TLK117
Based on 1 publication(s) in Google Scholar
TLK117, the active metabolite of TLK199, selective inhibits Glutathione S-transferase P1–1 (GSTP1-1) with a Ki of 0.4 μM for GSTP. TLK117 also competitively inhibits glyoxalase I with a Ki of 0.56 μM.
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- Reinheit: 99.86%
- CAS. Nr.: 152684-53-2
- Formel: C23H27N3O6S
- Molecular Weight:473.54
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Speicherung:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biologische Aktivität
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) TLK117
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Biologische Aktivität
TLK117 is the most specific GSTP inhibitor to date, with a binding affinity greater than GSH itself and a selectivity for GSTP over 50-fold greater than the GSTM and GSTA classes (Ki=0.4 μM)[1]. TER 117 is developed as a GST P1-1 isoenzyme inhibitor to circumvent the indicated contribution of GST P1-1 to drug resistance of tumor cells. To facilitate the cellular uptake of TER 117, it is delivered as a diethyl ester (TER 117 DEE, also called TER 199). TER 117 is found to be a competitive inhibitor of both GST P1-1 and glyoxalase I[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 152684-53-2
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Appearance Solid
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Molecular Weight 473.54
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Formel C23H27N3O6S
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Color White to off-white
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Synonyms
TER117
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Environ Sci Technol
High-Efficiency Degradation of PET Plastics by Glutathione S-Transferase under Mild Conditions. [Abstract]2024 Jul 16. PMID: 39012182
Lösungsmittel & Löslichkeit
DMSO : 150 mg/mL (316.76 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 (5.28 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 (5.28 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
Protokoll
The potency of TER 117 in the inhibition of GST P1-1/Ile-105 and GST P1-1/Val-105 is determined by means of GSH competition experiments using 1 μM TER 117 and three different fixed concentrations of GSH: 0.2, 0.6, and 2.0 mM. The concentration of the second substrate, 1-chloro-2,4-dinitrobenzene (CDNB) ranged between 0.15 and 1.8 mM. In addition, the inhibitor is tested at different concentrations, 0 to 8 μM, at a CDNB concentration of 1 mM and the above GSH concentrations. Initial velocities are determined spectrophotometrically at 30°C. The conjugation reaction between GSH and CDNB is monitored at 340 nm in 1 mL of 0.1 M sodium phosphate, pH 7.0[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
TLK117 is administered oropharyngeally at a dose of 50 mg/kg in a 0.375 M Tris-HCl solution, pH =7.4, with 0.02% DMSO. This Tris-HCl/DMSO solution is used as a vehicle control. Treatments are performed once every 3 days from day 14 to day 26 in both >bleomycin and AdTGFβ models
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. The human glutathione transferase P1-1 specific inhibitor TER 117 designed for overcomingcytostatic-drug resistance is also a strong inhibitor of glyoxalase I. Mol Pharmacol. 2000 Mar;57(3):619-24. [Content Brief]
[2]. McMillan DH, et al. Attenuation of lung fibrosis in mice with a clinically relevant inhibitor of glutathione-S-transferase π. JCI Insight. 2016 Jun 2;1(8). pii: e85717. [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, 6 months; -20°C, 1 month (sealed storage, away from moisture). 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 | 2.1118 mL | 10.5588 mL | 21.1175 mL | 52.7938 mL |
| 5 mM | 0.4224 mL | 2.1118 mL | 4.2235 mL | 10.5588 mL | |
| 10 mM | 0.2112 mL | 1.0559 mL | 2.1118 mL | 5.2794 mL | |
| 15 mM | 0.1408 mL | 0.7039 mL | 1.4078 mL | 3.5196 mL | |
| 20 mM | 0.1056 mL | 0.5279 mL | 1.0559 mL | 2.6397 mL | |
| 25 mM | 0.0845 mL | 0.4224 mL | 0.8447 mL | 2.1118 mL | |
| 30 mM | 0.0704 mL | 0.3520 mL | 0.7039 mL | 1.7598 mL | |
| 40 mM | 0.0528 mL | 0.2640 mL | 0.5279 mL | 1.3198 mL | |
| 50 mM | 0.0422 mL | 0.2112 mL | 0.4224 mL | 1.0559 mL | |
| 60 mM | 0.0352 mL | 0.1760 mL | 0.3520 mL | 0.8799 mL | |
| 80 mM | 0.0264 mL | 0.1320 mL | 0.2640 mL | 0.6599 mL | |
| 100 mM | 0.0211 mL | 0.1056 mL | 0.2112 mL | 0.5279 mL |
TLK117 Related Classifications
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