| Identification | Back Directory | [Name]
TLK117 | [CAS]
152684-53-2 | [Synonyms]
TLK117
TER117
Glycine, L-γ-glutamyl-S-(phenylmethyl)-L-cysteinyl-2-phenyl-, (2R)- | [Molecular Formula]
C23H27N3O6S | [MDL Number]
MFCD20272480 | [MOL File]
152684-53-2.mol | [Molecular Weight]
473.54 |
| Chemical Properties | Back Directory | [Boiling point ]
832.7±65.0 °C(Predicted) | [density ]
1.346±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
2.21±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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. | [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]. | [References]
[1] The human glutathione transferase P1-1 specific inhibitor TER 117 designed for overcomingcytostatic-drug resistance is also a strong inhibitor of glyoxalase I. Mol Pharmacol. 2000 Mar;57(3):619-24. DOI:10.1124/mol.57.3.619
[2] McMillan DH, et al. Attenuation of lung fibrosis in mice with a clinically relevant inhibitor of glutathione-S-transferase π. JCI Insight. 2016 Jun 2;1(8). pii: e85717. DOI:10.1172/jci.insight.85717 |
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