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(E/Z)-Locostatin

Names

[ CAS No. ]:
133812-16-5

[ Name ]:
(E/Z)-Locostatin

[Synonym ]:
MFCD00278769

Biological Activity

[Description]:

(E/Z)-Locostatin ((E/Z)-UIC-1005) is a racemic of 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 aggravates thioacetamide (HY-Y0698)-induced acute liver failure in mice [1][2][3].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Others >> Others

[Target]

RKIP[3]


[References]

[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.  

Chemical & Physical Properties

[ Density]:
1.205g/cm3

[ Boiling Point ]:
351ºC at 760mmHg

[ Melting Point ]:
84-88ºC(lit.)

[ Molecular Formula ]:
C14H15NO3

[ Molecular Weight ]:
245.27400

[ Flash Point ]:
166.1ºC

[ Exact Mass ]:
245.10500

[ PSA ]:
46.61000

[ LogP ]:
2.09050

[ Vapour Pressure ]:
4.22E-05mmHg at 25°C

[ Index of Refraction ]:
1.57

Safety Information

[ Hazard Codes ]:
Xn


Related Compounds