Leu-AMS
Based on 1 publication(s) in Google Scholar
Leu-AMS (compound 6), a leucine analogue, is a potent inhibitor of leucyl-tRNA synthetase (LRS) with an IC50 of 22.34 nM, which inhibits the catalytic activity of LRS but did not affect the leucine-induced mTORC1 activation. Leu-AMS shows cytotoxicity in cancer cells and normal cells, and inhibits the growth of bacteria.
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- Pureza : 99.57%
- No. CAS: 288591-93-5
- Fòrmula: C16H25N7O7S
- Peso molecular:459.48
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Almacenamiento:Powder -20°C, 3 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
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Leu-AMS (Standard)Reference Standard -
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Publications Citing Use of MedChemExpress (MCE) Leu-AMS
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Actividad biológica
Descripciòn
IC50 & Target
IC50: 22.34 nM (LRS)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
0.59 μM
Compound: 6
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Cytotoxicity in human A549 cells by sulforhodamine B colorimetric assay
Cytotoxicity in human A549 cells by sulforhodamine B colorimetric assay
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[PMID: 27933890] |
| HCT-116 | IC50 |
0.24 μM
Compound: 6
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Cytotoxicity in human HCT-116 cells by sulforhodamine B colorimetric assay
Cytotoxicity in human HCT-116 cells by sulforhodamine B colorimetric assay
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[PMID: 27933890] |
| K562 | IC50 |
0.4 μM
Compound: 6
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Cytotoxicity in human K562 cells by sulforhodamine B colorimetric assay
Cytotoxicity in human K562 cells by sulforhodamine B colorimetric assay
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[PMID: 27933890] |
| MDA-MB-231 | IC50 |
0.73 μM
Compound: 6
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Cytotoxicity in human MDA-MB-231 cells by sulforhodamine B colorimetric assay
Cytotoxicity in human MDA-MB-231 cells by sulforhodamine B colorimetric assay
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[PMID: 27933890] |
| MRC5 | IC50 |
5.9 μM
Compound: 6
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Cytotoxicity in human MRC5 cells by sulforhodamine B colorimetric assay
Cytotoxicity in human MRC5 cells by sulforhodamine B colorimetric assay
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[PMID: 27933890] |
| PBMC | IC50 |
1.1 μM
Compound: LeuSA
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Immunosuppressive activity against human PBMC assessed as inhibition of allogenic mixed lymphocyte reaction
Immunosuppressive activity against human PBMC assessed as inhibition of allogenic mixed lymphocyte reaction
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[PMID: 18438987] |
| SK-HEP1 | IC50 |
0.54 μM
Compound: 6
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Cytotoxicity in human SK-HEP1 cells by sulforhodamine B colorimetric assay
Cytotoxicity in human SK-HEP1 cells by sulforhodamine B colorimetric assay
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[PMID: 27933890] |
| SNU-638 | IC50 |
0.84 μM
Compound: 6
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Cytotoxicity in human SNU-638 cells by sulforhodamine B colorimetric assay
Cytotoxicity in human SNU-638 cells by sulforhodamine B colorimetric assay
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[PMID: 27933890] |
In Vitro
Leu-AMS is proved to be a potent inhibitor of Leucyl-tRNA Synthetase (LRS) with an IC50 value of 22.34 nM. Leu-AMS is highly cytotoxic in both cancer cells and normal cells. Leu-AMS does not affect S6 kinase (S6K) phosphorylation at all. Leu-AMS inhibits the catalytic activity of LRS but does not affect the leucine-induced mTORC1 activation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 288591-93-5
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Appearance Solid
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Peso molecular 459.48
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Fòrmula C16H25N7O7S
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Color White to off-white
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SMILES
O[C@@H]([C@H]([C@H](N1C=NC2=C1N=CN=C2N)O3)O)[C@H]3COS(=O)(NC([C@@H](N)CC(C)C)=O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (217.64 mM; Need ultrasonic; 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)
In Vivo:
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 (5.44 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 (5.44 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.
In Vivo Dissolution Calculator
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 (272 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 | 2.1764 mL | 10.8819 mL | 21.7637 mL | 54.4093 mL |
| 5 mM | 0.4353 mL | 2.1764 mL | 4.3527 mL | 10.8819 mL | |
| 10 mM | 0.2176 mL | 1.0882 mL | 2.1764 mL | 5.4409 mL | |
| 15 mM | 0.1451 mL | 0.7255 mL | 1.4509 mL | 3.6273 mL | |
| 20 mM | 0.1088 mL | 0.5441 mL | 1.0882 mL | 2.7205 mL | |
| 25 mM | 0.0871 mL | 0.4353 mL | 0.8705 mL | 2.1764 mL | |
| 30 mM | 0.0725 mL | 0.3627 mL | 0.7255 mL | 1.8136 mL | |
| 40 mM | 0.0544 mL | 0.2720 mL | 0.5441 mL | 1.3602 mL | |
| 50 mM | 0.0435 mL | 0.2176 mL | 0.4353 mL | 1.0882 mL | |
| 60 mM | 0.0363 mL | 0.1814 mL | 0.3627 mL | 0.9068 mL | |
| 80 mM | 0.0272 mL | 0.1360 mL | 0.2720 mL | 0.6801 mL | |
| 100 mM | 0.0218 mL | 0.1088 mL | 0.2176 mL | 0.5441 mL |
Leu-AMS Related Classifications
HY-108900 Related Classifications
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