133812-16-5 Usage
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
Check Digit Verification of cas no
The CAS Registry Mumber 133812-16-5 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,3,3,8,1 and 2 respectively; the second part has 2 digits, 1 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 133812-16:
(8*1)+(7*3)+(6*3)+(5*8)+(4*1)+(3*2)+(2*1)+(1*6)=105
105 % 10 = 5
So 133812-16-5 is a valid CAS Registry Number.
InChI:InChI=1/C14H15NO3/c1-2-6-13(16)15-12(10-18-14(15)17)9-11-7-4-3-5-8-11/h2-8,12H,9-10H2,1H3/b6-2+
133812-16-5Relevant articles and documents
Preparation method of chiral intermediate of omarigliptin
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Paragraph 0015; 0040-0042, (2018/04/01)
The invention discloses a novel synthesis method for preparing a chiral intermediate of omarigliptin. The method comprises the following steps: carrying out amidation, alder condensation, hydrazine hydrate condensation, rearrangement, Boc addition, ring opening and Grubbs catalyst ring formation on starting raw materials including crotonyl chloride and (S)-4-benzyl-2-oxazolidone and carrying out hydrolysis to obtain the chiral intermediate (IX). The preparation method disclosed by the invention has the advantages of relatively low cost, easiness for obtaining raw materials and relatively high yield, so that the preparation method is suitable for industrial production. The formula (IX) is shown in the description.
