Identification | Back Directory | [Name]
(S)-(+)-4-BENZYL-3-CROTONYL-2-OXAZOLIDI& | [CAS]
133812-16-5 | [Synonyms]
Locostatin (E/Z)-Locostatin 4-benzyl-3-crotonyl-2-oxazolidinone (S)-(+)-4-BENZYL-3-CROTONYL-2-OXAZOLIDI& Cell Sheet Migration Inhibitor, Locostatin (S)-4-Benzyl-3-(but-2-enoyl)oxazolidin-2-one (S,E)-4-benzyl-3-(but-2-enoyl)oxazolidin-2-one, 98% 2-Oxazolidinone, 3-(1-oxo-2-buten-1-yl)-4-(phenylmethyl)-, (4S)- | [Molecular Formula]
C14H15NO3 | [MDL Number]
MFCD00278769 | [MOL File]
133812-16-5.mol | [Molecular Weight]
245.27 |
Chemical Properties | Back Directory | [Melting point ]
84-88 °C(lit.) | [Boiling point ]
351.0±25.0 °C(Predicted) | [density ]
1.205±0.06 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
Soluble in DMSO (60 mg/ml) | [form ]
solid | [pka]
-1?+-.0.40(Predicted) | [color ]
Off-white | [Stability:]
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
Hazard Information | Back Directory | [Description]
Locostatin (133812-16-5) inhibits cell migration by disrupting the interaction between Raf kinase inhibitor protein (RKIP) and Raf-1 kinase.1 Locostatin covalently binds to His86 of RKIP and also disrupts its interaction with G protein-coupled receptor kinase 2.2 Effectively inhibits cytokine release by human lymphocytes.3? Alleviates CCl4-induced liver fibrosis in a mouse model.4 A useful probe to explore the complex functions of RKIP in cell physiology.5 | [Uses]
Locostatin is a cell permeable, potent inhibitor of Raf kinase inhibitor protein (RKIP)/Raf1 kinase interaction and an inhibitor of cell migration | [References]
Zhu et al. (2005), A chemical inhibitor reveals the role of Raf kinase inhibitor protein in cell migration; Chem. Biol., 12 981
Beshir et al. (2011), 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. 2 47
Menoret et al. (2009), The oxazolidinone derivative locostatin induces cytokine appeasement; J. Immunol. 183 7489
Ma et al. (2019), Locostatin Alleviates Liver Fibrosis Induced by Carbon Tetrachloride in Mice; Dig. Dis. Sci. 64 2570
Mc Henry et al. (2008), Raf kinase inhibitor protein positively regulates cell-cell adhesion; J. Cell Biochem. 103 972 |
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Energy Chemical
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