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Locostatin | RKIP/Raf-1 kinase disruptor

CAS:
133812-16-5
Catalog Number:
10-5381
Activity:
RKIP/Raf-1 kinase disruptor
Chemical Names:
(4S)-3-[(E)-But-2-enoyl]-4-benzyl-2-oxazolidinone; UIC-1005
Molecular Weight:
245.28
Molecular Formula:
C14H15O3
Solubility:
Soluble in DMSO (60 mg/ml)
Physical Properties:
Off-white solid
Purity:
>98% TLC
NMR (Conforms)
Storage Temperature:
-20°C
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.
Shipping Code:
RT

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

References:

  1. Zhu et al. (2005), A chemical inhibitor reveals the role of Raf kinase inhibitor protein in cell migration; Chem. Biol., 12 981
  2. 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
  3. Menoret et al. (2009), The oxazolidinone derivative locostatin induces cytokine appeasement; J. Immunol. 183 7489
  4. Ma et al. (2019), Locostatin Alleviates Liver Fibrosis Induced by Carbon Tetrachloride in Mice; Dig. Dis. Sci. 64 2570
  5. Mc Henry et al. (2008), Raf kinase inhibitor protein positively regulates cell-cell adhesion; J. Cell Biochem. 103 972
Locostatin | RKIP/Raf-1 kinase disruptor is also available in the Cellular Metabolism Library.
CAS:
133812-16-5
Catalog Number:
10-5381
Activity:
RKIP/Raf-1 kinase disruptor
Chemical Names:
(4S)-3-[(E)-But-2-enoyl]-4-benzyl-2-oxazolidinone; UIC-1005
Molecular Weight:
245.28
Molecular Formula:
C14H15O3
Solubility:
Soluble in DMSO (60 mg/ml)
Physical Properties:
Off-white solid
Purity:
>98% TLC
NMR (Conforms)
Storage Temperature:
-20°C
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.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

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