(N-CROTONYL)-(4S)-ISOPROPYL-2-OXAZOLIDINONE
- Product Name
- (N-CROTONYL)-(4S)-ISOPROPYL-2-OXAZOLIDINONE
- CAS No.
- 90719-30-5
- Chemical Name
- (N-CROTONYL)-(4S)-ISOPROPYL-2-OXAZOLIDINONE
- Synonyms
- UIC-1005;Locostatin - UIC 1005;Locostatin >=98% (HPLC);(R)-4-BENZYL-3-CROTONYL-2-OXAZOLIDINONE;(N-CROTONYL)-(4S)-BENZYL-2-OXAZOLIDINONE;(N-Crotonyl)-(R)-4-benzyl-2-oxazolidinone;4-but-2-enyl-3-propan-2-yl-2-oxazolidinone;(N-CROTONYL)-(4S)-ISOPROPYL-2-OXAZOLIDINONE;(S)-(+)-4-BENZYL-3-CROTONYL-2-OXAZOLIDINONE;(4S)-N-Crotonyl-4-benzyl-2-oxazolidinone,99%
- CBNumber
- CB4284497
- Molecular Formula
- C14H15NO3
- Formula Weight
- 245.27
- MOL File
- 90719-30-5.mol
(N-CROTONYL)-(4S)-ISOPROPYL-2-OXAZOLIDINONE Property
- Melting point:
- 84-88 °C(lit.)
- Boiling point:
- 351.0±25.0 °C(Predicted)
- Density
- 1.205±0.06 g/cm3(Predicted)
- storage temp.
- 2-8°C
- solubility
- DMSO: ≥30mg/mL
- pka
- -1?+-.0.40(Predicted)
- form
- powder
- color
- white to off-white
Safety
- Safety Statements
- 24/25
- WGK Germany
- 3
- HS Code
- 29349990
N-Bromosuccinimide Price
- Product number
- L5670
- Product name
- Locostatin
- Purity
- ≥98% (HPLC)
- Packaging
- 10mg
- Price
- $67.8
- Updated
- 2025/07/31
- Product number
- L5670
- Product name
- Locostatin
- Purity
- ≥98% (HPLC)
- Packaging
- 50mg
- Price
- $262
- Updated
- 2025/07/31
- Product number
- Axon2590
- Product name
- Locostatin-UIC1005
- Purity
- 100%
- Packaging
- 10mg
- Price
- $60.5
- Updated
- 2021/12/16
- Product number
- AA006AZ1
- Product name
- (S,E)-4-Benzyl-3-(but-2-enoyl)oxazolidin-2-one
- Purity
- 100%
- Packaging
- 50mg
- Price
- $332
- Updated
- 2021/12/16
- Product number
- A127375
- Product name
- (S,E)-4-Benzyl-3-(but-2-enoyl)oxazolidin-2-one
- Purity
- 98%
- Packaging
- 250mg
- Price
- $375
- Updated
- 2021/12/16
(N-CROTONYL)-(4S)-ISOPROPYL-2-OXAZOLIDINONE Chemical Properties,Usage,Production
Uses
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].
Biochem/physiol Actions
Locostatin is a cell permeable, potent inhibitor of Raf kinase inhibitor protein (RKIP)/Raf1 kinase interaction and an inhibitor of cell migration.
in vivo
Locostatin (0.5 mg/kg; i.p.; once a day for 7 days) aggravates thioacetamide (HY-Y0698)-induced acute liver failure in mice[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
[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. DOI:10.1615/forumimmundisther.v2.i1.60
[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. DOI:10.1002/1439-7633(20021104)3:11<1105::AID-CBIC1105>3.0.CO;2-S
[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. DOI:10.3892/etm.2018.6542
(N-CROTONYL)-(4S)-ISOPROPYL-2-OXAZOLIDINONE Preparation Products And Raw materials
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