| Size | Price | Stock | Qty |
|---|---|---|---|
| 250mg |
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| Other Sizes |
| Targets |
Methionine aminopeptidase 2 (MetAP2). MetAP2-IN-1 is a selective inhibitor of MetAP2, an enzyme involved in the removal of N-terminal methionine residues from nascent proteins. MetAP2 plays a critical role in protein processing and is involved in angiogenesis. By inhibiting MetAP2, the compound may affect protein function and cellular processes including angiogenesis. The compound's mechanism of action involves binding to the active site of MetAP2 and preventing its enzymatic activity.
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| ln Vitro |
MetAP2-IN-1 is a MetAP2 inhibitor that can be used for research in conditions mediated by angiogenesis. As a selective inhibitor of MetAP2, it blocks the removal of N-terminal methionine residues from nascent proteins. The compound's inhibitory activity can be measured using enzyme assays with purified MetAP2 or in cell-based systems. Its specific IC₅₀ value and selectivity profile would depend on the assay conditions. Further studies are needed to fully characterize its in vitro activity profile.
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| ln Vivo |
MetAP2-IN-1 can be used for research in conditions mediated by angiogenesis. As a MetAP2 inhibitor, it may have potential applications in diseases where angiogenesis plays a role, such as cancer and inflammatory disorders. The compound may be evaluated in animal models of angiogenesis-dependent diseases. Further in vivo studies are needed to characterize its pharmacokinetic and pharmacodynamic properties, as well as its efficacy and safety profile.
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| Enzyme Assay |
Non-cell-based assays for MetAP2-IN-1 include enzyme inhibition assays using purified MetAP2. The enzyme is incubated with a peptide substrate and various concentrations of MetAP2-IN-1, and enzymatic activity is measured by detecting the release of methionine or using coupled enzyme assays. The IC₅₀ value is calculated from the dose-response curve. Selectivity can be assessed by testing the compound against other aminopeptidases. Standard analytical methods including HPLC, NMR, and mass spectrometry are used for compound characterization.
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| Cell Assay |
Cell-based assays for MetAP2-IN-1 use various cell lines to assess its effects on MetAP2 activity and angiogenesis. Cells are treated with the compound at various concentrations, and MetAP2 activity is assessed by measuring the processing of MetAP2 substrates. Angiogenesis-related endpoints such as endothelial cell proliferation, migration, and tube formation can be assessed in endothelial cell models. Cell viability is assessed using MTT or similar assays. The compound's effects on signaling pathways can be studied using Western blot.
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| Animal Protocol |
In vivo studies of MetAP2-IN-1 are limited. Based on its mechanism of action, potential animal models include: tumor xenograft models for evaluating anti-angiogenic effects; and models of angiogenesis-dependent diseases. Standard protocols for these models involve administration of the compound (oral, intraperitoneal, or intravenous) followed by measurement of relevant endpoints including tumor volume, angiogenesis markers, and histopathological analysis.
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| ADME/Pharmacokinetics |
MetAP2-IN-1 has a molecular formula of C₈H₆BrN₃ and a molecular weight of 224.06 g/mol. The CAS number is 5301-98-4. The compound is also known as 4-(4-bromophenyl)-1H-1,2,3-triazole. It should be stored as a powder at -20°C for up to 3 years or at 4°C for up to 2 years. In solvent, it can be stored at -80°C for 6 months or at -20°C for 1 month. It is intended for research use only.
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| Toxicity/Toxicokinetics |
Specific toxicity data for MetAP2-IN-1 are limited. As an enzyme inhibitor, it may have effects on normal protein processing at high doses. The compound is intended for research use only. Standard laboratory safety practices should be followed when handling this compound, including the use of personal protective equipment.
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| References | |
| Additional Infomation |
MetAP2-IN-1 (CAS 5301-98-4) is a selective inhibitor of methionine aminopeptidase 2 (MetAP2), an enzyme involved in the removal of N-terminal methionine residues from nascent proteins. MetAP2 plays a critical role in protein processing and is involved in angiogenesis. By inhibiting MetAP2, the compound may affect protein function and cellular processes including angiogenesis. MetAP2-IN-1 can be used for research in conditions mediated by angiogenesis and is suitable for research applications aimed at understanding the role of MetAP2 in various pathological conditions. It is for research use only.
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| Molecular Formula |
C8H6BRN3
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|---|---|
| Molecular Weight |
224.06
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| Exact Mass |
222.975
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| CAS # |
5301-98-4
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| PubChem CID |
6419341
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
2.234
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
12
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| Complexity |
145
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC(=CC=C1C2=NNN=C2)Br
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| InChi Key |
RYKZCPFWGNDOQV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C8H6BrN3/c9-7-3-1-6(2-4-7)8-5-10-12-11-8/h1-5H,(H,10,11,12)
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| Chemical Name |
4-(4-bromophenyl)-2H-triazole
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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 |
| 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) |
DMSO: 50 mg/mL (223.15 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (11.16 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (11.16 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. 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 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (11.16 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 | 4.4631 mL | 22.3155 mL | 44.6309 mL | |
| 5 mM | 0.8926 mL | 4.4631 mL | 8.9262 mL | |
| 10 mM | 0.4463 mL | 2.2315 mL | 4.4631 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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