2. Metabolic Enzyme/Protease Apoptosis
  3. Glutathione S-transferase Apoptosis
  4. Ezatiostat hydrochloride

Ezatiostat hydrochloride  (Synonyms: TER199; TLK199 hydrochloride)

Cat. No.: HY-13634
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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.

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CAS No. : 286942-97-0

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Ezatiostat hydrochloride Related Antibodies

Top Publications Citing Use of Products

    Ezatiostat hydrochloride purchased from MedChemExpress. Usage Cited in: Redox Biol. 2024 Aug 20:76:103323.  [Abstract]

    Huh7 cells were treated with 0, 5, 10, and 20 μM Ezatiostat (TLK199) for 72 h, followed by FACS analysis to assess ROS production.

    Ezatiostat hydrochloride purchased from MedChemExpress. Usage Cited in: Redox Biol. 2024 Aug 20:76:103323.  [Abstract]

    Protein expression levels of Lamin B1, p21, γ-H2AX and H2AX were detected by western blot upon treatment of Ezatiostat (TLK199, 0-20 μM, 72 h), with β-actin as a loading control.

    Ezatiostat hydrochloride purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2023 Mar;10(7):e2205262.  [Abstract]

    In vitro effects of treatment with the GSTP1 inhibitor Ezatiostat (12.5 μM) on crizotinib sensitivity in LUAD-OG1 evaluated by Cell titer-Glo cell viability assay.

    Ezatiostat hydrochloride purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2023 Mar;10(7):e2205262.  [Abstract]

    Schematic diagram of the treatment regimen with 1% Tween 80/saline (Group 1), crizotinib (10 mg/kg; Group2), ezatiostat (25 mg/kg; Group 3), or the combination of ezatiostat with crizotinib (Group 4) in NOD-SCID mice. n = 4 mice per group. Representative image of LUAD-OG1 xenografts from the four groups at the endpoint are shown.

    Ezatiostat hydrochloride purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2023 Mar;10(7):e2205262.  [Abstract]

    Ex vivo effects of GSTP1 inhibitor Ezatiostat (12.5 and 25 μM) treatment on crizotinib sensitivity in crizotinib-resistant LUAD-OG1 evaluated by Cell titer-Glo cell viability assay.

    Ezatiostat hydrochloride purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2023 Mar;10(7):e2205262.  [Abstract]

    Schematic diagram of oral gavage of the treatment regimen with 1% Tween 80/saline (Group 1), crizotinib (25 mg kg−1; Group2), ezatiostat (25 mg/kg; Group 3), or the combination of ezatiostat with crizotinib (Group 4) in SCID mice.

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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].

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

    Ezatiostat hydrochloride Related Antibodies
    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].

    MedChemExpress (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.
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.
    Purity & Documentation
    References
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    Ezatiostat hydrochloride Related Classifications

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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Ezatiostat286942-97-0TER199TLK199TER 199TER-199TLK 199TLK-199Glutathione S-transferaseApoptosisGlutathione transferasesGSTsMDSGSTP1JNKtripeptideproliferationlymphocyteERK1c-JunInhibitorinhibitorinhibit

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