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Ezatiostat

Catalog No. T5097   CAS 168682-53-9
Synonyms: TER199(free base), TLK199

Ezatiostat (TER199(free base)) is a tripeptide analog of glutathione that can selectively inhibit GSTP1-1 catalytic activity.

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Ezatiostat Chemical Structure
Ezatiostat, CAS 168682-53-9
Pack Size Availability Price/USD Quantity
1 mg In stock $ 31.00
5 mg In stock $ 65.00
10 mg In stock $ 113.00
25 mg In stock $ 205.00
50 mg In stock $ 342.00
100 mg In stock $ 583.00
1 mL * 10 mM (in DMSO) In stock $ 77.00
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Purity: 97.95%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Ezatiostat (TER199(free base)) is a tripeptide analog of glutathione that can selectively inhibit GSTP1-1 catalytic activity.
In vivo Ezatiostat was administered to 19 patients with non-deletion(5q) myelodysplastic syndrome (MDS) at one of two doses (2000 mg or 2500 mg/day) in combination with 10 mg of lenalidomide on days 1-21 of a 28-day cycle. One of 4 evaluable patients (25%) in the 2500/10 mg dose group experienced an erythroid hematologic improvement (HI-E) response by 2006 MDS International Working Group (IWG) criteria. Four of 10 evaluable patients (40%) in the 2000 mg/10 mg dose group experienced a HI-E response [1]. Systemic inhibition of GSTP1 with Ezatiostat (0-30 mg/kg, i.p.) dose-dependently reduced the reinforcing effects of alcohol as measured by operant self-administration, in the absence of motor effects [2].
Synonyms TER199(free base), TLK199
Molecular Weight 529.65
Formula C27H35N3O6S
CAS No. 168682-53-9

Storage

keep away from moisture

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: Insoluble

DMSO: >50 mg/mL (94.4 mM)

Ethanol: 20 mg/mL (37.76)

TargetMolReferences and Literature

1. Raza A, et al. Phase 1 dose-ranging study of ezatiostat hydrochloride in combination with lenalidomide in patients with non-deletion (5q) low to intermediate-1 risk myelodysplastic syndrome (MDS). J Hematol Oncol. 2012 Apr 30;5:18. 2. Faccidomo S, et al. Mining the nucleus accumbens proteome for novel targets of alcohol self-administration in male C57BL/6J mice. Psychopharmacology (Berl). 2018 Jun;235(6):1681-1696.

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Keywords

Ezatiostat 168682-53-9 Apoptosis Metabolism oxidation-reduction Glutathione Peroxidase GST Inhibitor lymphocyte inhibit Glutathione transferases TLK 199 GSTs Gutathione S-transferase proliferation c-Jun JNK GSTP1 TLK-199 ERK1 MDS TER199(free base) TLK199 tripeptide inhibitor

 

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