS One, 6(5) e19798
4) Tian et al. (2012), Phosphatase of regenerating liver-3 directly interacts with integrin β1 and regulates its phosphorylation at tyrosine 783; BMC Biochemistry, 13 22
