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Ezatiostat

CAS No. : 168682-53-9

MCE 站：Ezatiostat

产品活性：Ezatiostat (TER199 free base; TLK199) 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 通过抑制 GSTP1 导致 JNK 激活。Ezatiostat 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。

研究领域：Metabolic Enzyme/Protease  |  Apoptosis

作用靶点：Gutathione S-transferase  |  Apoptosis

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.
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.

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.

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