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168682-53-9

中文名称 EZATIOSTAT游离的
英文名称 Glycine, L-g-glutaMyl-S-(phenylMethyl)-L-cysteinyl-2-phenyl-,1,3-diethyl ester, (2R)-
CAS 168682-53-9
分子式 C27H35N3O6S
分子量 529.65
MOL 文件 168682-53-9.mol
更新日期 2024/07/07 16:57:59
168682-53-9 结构式 168682-53-9 结构式

基本信息

中文别名
EZATIOSTAT游离
EZATIOSTAT游离的
GSTP1-1抑制剂(EZATIOSTAT)
英文别名
CS-1110
Ezatiostat
Terrapin 199
Ezatiostat, >96%
Ezatiostat, >=98%
TER199(free base)
Ezatiostat (TER199)
Ezatiostat TFA (free base)
TER 199
TLK-199
TELINTRA
(2R)-L-gamma-Glutamyl-S-(phenylmethyl)-L-cysteinyl-2-phenylglycine 1,3-diethyl ester
所属类别
生物化工:激动剂抑制剂

物理化学性质

熔点>94°C (dec.)
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
溶解度可溶于DMSO(少许)、甲醇(少许)
酸度系数(pKa)12?+-.0.46(Predicted)
形态固体
颜色白色至灰白色
EZATIOSTAT游离的价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2024/04/30HY-13634AEZATIOSTAT游离的
Ezatiostat
168682-53-95mg744元
2024/04/30S9698EZATIOSTAT游离的
Ezatiostat
168682-53-95mg795.31元
2024/04/30HY-13634AEZATIOSTAT游离的
Ezatiostat
168682-53-910mM * 1mLin DMSO867元

常见问题列表

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
TargetValue
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.

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