893449-38-2

Basic information

• Product Name: PRL-3 INHIBITOR I
• Synonyms: Phosphatase of regenerating liver-3, Inhibitor I;PRL-3 Inhibitor;PRL-3 INHIBITOR I;Phosphatase of regenerating liver-3, Inhibitor I, 5-[[5-bromo-2-[(2-bromophenyl)methoxy]phenyl]methylene]-2-thioxo-4-thiazolidinone;5-[[5-bromo-2-[(2-bromophenyl)methoxy]phenyl]methylene]-2-thioxo-4-thiazolidinone
• CAS NO: 893449-38-2
• Molecular Formula: C17H11Br2NO2S2
• Molecular Weight: 485.219
• Mol File: 893449-38-2.mol
• Article Data: 1

Chemical Properties

• Appearance: yellow/
• Storage Temp.: −20°C
• Solubility: DMSO: >10mg/mL
• Stability: Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
• CAS DataBase Reference: PRL-3 INHIBITOR I(CAS DataBase Reference)
• NIST Chemistry Reference: PRL-3 INHIBITOR I(893449-38-2)
• EPA Substance Registry System: PRL-3 INHIBITOR I(893449-38-2)

Safety Data

• Hazard Codes: Xi,N
• Statements: 36/37/38-50/53
• Safety Statements: 26-36/37-60-61
• RIDADR: UN 3077 9/PG 3
• WGK Germany: 3
• Hazardous Substances Data: 893449-38-2(Hazardous Substances Data)

Usage

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).

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

Upstream product

• 141-84-4 2-thioxo-4-thiazolidinone 
• 1039844-65-9 C₁₄H₁₀Br₂O₂ 

Relevant articles and documents

Rhodanine-based PRL-3 inhibitors blocked the migration and invasion of metastatic cancer cells

PRL-3, phosphatase of regenerating liver-3, plays a role in cancer progression through its involvement in invasion, migration, metastasis, and angiogenesis. We synthesized rhodanine derivatives, CG-707 and BR-1, which inhibited PRL-3 enzymatic activity wi