| Bioactivity | Locostatin (UIC-1005) is a potent RKIP inhibitor. Locostatin binds Raf kinase inhibitor RKIP protein and disrupts the interaction of RKIP with Raf-1 kinase and G protein-coupled receptor kinase 2. Locostatin inhibits cell proliferation and migration. Locostatin can be used to synthesize chemical probes toward PEBP-proteins. Locostatin aggravates thioacetamide (HY-Y0698)-induced acute liver failure in mice [1][2][3]. | ||||||||||||
| Target | RKIP | ||||||||||||
| Invitro | Locostatin (200 µM；37 °C；6 小时) 破坏 RKIP 与 Raf-1 和 GRK2 的相互作用[1]。Locostatin (50 µM；0-48 小时) 抑制 MDCK 细胞的增殖和迁移[2]。 Cell Proliferation Assay[2] Cell Line: | ||||||||||||
| In Vivo | Locostatin (0.5 mg/kg；腹腔注射；每天一次，连续 7 天) 加重硫代乙酰胺 (HY-Y0698) 诱导的小鼠急性肝衰竭[3]。 Animal Model: | ||||||||||||
| Name | Locostatin | ||||||||||||
| CAS | 90719-30-5 | ||||||||||||
| Formula | C14H15NO3 | ||||||||||||
| Molar Mass | 245.27 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Beshir AB, 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. [2]. Mc Henry KT, et al. A non-antibacterial oxazolidinone derivative that inhibits epithelial cell sheet migration. Chembiochem. 2002 Nov 4;3(11):1105-11. [3]. Lin X, et al. Inhibition of RKIP aggravates thioacetamide-induced acute liver failure in mice. Exp Ther Med. 2018 Oct;16(4):2992-2998. |