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Ezatiostat hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Ezatiostat hydrochloride图片
CAS NO:286942-97-0
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
TER199
TLK199 hydrochloride
产品介绍
Ezatiostat hydrochloride (TER199; TLK199 hydrochloride) 是一种谷胱甘肽的三肽类似物,也是一种选择性的口服活性的谷胱甘肽 S-转移酶 P1-1 (GSTP1) 抑制剂。Ezatiostat hydrochloride 通过抑制GSTP1导致 JNK 激活。Ezatiostat hydrochloride 刺激淋巴细胞生成和骨髓祖细胞增殖,可用于骨髓增生异常综合症 (MDS) 的研究。
生物活性

Ezatiostat hydrochloride (TER199; TLK199 hydrochloride) is a tripeptide analog of glutathione and is a selective and orally activeglutathione S-transferase P1-1 (GSTP1)inhibitor. Ezatiostat hydrochloride leads toJNKactivation by inhibitingGSTP1. Ezatiostat hydrochloride stimulates both lymphocyte production and bone marrow progenitor proliferation. Ezatiostat hydrochloride has the potential for myelodysplastic syndrome (MDS) treatment[1][2].

IC50& Target

Glutathione S-transferase P1-1 (GSTP1)[1]

体外研究
(In Vitro)

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[1].
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[2].

体内研究
(In Vivo)

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[2].

Clinical Trial
分子量

566.11

Formula

C27H36ClN3O6S

CAS 号

286942-97-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.