中文同义词:
EZATIOSTAT游离的;GSTP1-1抑制剂(EZATIOSTAT);EZATIOSTAT游离
英文名称:
Glycine, L-g-glutaMyl-S-(phenylMethyl)-L-cysteinyl-2-phenyl-,1,3-diethyl ester, (2R)-
英文同义词:
Ezatiostat, >96%;CS-1110;TER 199; TLK-199; TELINTRA;(S)-ETHYL 2-AMINO-5-((R)-3-(BENZYLTHIO)-1-((R)-2-ETHOXY-2-OXO-1-PHENYLETHYLAMINO)-1-OXOPROPAN-2-YLAMINO)-5-OXOPENTANOATE;(2R)-L-gamma-Glutamyl-S-(phenylmethyl)-L-cysteinyl-2-phenylglycine 1,3-diethyl ester;Glycine, L-g-glutaMyl-S-(phenylMethyl)-L-cysteinyl-2-phenyl-,1,3-diethyl ester, (2R)-;Ezatiostat;Terrapin 199
沸点
749.7±60.0 °C(Predicted)
密度
1.216±0.06 g/cm3(Predicted)
储存条件
Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
酸度系数(pKa)
12?+-.0.46(Predicted)
生物活性
Ezatiostat (TER199, TLK199, Telintra) 是一种谷胱甘肽的三肽类似物，是 Glutathione S-transferase P1-1 (GSTP1-1) 的拟肽抑制剂。Ezatiostat 可激活 c-Jun NH2 terminal kinase (JNK1) 和 ERK1/ERK2 并诱导凋亡。
靶点
Target Value
GSTP1-1
()
JNK1
()
ERK1/ERK2
()
体外研究
Ezatiostat causes dissociation of the enzyme from the jun-N-terminal kinase/c-Jun (JNK/JUN) complex, leading to JNK activation by phosphorylation. The therapeutic action of ezatiostat appears to include both proliferation of normal myeloid progenitors as well as apoptosis of the malignant clone.
Selection of a resistant clone of an HL60 tumor cell line through chronic exposure to Ezatiostat (TLK199) results in cells with elevated activities of c-Jun NH2 terminal kinase (JNK1) and ERK1/ERK2, and allowes the cells to proliferate under stress conditions that induced high levels of apoptosis in the wild type cells.
体内研究
Administration of Ezatiostat (TLK199), stimulates both lymphocyte production and bone marrow progenitor (colony-forming unit-granulocyte macrophage) proliferation, but only in glutathione S-transferase P1-1 (GSTP1 +/+ ) and not in GSTP1 -/- animals.
