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152684-53-2

中文名稱 152684-53-2
英文名稱 TLK117
CAS 152684-53-2
分子式 C23H27N3O6S
分子量 473.54
MOL 文件 152684-53-2.mol
152684-53-2 結(jié)構(gòu)式 152684-53-2 結(jié)構(gòu)式

基本信息

中文別名
化合物 T8424
英文別名
TER117
TLK117
Glycine, L-γ-glutamyl-S-(phenylmethyl)-L-cysteinyl-2-phenyl-, (2R)-

物理化學(xué)性質(zhì)

沸點(diǎn)832.7±65.0 °C(Predicted)
密度1.346±0.06 g/cm3(Predicted)
酸度系數(shù)(pKa)2.21±0.10(Predicted)
形態(tài)Solid
顏色White to off-white
152684-53-2價(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱CAS號(hào)包裝價(jià)格
2024/11/08HY-13634B152684-53-2
TLK117
152684-53-25mg1800元
2024/11/08HY-13634B152684-53-2
TLK117
152684-53-210mM * 1mLin DMSO1980元
2024/11/08HY-13634B152684-53-2
TLK117
152684-53-210mg2800元

常見問(wèn)題列表

生物活性
TLK197是TLK199的活性代謝物,選擇性抑制谷胱甘肽S-轉(zhuǎn)移酶P1-1 (Glutathione S-transferase P1–1 (GSTP1-1)),結(jié)合 GSTP的 Ki 值為0.4 μM。 TLK117還競(jìng)爭(zhēng)性地抑制乙二醛酶I (glyoxalase I), Ki值為0.56 μM。
靶點(diǎn)

Ki: 0.4 μM, 0.56 μM (glyoxalase I)

體外研究

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.

體內(nèi)研究

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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