1. Metabolic Enzyme/Protease
  2. Gutathione S-transferase
  3. TLK117

TLK117 (Synonyms: TER117)

目录号: HY-13634B 纯度: 98.32%

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。

MCE 的所有产品仅用作科学研究,我们不为任何个人用途提供产品和服务

TLK117 Chemical Structure

TLK117 Chemical Structure

CAS No. : 152684-53-2

1.  客户无需承担相应的运输费用。

2.  同一机构(单位)同一产品试用装仅限申领一次,同一机构(单位)一年内


3.  试用装只面向终端客户

Size Price Stock Quantity
10 mM * 1 mL in DMSO ¥1980 In-stock
5 mg ¥1800 In-stock
10 mg ¥2800 In-stock
50 mg   Get quote  
100 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Other Forms of TLK117:

Top Publications Citing Use of Products
  • 生物活性

  • 实验参考方法

  • 技术信息

  • 纯度 & 产品资料

  • 参考文献


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].

Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 150 mg/mL (316.76 mM; Need ultrasonic)

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.
In Vivo:
  • 1.

    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

  • 2.

    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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.28 mM); Clear solution

Kinase Assay

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


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.

Molecular Weight









Room temperature in continental US; may vary elsewhere

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2


Your information is safe with us. * Required Fields.



* 需求量:

* 客户姓名:


* Email:

* 电话:


* 公司或机构名称:


Bulk Inquiry

Inquiry Information



Cat. No.: HY-13634B