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Ezatiostat

Catalog No. T5097 CAS 168682-53-9

Synonyms: TLK199, TER199(free base)

Ezatiostat is a tripeptide analog of glutathione that can selectively inhibit GSTP1-1 catalytic activity.

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Ezatiostat, CAS 168682-53-9

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description

Ezatiostat 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	TLK199, TER199(free base)
Molecular Weight	529.65
Formula	C27H35N3O6S
CAS No.	168682-53-9

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

H2O: Insoluble

DMSO: >50 mg/mL (94.4 mM)

Ethanol: 20 mg/mL (37.76)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References 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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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

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

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