1. Metabolic Enzyme/Protease
  2. Gutathione S-transferase

TLK117 (Synonyms: TER117)

目录号: HY-13634B
产品使用指南

TLK197是TLK199的活性代谢物,选择性抑制谷胱甘肽S-转移酶P1-1 (Glutathione S-transferase P1–1 (GSTP1-1)),结合 GSTP的 Ki 值为0.4 μM。 TLK117还竞争性地抑制乙二醛酶I (glyoxalase I), Ki值为0.56 μM。

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TLK117 Chemical Structure

TLK117 Chemical Structure

CAS No. : 152684-53-2

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Description

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.

IC50 & Target

Ki: 0.4 μM[1], 0.56 μM (glyoxalase I)[2]

In Vitro

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].

In Vivo

Oropharyngeal administration of the GSTP inhibitor, TLK117, at a time when fibrosis is already apparent, attenuated bleomycin- and AdTGFβ-induced remodeling, α-SMA, caspase activation, FAS S-glutathionylation, and total protein S-glutathionylation. Four hours after administration of 50 mg/kg TLK117, GSTP activity is strongly decreased and remains decreased by about 60% for at least 24 hours[2].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1118 mL 10.5588 mL 21.1175 mL
5 mM 0.4224 mL 2.1118 mL 4.2235 mL
10 mM 0.2112 mL 1.0559 mL 2.1118 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

473.54

Formula

C₂₃H₂₇N₃O₆S

CAS No.

152684-53-2

SMILES

O=C(O)[C@@H](C1=CC=CC=C1)NC([C@@H](NC(CC[C@H](N)C(O)=O)=O)CSCC2=CC=CC=C2)=O

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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产品名称:
TLK117
目录号:
HY-13634B
需求量:

TLK117

Cat. No.: HY-13634B