Introduction:Basic information about CAS 90719-30-5|Locostatin, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | Locostatin |
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| CAS Number | 90719-30-5 | Molecular Weight | 197.23100 |
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| Density | 1.205 g/cm3 | Boiling Point | 351ºC at 760 mmHg |
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| Molecular Formula | C10H15NO3 | Melting Point | 84-88ºC(lit.) |
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| MSDS | USA | Flash Point | 166.1ºC |
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Names
| Name | (n-crotonyl)-(4s)-isopropyl-2-oxazolidinone |
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| Synonym | More Synonyms |
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Locostatin BiologicalActivity
| Description | 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]. |
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| Related Catalog | Research Areas >>CancerSignaling Pathways >>Others >>Others |
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| Target | RKIP[3] |
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| In Vitro | 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: MDCK cells Concentration: 50 µM Incubation Time: 0-48 h Result: Inhibited cell proliferation and sheet migration. |
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| 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: 6 weeks, 18-22 g, male ICR mice (TAA model; injected intraperitoneally with 300 mg/kg TAA once a day for 2 days)[3] Dosage: 0.5 mg/kg Administration: I.p.; once a day for 7 days Result: Decreased the expression of RKIP, led to more severe damage, such as steatosis and hepatic lesions, increased the production of ROS in the liver and TNF-α, IL-6 and IL-1β in the sera of mice with acute liver injury, inhibitd Nrf2 and HO-1 expression in the livers of mice, induced NF-κB activation in the livers of mice,increased the phosphorylation of JNK, p38 and ERK in liver tissues. |
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| References | [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. |
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Chemical & Physical Properties
| Density | 1.205 g/cm3 |
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| Boiling Point | 351ºC at 760 mmHg |
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| Melting Point | 84-88ºC(lit.) |
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| Molecular Formula | C10H15NO3 |
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| Molecular Weight | 197.23100 |
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| Flash Point | 166.1ºC |
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| Exact Mass | 197.10500 |
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| PSA | 46.61000 |
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| LogP | 1.29870 |
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| Appearance of Characters | white to off-white |
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| InChIKey | UTZAFVPPWUIPBH-QSLRECBCSA-N |
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| SMILES | CC=CC(=O)N1C(=O)OCC1Cc1ccccc1 |
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| Storage condition | 2-8°C |
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| Water Solubility | DMSO: ≥30mg/mL |
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Safety Information
| Risk Phrases | 24/25 |
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| Safety Phrases | 24/25 |
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| RIDADR | NONH for all modes of transport |
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| WGK Germany | 3 |
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| HS Code | 29349990 |
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Synonyms
| (4S)-N-Crotonyl-4-benzyl-2-oxazolidinone |
| (R)-4-BENZYL-3-CROTONYL-2-OXAZOLIDINONE |
| (S,E)-3-(but-2'-enoyl)-4-benzyloxazolidin-2-one |
| (S)-3-((E)-but-2-enoyl)-4-benzyloxazolidin-2-one |
| 4-(S)-benzyl-((E)-2'-butenoyl)-1,3-oxazolidin-2-one |
| (4S)-3-((E)-2-butenoyl)-4-(phenylmethyl)-2-oxazolidinone |
| (4S)-3-[(E)-BUT-2-ENOYL]-4-BENZYL-2-OXAZOLIDINONE |
| (4S)-N-[(2E)-but-2-enoyl]-4-phenylmethyl-1,3-oxazolidin-2-one |
| (N-CROTONYL)-(4S)-BENZYL-2-OXAZOLIDINONE |
| UIC-1005 |
| (S,E)-4-benzyl-3-(but-2-enoyl)oxazolidin-2-one |
| MFCD00278769 |
| (S)-3-((E)-but-2-enoyl)-4-benzyloxazolidinone |
| (N-Crotonyl)-(R)-4-benzyl-2-oxazolidinone |
| (S)-(+)-4-BENZYL-3-CROTONYL-2-OXAZOLIDINONE |