Ezatiostat hydrochloride

Research use only, not for human use.

Ezatiostat hydrochloride is an effective inhibitor of glutathione S-transferase. Ezatiostat hydrochloride is a novel glutathione analog and the potential treatment of cytopenias.

Ezatiostat hydrochloride is an effective inhibitor of glutathione S-transferase. Ezatiostat hydrochloride is a novel glutathione analog and the potential treatment of cytopenias. In addition, Ezatiostat hydrochloride has been revealed to selectively bind to and thus inhibit GSTP1-1.(In Vitro):Because GST P1-1 can bind to and inhibit JNK, Ezatiostat hydrochloride has also been exhibited to inhibit GST P1-1, activate JNK, and promote the growth and maturation of hematopoietic progenitors in preclinical models. Moreover, Ezatiostat hydrochloride has been reported to stimulate the proliferation of myeloid precursors. Ezatiostat hydrochloride has been elucidated to induce growth inhibition and cellular apoptosis in human leukemia cells (CC50: 6-17μM). Apart from these, Ezatiostat hydrochloride has shown the stimulation of multilineage differentiation in mature monocytes, granulocytes, and erythrocytes .(In Vivo):Administration of Ezatiostat stimulates both lymphocyte production and bone marrow progenitor proliferation only in glutathione S-transferase P1-1 (GSTP1+/+) and not in GSTP1-/- animals.

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.

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.

TER199 | TLK199 HCl

Others

Other Targets

——

——

——

286942-97-0

566.11

C27H36ClN3O6S

>98% (HPLC)

——

Cl.CCOC(=O)C(N)CCC(=O)NC(CSCc1ccccc1)C(=O)NC(C(=O)OCC)c1ccccc1

——

(-20℃)

With Ice Pack

≥ 2 years