A tripeptide analog of glutathione that can selectively inhibit GSTP1-1 catalytic activity (Ki = 400 nM) with minimal effect on the related GSTα and -µ families (Kis range from 20-75 µM); restores JNK-mediated cellular proliferation and differentiation signaling pathways

Ezatiostat – 1 mg

Brand:
Cayman
CAS:
168682-53-9
Storage:
-20
UN-No:
Non-Hazardous - /

Glutathione S-transferases (GSTs) are ubiquitous multifunctional enzymes that play key roles in cellular detoxification and signal transduction by conjugating target substrates to glutathione. GSTP1-1, the most prevalent GST isozyme in nonhepatic tissues, binds to and inhibits the stress-activated c-Jun N-terminal kinase (JNK), an important regulator of cell proliferation, differentiation, and apoptosis.{27831} GSTP1-1 is overexpressed in many cancers and has been linked to drug resistance.{27832} Ezatiostat is a tripeptide analog of glutathione that can selectively inhibit GSTP1-1 catalytic activity (Ki = 400 nM) with minimal effect on the related GSTα and -µ families (Kis range from 20-75 µM).{27831} After intracellular de-esterification, the active form of ezatiostat, TLK117, binds to and inhibits GSTP1-1, restoring JNK-mediated cellular proliferation and differentiation signaling pathways.{27832,27833,27834} Ezatiostat has been shown to stimulate the proliferation of myeloid precursors in preclinical models and is under clinical examination for its potential prevention of myelosuppression in myelodysplastic syndrome.{27833,27834}  

 

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Description

A tripeptide analog of glutathione that can selectively inhibit GSTP1-1 catalytic activity (Ki = 400 nM) with minimal effect on the related GSTα and -µ families (Kis range from 20-75 µM); restores JNK-mediated cellular proliferation and differentiation signaling pathways

Formal name: (2R)-L-γ-glutamyl-S-(phenylmethyl)-L-cysteinyl-2-phenyl-glycine-1,3-diethyl ester

Synonyms:  Terrapin 199|TLK199

Molecular weight: 529.7

CAS: 168682-53-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cancer|Cell Signaling|JNK Signaling

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