Art. -Nr.: HY-108900

Leu-AMS

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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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Reinheit: 99.57%
CAS. Nr.: 288591-93-5
Formel: C₁₆H₂₅N₇O₇S
Molecular Weight:459.48

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

Leu-AMS Chemical Structure

CAS. Nr.: 288591-93-5

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 22.34 nM (LRS)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.59 μM Compound: 6	Cytotoxicity in human A549 cells by sulforhodamine B colorimetric assay Cytotoxicity in human A549 cells by sulforhodamine B colorimetric assay	[PMID: 27933890]
HCT-116	IC₅₀	0.24 μM Compound: 6	Cytotoxicity in human HCT-116 cells by sulforhodamine B colorimetric assay Cytotoxicity in human HCT-116 cells by sulforhodamine B colorimetric assay	[PMID: 27933890]
K562	IC₅₀	0.4 μM Compound: 6	Cytotoxicity in human K562 cells by sulforhodamine B colorimetric assay Cytotoxicity in human K562 cells by sulforhodamine B colorimetric assay	[PMID: 27933890]
MDA-MB-231	IC₅₀	0.73 μM Compound: 6	Cytotoxicity in human MDA-MB-231 cells by sulforhodamine B colorimetric assay Cytotoxicity in human MDA-MB-231 cells by sulforhodamine B colorimetric assay	[PMID: 27933890]
MRC5	IC₅₀	5.9 μM Compound: 6	Cytotoxicity in human MRC5 cells by sulforhodamine B colorimetric assay Cytotoxicity in human MRC5 cells by sulforhodamine B colorimetric assay	[PMID: 27933890]
PBMC	IC₅₀	1.1 μM Compound: LeuSA	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	[PMID: 18438987]
SK-HEP1	IC₅₀	0.54 μM Compound: 6	Cytotoxicity in human SK-HEP1 cells by sulforhodamine B colorimetric assay Cytotoxicity in human SK-HEP1 cells by sulforhodamine B colorimetric assay	[PMID: 27933890]
SNU-638	IC₅₀	0.84 μM Compound: 6	Cytotoxicity in human SNU-638 cells by sulforhodamine B colorimetric assay Cytotoxicity in human SNU-638 cells by sulforhodamine B colorimetric assay	[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

CAS. Nr. 288591-93-5
Appearance Solid
Molecular Weight 459.48
Formel C₁₆H₂₅N₇O₇S
Color White to off-white
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1764 mL

10.8819 mL

21.7637 mL

5 mM

0.4353 mL

2.1764 mL

4.3527 mL

10 mM

0.2176 mL

1.0882 mL

2.1764 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.44 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Yoon S, et al. Discovery of Leucyladenylate Sulfamates as Novel Leucyl-tRNA Synthetase (LRS)-TargetedMammalian Target of Rapamycin Complex 1 (mTORC1) Inhibitors. J Med Chem. 2016 Nov 23;59(22):10322-10328. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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Leu-AMS

MCE Bioactive Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Leu-AMS Related Classifications

HY-108900 Related Classifications