GOT1 inhibitor-1
Based on 2 publication(s) in Google Scholar
GOT1 inhibitor-1 (compound 2c), a tryptamine-based derivative, acts as a novel, potent and non-covalent inhibitor of glutamate oxaloacetate transaminase 1 (GOT1) with an IC50 of 8.2 uM. GOT1 plays an important role in energy metabolism and Reactive Oxygen Species (ROS) balance. GOT1 inhibitor-1 can be used for the research of pancreatic ductal adenocarcinoma (PDAC).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.75%
- CAS. Nr.: 732973-87-4
- Formel: C19H19ClN4O
- Molecular Weight:354.83
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Speicherung:Powder -20°C, 3 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) GOT1 inhibitor-1
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Biologische Aktivität
Beschreibung
In Vitro
PDAC tumors are dependent upon a metabolic pathway involving aspartate aminotransferase 1 (glutamate-oxaloacetate transaminase 1 (GOT1)), for the maintenance of redox homeostasis and sustained proliferation. Small molecule inhibitors targeting this metabolic pathway may provide a novel way for cancer research. In the MDH coupled GOT1 enzymatic assay, GOT1 inhibitor-1 shows an inhibitory effect on GOT1 activity with an IC50 value of 8.2 uM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 732973-87-4
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Appearance Solid
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Molecular Weight 354.83
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Formel C19H19ClN4O
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Color Off-white to light yellow
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SMILES
O=C(N1CCN(C2=CC=CC3=C2C=CN3)CC1)NC4=CC=C(Cl)C=C4
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Cancer Res
GOT2 Silencing Promotes Reprogramming of Glutamine Metabolism and Sensitizes Hepatocellular Carcinoma to Glutaminase Inhibitors. [Abstract]2022 Sep 16;82(18):3223-3235. PMID: 35895805 -
EMBO Rep
Glycogenesis and glyconeogenesis from glutamine, lactate and glycerol support human macrophage functions. [Abstract]2024 Dec;25(12):5383-5407. PMID: 39424955
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 125 mg/mL (352.28 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: ≥ 2.08 mg/mL (5.86 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: 2.08 mg/mL (5.86 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Reinheit & Dokumentation
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Data Sheet (272 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Justin Anglin, et al. Discovery and optimization of aspartate aminotransferase 1 inhibitors to target redox balance in pancreatic ductal adenocarcinoma. Bioorg Med Chem Lett. 2018 Sep 1;28(16):2675-2678 [Content Brief]
[2]. Sun W, et al. Aspulvinone O, a natural inhibitor of GOT1 suppresses pancreatic ductal adenocarcinoma cells growth by interfering glutamine metabolism. Cell Commun Signal. 2019;17(1):111. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.8183 mL | 14.0913 mL | 28.1825 mL | 70.4563 mL |
| 5 mM | 0.5637 mL | 2.8183 mL | 5.6365 mL | 14.0913 mL | |
| 10 mM | 0.2818 mL | 1.4091 mL | 2.8183 mL | 7.0456 mL | |
| 15 mM | 0.1879 mL | 0.9394 mL | 1.8788 mL | 4.6971 mL | |
| 20 mM | 0.1409 mL | 0.7046 mL | 1.4091 mL | 3.5228 mL | |
| 25 mM | 0.1127 mL | 0.5637 mL | 1.1273 mL | 2.8183 mL | |
| 30 mM | 0.0939 mL | 0.4697 mL | 0.9394 mL | 2.3485 mL | |
| 40 mM | 0.0705 mL | 0.3523 mL | 0.7046 mL | 1.7614 mL | |
| 50 mM | 0.0564 mL | 0.2818 mL | 0.5637 mL | 1.4091 mL | |
| 60 mM | 0.0470 mL | 0.2349 mL | 0.4697 mL | 1.1743 mL | |
| 80 mM | 0.0352 mL | 0.1761 mL | 0.3523 mL | 0.8807 mL | |
| 100 mM | 0.0282 mL | 0.1409 mL | 0.2818 mL | 0.7046 mL |
GOT1 inhibitor-1 Related Classifications
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