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TLK117

CAS No. : 152684-53-2

MCE 站：TLK117

产品活性：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 P11 (GSTP1-1))，结合 GSTP的 K_i 值为0.4 μM。 TLK117还竞争性地抑制乙二醛酶I (glyoxalase I)， K_i值为0.56 μM。

研究领域：Metabolic Enzyme/Protease

作用靶点：Gutathione S-transferase

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 (K_i=0.4 μM). 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.

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.

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