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

Available Options

Size:PriceQuantity 
5 mg$48.00
25 mg$135.00

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
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:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

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