Locostatin
Based on 3 publication(s) in Google Scholar
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 .
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- Pureza: 99.88%
- No. CAS: 90719-30-5
- Fòrmula: C14H15NO3
- Peso molecular:245.27
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) Locostatin
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Actividad biológica
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GRK2 |
Locostatin (200 µM; 37 °C; 6 h) disrupts the interaction of RKIP with Raf-1, and GRK2[1].
Locostatin (50 µM; 0-48 h) inhibits cell proliferation and migration in MDCK cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDCK cells
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Concentration:50 µM
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Incubation Time:0-48 h
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Result:Inhibited cell proliferation and sheet migration.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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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]
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Dosage:0.5 mg/kg
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Administration:I.p.; once a day for 7 days
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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.
Chemical Information
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No. CAS 90719-30-5
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Appearance Solid
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Peso molecular 245.27
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Fòrmula C14H15NO3
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Color White to light yellow
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SMILES
O=C1OC[C@H](CC2=CC=CC=C2)N1C(/C=C/C)=O
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Synonyms
UIC-1005
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
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Most Recent
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Nat Commun
RKIP regulates bone marrow macrophage differentiation to mediate osteoclastogenesis and H-type vessel formation. [Abstract]2025 Aug 15;16(1):7604. PMID: 40817102 -
J Ethnopharmacol
Didymin alleviates neuropathic pain by targeting RKIP-mediated NF-κB/NLRP3 crosstalk to inhibit pyroptosis and neuroinflammation. [Abstract]2026 Mar 25:359:121046. PMID: 41453551 -
J Vis Exp
Neuronal Ferroptosis Attenuation by RKIP Inhibition Following Spontaneous Intracerebral Hemorrhage via NRF2/HO-1 Pathway Activation. [Abstract]2025 Oct 31:(224). PMID: 41247931
Solvente y solubilidad
DMSO : 100 mg/mL (407.71 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (10.19 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (10.19 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.0771 mL | 20.3857 mL | 40.7714 mL | 101.9285 mL |
| 5 mM | 0.8154 mL | 4.0771 mL | 8.1543 mL | 20.3857 mL | |
| 10 mM | 0.4077 mL | 2.0386 mL | 4.0771 mL | 10.1928 mL | |
| 15 mM | 0.2718 mL | 1.3590 mL | 2.7181 mL | 6.7952 mL | |
| 20 mM | 0.2039 mL | 1.0193 mL | 2.0386 mL | 5.0964 mL | |
| 25 mM | 0.1631 mL | 0.8154 mL | 1.6309 mL | 4.0771 mL | |
| 30 mM | 0.1359 mL | 0.6795 mL | 1.3590 mL | 3.3976 mL | |
| 40 mM | 0.1019 mL | 0.5096 mL | 1.0193 mL | 2.5482 mL | |
| 50 mM | 0.0815 mL | 0.4077 mL | 0.8154 mL | 2.0386 mL | |
| 60 mM | 0.0680 mL | 0.3398 mL | 0.6795 mL | 1.6988 mL | |
| 80 mM | 0.0510 mL | 0.2548 mL | 0.5096 mL | 1.2741 mL | |
| 100 mM | 0.0408 mL | 0.2039 mL | 0.4077 mL | 1.0193 mL |
Locostatin Related Classifications
HY-W013411A Related Classifications
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