Locostatin

Locostatin (UIC-1005) is a potent RKIP inhibitor. Locostatin binds Raf kinase inhibitor RKIP protein and disrupts the interaction of RKIP with Raf-1 kinase and G protein-coupled receptor kinase 2. Locostatin inhibits cell proliferation and migration. Locostatin can be used to synthesize chemical probes toward PEBP-proteins. Locostatin aggravates thioacetamide (HY-Y0698) -induced acute liver failure in mice [1][2][3].

Product Specifications

CAS Number

[90719-30-5]

Product Name Alternative

UIC-1005

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

G Protein-coupled Receptor Kinase (GRK) ; Raf

Type

Reference compound

Related Pathways

GPCR/G Protein; MAPK/ERK Pathway

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/locostatin.html

Purity

99.88

Solubility

DMSO : 100 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C1OC[C@H](CC2=CC=CC=C2)N1C(/C=C/C)=O

Molecular Formula

C14H15NO3

Molecular Weight

245.27

Precautions

H302, H315, H319, H335

References & Citations

[1]Beshir AB, et al. Locostatin Disrupts Association of Raf Kinase Inhibitor Protein With Binding Proteins by Modifying a Conserved Histidine Residue in the Ligand-Binding Pocket. For Immunopathol Dis Therap. 2011;2 (1) :47-58.|[2]Mc Henry KT, et al. A non-antibacterial oxazolidinone derivative that inhibits epithelial cell sheet migration. Chembiochem. 2002 Nov 4;3 (11) :1105-11.|[3]Lin X, et al. Inhibition of RKIP aggravates thioacetamide-induced acute liver failure in mice. Exp Ther Med. 2018 Oct;16 (4) :2992-2998.