Name: Ezatiostat hydrochloride
Price: 276.00 USD

- Overview
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    Background
    
    Ezatiostat hydrochloride(TLK199) is an effective inhibitor of glutathione S-transferase （GST）[1].
    Ezatiostat hydrochloride (TLK199) 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 GST P1-1. 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 (HL-60) with a CC50 value of 6-17μM. Apart from these, Ezatiostat hydrochloride has shown the stimulation of multilineage differentiation in mature monocytes, granulocytes and erythrocytes [1,2].
    
    [1] Tew KD1, Dutta S, Schultz M.Inhibitors of glutathione S-transferases as therapeutic agents. Adv Drug Deliv Rev. 1997 Jul 7;26(2-3):91-104.
    [2] Raza A1, Galili N, Callander N, Ochoa L, Piro L, Emanuel P, Williams S, Burris H 3rd, Faderl S, Estrov Z, Curtin P, Larson RA, Keck JG, Jones M, Meng L, Brown GL. Phase 1-2a multicenter dose-escalation study of ezatiostat hydrochloride liposomes for injection (Telintra, TLK199), a novel glutathione analog prodrug in patients with myelodysplastic syndrome. J Hematol Oncol. 2009 May 13;2:20.
- Properties
  - Alternative Name
    
    ethyl (2S)-2-amino-5-[[(2R)-3-benzylsulfanyl-1-[[(1R)-2-ethoxy-2-oxo-1-phenylethyl]amino]-1-oxopropan-2-yl]amino]-5-oxopentanoate;hydrochloride
    
    CAS Number
    
    286942-97-0
    
    Molecular Formula
    
    C27H36ClN3O6S
    
    Molecular Weight
    
    566.11
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥28.3 mg/mL in DMSO; ≥3.32 mg/mL in H2O with ultrasonic; ≥3.4 mg/mL in EtOH with ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Zhao S, Wang B, et al. "Contributions of enzymes and gut microbes to biotransformation of perfluorooctane sulfonamide in earthworms (Eisenia fetida)." Chemosphere. 2019 Aug 19;238:124619. PMID:31450114
    1. Liberti, Eileen. "An In-vitro Investigation of Glutathione Transferases in Idiopathic Pulmonary Fibrosis." George Mason University.2018.
    2. Faccidomo S, Swaim KS, et al. "Mining the nucleus accumbens proteome for novel targets of alcohol self-administration in male C57BL/6J mice."Psychopharmacology (Berl).2018 Mar 3. PMID:29502276
    3. Liu X, et al. "Human glutathione S-transferase P1-1 functions as an estrogen receptor α signaling modulator." Biochem Biophys Res Commun. 2014 Sep 16. pii: S0006-291X(14)01625-8. PMID:25218501

Ezatiostat hydrochloride

Ezatiostat hydrochloride

Background

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