Ezatiostat hydrochloride(Synonyms: TER199; TLK199 hydrochloride)

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Ezatiostat hydrochloride (Synonyms: TER199; TLK199 hydrochloride)

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。

Ezatiostat hydrochloride(Synonyms: TER199; TLK199 hydrochloride)

Ezatiostat hydrochloride Chemical Structure

CAS No. : 286942-97-0

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Ezatiostat hydrochloride 的其他形式现货产品:

Ezatiostat

生物活性

Ezatiostat hydrochloride (TER199; TLK199 hydrochloride) is a tripeptide analog of glutathione and is a selective and orally active glutathione S-transferase P1-1 (GSTP1) inhibitor. Ezatiostat hydrochloride leads to JNK activation by inhibiting GSTP1. 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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

参考文献
  • [1]. Galili N, et al. Prediction of response to therapy with ezatiostat in lower risk myelodysplastic syndrome. J Hematol Oncol. 2012 May 6;5:20

    [2]. Ruscoe JE, et al. Pharmacologic or genetic manipulation of glutathione S-transferase P1-1 (GSTpi) influences cell proliferation pathways. J Pharmacol Exp Ther. 2001 Jul;298(1):339-45.

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