TLK117, the active metabolite of TLK199, selective inhibits Glutathione S-transferase P1–1 (GSTP1-1) with a K i of 0.4 μM for GSTP. TLK117 also competitively inhibits glyoxalase I with a K i of 0.56 μM. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:Ki: 0.4 μM, 0.56 μM (glyoxalase I)
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TLK117
CAS number：152684-53-2 molecular formula：C23H27N3O6S
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Specs
| Chinese alias | - | ||
| English alias | VWW | Glycine, N-[N-L-gamma-glutamyl-S-(phenylmethyl)-L-cysteinyl]-D-2-phenyl- | L-Gamma-Glutamyl-S-Benzyl-N-[(S)-Carboxy(Phenyl)methyl]-L-Cysteinamide | TER117 | 10gs | MS-28779 | Glycine, L-gamma-glutamyl-S-(phenylmethyl)-L-cysteinyl-2-phenyl-, (2R)- | | ||
| CAS number | 152684-53-2 | molecular formula | C23H27N3O6S |
| molecular weight | 473.54 g/mol | Exact mass | ≥98% |
| PSA | 184.000 Ų | logp | -0.900 |
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