| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Ki: 1.32 µM (GlnRS)[1]
Glutaminyl-tRNA synthetase (GlnRS). Gln-AMS is a type Ia aminoacyl-tRNA synthetase (AARS) inhibitor that specifically targets glutaminyl-tRNA synthetase (GlnRS). GlnRS catalyzes the ATP-dependent ligation of glutamine to its cognate tRNA, a critical step in protein biosynthesis. By binding to the active site, Gln-AMS competes with the natural substrate glutamine, thereby preventing the formation of glutaminyl-tRNA and halting protein synthesis. This inhibition is reversible and competitive with respect to glutamine. The TFA salt form is used to enhance compound stability and solubility for research applications. |
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| ln Vitro |
Gln-AMS(TFA) is an inhibitor of type Ia aminoacyl-tRNA synthetase (AARS)[2].
In vitro, Gln-AMS (TFA) inhibits glutaminyl-tRNA synthetase (GlnRS) with a Ki value of 1.32 microM. This Ki indicates the binding affinity of the inhibitor for the enzyme and reflects its potency as a competitive inhibitor. The compound is classified as a type Ia aminoacyl-tRNA synthetase (AARS) inhibitor based on its structural and inhibitory properties. In bacterial and eukaryotic cell-free translation systems, Gln-AMS inhibits protein synthesis in a concentration-dependent manner. However, the effective intracellular concentration required for cellular activity may be higher due to compound permeability and efflux mechanisms. |
| ln Vivo |
No specific in vivo data are available for Gln-AMS TFA. As an aminoacyl-tRNA synthetase (AARS) inhibitor, this class of compounds is generally used for mechanistic studies in cell-free systems or for exploring potential antibacterial applications, because AARS inhibitors have been validated as targets for novel antibiotics (e.g., mupirocin). Gln-AMS TFA is a standard tool compound for studying glutaminyl-tRNA synthetase biology and evaluating the functional consequences of GlnRS inhibition in various cellular contexts. It is not intended for in vivo therapeutic use.
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| Enzyme Assay |
For a typical non-cellular enzyme inhibition assay, recombinant glutaminyl-tRNA synthetase (GlnRS) is prepared in assay buffer (50 mM HEPES pH 7.5, 150 mM KCl, 10 mM MgCl2, 1 mM DTT). The reaction mixture contains 0.1-10 uM Gln-AMS TFA, 1-500 uM L-glutamine, 1-100 uM ATP, and 0.1-10 uM tRNAGln. The reaction is initiated by adding GlnRS (0.1-1 nM) and incubated at 37degC for 10-30 minutes. Aliquots are quenched with trichloroacetic acid, and product formation is measured by either P32-ATP incorporation or colorimetric detection of pyrophosphate. Ki values are determined by measuring initial rates at varying substrate and inhibitor concentrations, fitting to a competitive inhibition model.
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| Cell Assay |
A typical cellular assay for Gln-AMS TFA can be conducted using E. coli or mammalian cell lines. Cells are grown to mid-log phase and then incubated with varying concentrations of Gln-AMS TFA (0.1-100 uM) for 2-24 hours. For protein synthesis inhibition studies, cells are pulsed with 35S-methionine for 30 minutes at 37degC, then lysed, and trichloroacetic acid-precipitable radioactivity is quantified by liquid scintillation counting. Alternatively, cell viability is assessed using MTT or resazurin reduction assays after 24-48 hours of compound exposure. IC50 values for cell growth inhibition can be derived from dose-response curves. Gln-AMS TFA can also be used to study GlnRS-dependent cellular responses and metabolic consequences of GlnRS inhibition.
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| Animal Protocol |
For in vivo studies, a typical protocol is not available for this specific compound. For a generic type Ia AARS inhibitor, laboratory animals (e.g., mice) may be administered the compound intravenously (5-20 mg/kg) or intraperitoneally. Blood and tissue samples are collected at various time points (0.5, 1, 2, 4, 8, 12, 24 hours post-dose). Tissues (liver, kidney, spleen) are homogenized, and compound concentrations are quantified by LC-MS/MS. Efficacy studies may involve infection models (e.g., bacterial peritonitis) to assess antibacterial activity, but Gln-AMS TFA is not typically used in such models.
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| ADME/Pharmacokinetics |
As a small-molecule inhibitor, the pharmacokinetic properties of Gln-AMS TFA are not well characterized. Based on its chemical structure (containing an adenosine moiety and a peptide-like link), the compound is expected to have polar characteristics with high aqueous solubility but low membrane permeability (negative LogP). It is likely to be primarily renally excreted and may undergo hydrolysis or metabolic cleavage. The TFA counterion is present in stoichiometric amounts (1:1 or 2:1 ratio with the active molecule) and does not significantly affect pharmacokinetics. Detailed PK parameters (half-life, clearance, volume of distribution) have not been reported for this compound.
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| Toxicity/Toxicokinetics |
Aminoacyl-tRNA synthetase (AARS) inhibitors such as Gln-AMS are generally considered to have low inherent toxicity because they target bacterial AARSs with higher selectivity than mammalian enzymes. However, Gln-AMS TFA inhibits mammalian GlnRS with a Ki of 1.32 microM, suggesting potential for cellular toxicity in eukaryotic cells at high concentrations. In vitro cytotoxicity assays may show reduced viability at concentrations >50-100 uM. No specific genotoxicity, organ toxicity, or carcinogenicity data are available. For research use, standard precautions (gloves, lab coat) should be used. Gln-AMS TFA is not intended for human use.
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| References | |
| Additional Infomation |
Gln-AMS (glutaminyl-adenosine monophosphoramide sulfamate) is a bisubstrate analog inhibitor that mimics the reaction intermediate of the glutaminyl-tRNA synthetase (GlnRS)-catalyzed aminoacylation reaction. The compound contains a sulfamoyl linkage that is non-hydrolyzable, providing stable inhibition. It has been used extensively as a mechanistic probe for aminoacyl-tRNA synthetase function. The TFA salt form (trifluoroacetate) is prepared to improve solid-state stability and water solubility compared to other salt forms (e.g., hydrochloride). Gln-AMS is a well-established tool compound in enzymology and chemical biology, but it is not an approved drug. The compound is for research use only.
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| Molecular Formula |
C17H23F3N8O10S
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| Molecular Weight |
588.47
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| Related CAS # |
Gln-AMS;209543-57-7
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| Appearance |
White to off-white solid powder
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O :~130 mg/mL (~220.91 mM)
DMSO :~50 mg/mL (~84.97 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 4.25 mg/mL (7.22 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 42.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.25 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.25 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6993 mL | 8.4966 mL | 16.9932 mL | |
| 5 mM | 0.3399 mL | 1.6993 mL | 3.3986 mL | |
| 10 mM | 0.1699 mL | 0.8497 mL | 1.6993 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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