PRL-3 INHIBITOR I Property

Density 

1.85±0.1 g/cm3(Predicted)

storage temp. 

−20°C

solubility 

DMSO: >10mg/mL

form 

Yellow solid

pka

7.11±0.50(Predicted)

color 

yellow

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.

Safety

Hazard Codes 

Xi,N

Risk Statements 

36/37/38-50/53

Safety Statements 

26-36/37-60-61

RIDADR 

UN 3077 9/PG 3

WGK Germany 

3

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

H410Very toxic to aquatic life with long lasting effects

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P273Avoid release to the environment.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P501Dispose of contents/container to..…

PRL-3 INHIBITOR I Chemical Properties,Usage,Production

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