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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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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 代谢凋亡氧化还原 Apoptosis 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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