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Locostatin
- UIC 1005- Optical Purity: Optically pure
- Soluble in DMSO and EtOH
- MF: C14H15NO3
- MW: 245.27
Description
Non-toxic Raf kinase inhibitory protein (RKIP) inhibitor; disrupts the interaction of RKIP, not only with Raf-1 kinase, but also with GRK2; Locostatin is an inhibitor of cell sheet migration and cell growth in an epithelial cell proliferation assay, and it induced T cell anergy by blocking cytokine production after Ag recall. Other evidence suggested that Locostatin’s effects on cytoskeletal structure and migration are caused through mechanisms independent of its binding to RKIP and Raf/MAP kinase signaling.
More Information
| Parent CAS No. | 90719-30-5 |
|---|---|
| Chemical Name | (S,E)-4-benzyl-3-but-2-enoyloxazolidin-2-one |
| SMILES | O1C[C@H](CC2=CC=CC=C2)N(C(=O)/C=C/C)C1=O |&1:2,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C10H15NO3/c1-4-5-9(12)8-6-14-10(13)11(8)7(2)3/h4-5,7-8H,6H2,1-3H3/b5-4+/t8-/m0/s1 |
| InChiKey | OUALYNREYGXYFG-ZJELKQJVSA-N |
| CID | 90478199 |
| Short Description | RKIP/Raf inhibitor |
References
- KT Mc Henry et al. A non-antibacterial oxazolidinone derivative that inhibits epithelial cell sheet migration. Chembiochem. 2002 Nov 4;3(11):1105-11.
- AN Shemon et al. Raf Kinase Inhibitory Protein protects cells against locostatin-mediated inhibition of migration. PLoS One. 2009 Jun 24;4(6):e6028.
- A Ménoret et al. The oxazolidinone derivative locostatin induces cytokine appeasement. J Immunol. 2009 Dec 1;183(11):7489-96.
- AB Beshir 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.
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