Ezatiostat

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Ezatiostat

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Cat No: 16248

Biochemicals - Small Molecule Inhibitors

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 tissu...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

(2R)-L-?-glutamyl-S-(phenylmethyl)-L-cysteinyl-2-phenyl-glycine, 1,3-diethyl ester

Correlated keywords:

286942-97-0 S-transferase GST signal transduction glutathione GSTP1-1 c-Jun N-terminal kinase JNK proliferation drug resistance inhibitor TLK117 cancer myelodysplastic syndrome TLK Telintra TER199 TER 199 TLK selective inhibit biochemical intracellular signaling tripeptide analog restore cell proliferation differentiation pathway myeloid precursor preclinical model clinical prevention myelosuppression myelodysplastic syndrome

Product Overview:
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}

Size	1 mg
Shipping	dry ice
CAS Number	168682-53-9
Molecular Formula	C₂₇H₃₅N₃O₆S
SMILES	O=C(OCC)[C@H](NC([C@@H](NC(CC[C@H](N)C(OCC)=O)=O)CSCC1=CC=CC=C1)=O)C2=CC=CC=C2
Molecular Weight	529,7
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2922.19
UNSPSC code	12352100

Technical File

MSDS

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Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

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ISO/IEC 17025:2005
ISO Guide 34:2009

Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.