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Locostatin
- UIC 1005
- Optical Purity: Optically pure
- Soluble in DMSO and EtOH
- MF: C14H15NO3
- MW: 245.27
Description
Locostatin (UIC-1005) is a cell-permeable non-toxic RKIP inhibitor that disrupts RKIP interactions with Raf-1 and GRK2. It blocks epithelial cell migration, controls cell growth, and induces T-cell anergy. Notably, its effects on cell migration and the cytoskeleton also occur through pathways independent of RKIP and classical Raf/MAP kinase signaling.
Locostatin (UIC-1005) is used to probe RKIP/Raf pharmacology across diverse biochemical profiles, cell lines, and translational disease models.
Key Features
- RKIP/Raf inhibitor
- Useful probe for RKIP/Raf pathway modulation
- Supports RKIP/Raf pathway-specific assay development
Applications
- RKIP/Raf pharmacology and target-validation studies
- RKIP/Raf pathway and signaling assays
- Disease-relevant cellular and translational model systems
- Receptor signaling, ligand profiling and functional response assays
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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