Locostatin
Modify Date: 2024-01-09 20:00:41
Locostatin structure
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Common Name | Locostatin | ||
|---|---|---|---|---|
| CAS Number | 90719-30-5 | Molecular Weight | 197.23100 | |
| Density | 1.205 g/cm3 | Boiling Point | 351ºC at 760 mmHg | |
| Molecular Formula | C10H15NO3 | Melting Point | 84-88ºC(lit.) | |
| MSDS | USA | Flash Point | 166.1ºC | |
Use of LocostatinLocostatin (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]. |
| Name | (n-crotonyl)-(4s)-isopropyl-2-oxazolidinone |
|---|---|
| Synonym | More Synonyms |
| 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]. |
|---|---|
| Related Catalog | |
| Target |
RKIP[3] |
| 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. |
| 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. |
| References |
| Density | 1.205 g/cm3 |
|---|---|
| Boiling Point | 351ºC at 760 mmHg |
| Melting Point | 84-88ºC(lit.) |
| Molecular Formula | C10H15NO3 |
| Molecular Weight | 197.23100 |
| Flash Point | 166.1ºC |
| Exact Mass | 197.10500 |
| PSA | 46.61000 |
| LogP | 1.29870 |
| Appearance of Characters | white to off-white |
| Storage condition | 2-8°C |
| Water Solubility | DMSO: ≥30mg/mL |
|
~90%
Locostatin CAS#:90719-30-5 |
| Literature: Rueck, Karola; Kunz, Horst Synthesis, 1993 , # 10 p. 1018 - 1028 |
|
~87%
Locostatin CAS#:90719-30-5 |
| Literature: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS Patent: WO2003/106437 A1, 2003 ; Location in patent: Page 51-52 ; |
|
~98%
Locostatin CAS#:90719-30-5 |
| Literature: Sakaguchi, Hiroshi; Tokuyama, Hidetoshi; Fukuyama, Tohru Organic Letters, 2007 , vol. 9, # 9 p. 1635 - 1638 |
CAS#:145589-03-3![(3S,4S)-3,4-BIS[[(1,1-DIMETHYLETHYL)DIMETHYLSILYL]OXY]PYRROLIDINE structure](https://www.chemsrc.com/caspic/042/133729-84-7.png)
CAS#:133729-84-7| (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 |