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Ezatiostat

CAS No. : 168682-53-9

MCE 国际站：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.

相关产品：Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Apoptosis Compound Library | Metabolism/Protease Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Peptidomimetic Library | Drug Repurposing Compound Library | Antioxidants Compound Library | Oxygen Sensing Compound Library | Anti-COVID-19 Compound Library | Endoplasmic Reticulum Stress Compound Library | Orally Active Compound Library | MG-132 | LY294002 | Doxorubicin hydrochloride | Bafilomycin A1 | Paclitaxel | Y-27632 dihydrochloride | Acetylcysteine | Angiotensin II human | SP600125 | 5-Fluorouracil | Staurosporine | Bortezomib | Tamoxifen | 2-Deoxy-D-glucose | Gemcitabine | Verteporfin | Decitabine | Actinomycin D | Temozolomide | BAY 11⁻⁷082 | Etoposide | Mitomycin C | CCCP | DAPT | Rotenone | Etomoxir | Stattic | Docetaxel | Fulvestrant

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