152684-53-2
基本信息
TLK117
Glycine, L-γ-glutamyl-S-(phenylmethyl)-L-cysteinyl-2-phenyl-, (2R)-
物理化学性质
| 沸点 | 832.7±65.0 °C(Predicted) |
| 密度 | 1.346±0.06 g/cm3(Predicted) |
| 酸度系数(pKa) | 2.21±0.10(Predicted) |
| 形态 | Solid |
| 颜色 | White to off-white |
152684-53-2价格(试剂级)
| 报价日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
| 2024/04/30 | HY-13634B | 152684-53-2 TLK117 | 152684-53-2 | 5mg | 1800元 |
| 2024/04/30 | HY-13634B | 152684-53-2 TLK117 | 152684-53-2 | 10mg | 2800元 |
| 2024/01/25 | HY-13634B | 152684-53-2 TLK117 | 152684-53-2 | 10mM * 1mLin DMSO | 1980元 |
常见问题列表
Ki: 0.4 μM, 0.56 μM (glyoxalase I)
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.
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.