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TLK117

Name: TLK117
Brand: TargetMol
SKU: T8424
Rating: 4.5 (1 reviews)

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Catalog No. T8424Cas No. 152684-53-2

Alias TLK-117, TER-117, TER117

TLK117 is an inhibitor of GSTs that reduces the severity of pulmonary fibrosis and can be used to study idiopathic pulmonary fibrosis.

TLK117

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Purity: 99.89%

Catalog No. T8424Alias TLK-117, TER-117, TER117Cas No. 152684-53-2

TLK117 is an inhibitor of GSTs that reduces the severity of pulmonary fibrosis and can be used to study idiopathic pulmonary fibrosis.

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
2 mg	$149	7-10 days	7-10 days

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.89%

Appearance:Solid

Color:White

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Product Introduction

Bioactivity

Description	TLK117 is an inhibitor of GSTs that reduces the severity of pulmonary fibrosis and can be used to study idiopathic pulmonary fibrosis.
Targets&IC50	glutathione S-transferase P:0.4 μM (Ki), aldolase I:0.56 μM (Ki)
In vitro	TLK117 is a potent and specific glutathione S-transferase P (GSTP) inhibitor with a higher binding affinity to the target than glutathione (GSH) and more than 50-fold selectivity for GSTP compared to GSTM and GSTA classes, with a constant of inhibition (Ki) of 0.4 μM.[1] TLK117 was developed as an inhibitor of the GST P1-1 isoenzyme to address the critical role of GST P1-1 in drug resistance in tumor cells. To enhance the cellular uptake efficiency of TLK117, the compound is delivered as a diethyl ester (TER 117 DEE, also known as TER 199).TLK117 competitively inhibits GST P1-1 and aldolase I. The inhibition constant (Ki) of TLK117 on aldolase I is 0.56 μM.[2]
In vivo	In cases where fibrosis has already formed, TLK117 attenuates pathological changes by inhibiting GSTP to attenuate tissue remodeling induced by bleomycin and adenoviral TGFβ (AdTGFβ), and decreasing the levels of α-SMA, cysteine asparaginase activity, FAS S-glutathionylation, and total protein S-glutathionylation. Within 4 hours after administration of 50 mg/kg TLK117, GSTP activity was substantially reduced and maintained at approximately 60% inhibition for at least 24 hours. [2]
Synonyms	TLK-117, TER-117, TER117

Chemical Properties

Molecular Weight	473.54
Formula	C₂₃H₂₇N₃O₆S
Cas No.	152684-53-2
Smiles	[C@H](NC([C@@H](NC(CC[C@@H](C(O)=O)N)=O)CSCC1=CC=CC=C1)=O)(C(O)=O)C2=CC=CC=C2
Relative Density.	1.346 g/cm3 (Predicted)
Sequence	H-gGlu-Cys(Bn)-D-Phg-OH
Sequence Short	XXX

Storage & Solubility Information

Storage

keep away from moisture,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 150 mg/mL (316.76 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (8.45 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1118 mL	10.5588 mL	21.1175 mL	105.5877 mL
5 mM	0.4224 mL	2.1118 mL	4.2235 mL	21.1175 mL
10 mM	0.2112 mL	1.0559 mL	2.1118 mL	10.5588 mL
20 mM	0.1056 mL	0.5279 mL	1.0559 mL	5.2794 mL
50 mM	0.0422 mL	0.2112 mL	0.4224 mL	2.1118 mL
100 mM	0.0211 mL	0.1056 mL	0.2112 mL	1.0559 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc