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- 技术资料
- 保存条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
- 英文名:
TER199; TLK199 hydrochloride
- 库存:
货期:询盘
- 供应商:
MedChemExpress LLC
- 规格:
询盘
MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务。
Ezatiostat hydrochloride
CAS No. : 286942-97-0
MCE 国际站:Ezatiostat hydrochloride
产品活性: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。
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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