1. Metabolic Enzyme/Protease
    Apoptosis
  2. Gutathione S-transferase
    Apoptosis
  3. Ezatiostat hydrochloride

Ezatiostat hydrochloride (Synonyms: TER199; TLK199 hydrochloride)

Cat. No.: HY-13634
Handling Instructions

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.

For research use only. We do not sell to patients.

Custom Peptide Synthesis

Ezatiostat hydrochloride Chemical Structure

Ezatiostat hydrochloride Chemical Structure

CAS No. : 286942-97-0

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Description

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]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

566.11

Formula

C27H36ClN3O6S

CAS No.
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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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Product Name:
Ezatiostat hydrochloride
Cat. No.:
HY-13634
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