PKR Inhibitor

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PKR Inhibitor

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Cat No: 15323

Biochemicals - Kinase Inhibitors

The activity of double-stranded RNA-activated protein kinase (PKR) is altered by viral infection as well as by various neuropathologies.{25319,25322} A primary phosphorylation target of PKR is eukaryotic initiation factor 2 subunit α (eIF2α), blocking ...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

6,8-dihydro-8-(1H-imidazol-5-ylmethylene)-7H-pyrrolo[2,3-g]benzothiazol-7-one

Correlated keywords:

1159885-47-8 nootropics apoptosis neurosciences inhibitors inhibits inhibitions proteins kinases PKRs oxindole imidazole derivatives ATP autophosphorylation neuroblastoma cells FADD fas associated Fas-associated protein death domains caspases long-term long term memory storage contextual auditory fear memories GWs 506033X GW506033X GW-506033X PXRi double-stranded double stranded RNA-activated RNAs activated viral infections neuropathologies primary phosphorylation targets eukaryotic initiation factors 2 two subunit .alpha. alpha ? eIF2? eIF2alpha eIF2.alpha. eIF2-alpha blocking blocks translation apoptosis ATP-binding site binding sites humans damages tunicamycin-mediated tunicamycin endoplasmic reticulum stress prevents protects intraperitoneal administrations rats brains mice

Product Overview:
The activity of double-stranded RNA-activated protein kinase (PKR) is altered by viral infection as well as by various neuropathologies.{25319,25322} A primary phosphorylation target of PKR is eukaryotic initiation factor 2 subunit α (eIF2α), blocking translation and driving apoptosis.{25323} PKR Inhibitor is an oxindole/imidazole derivative that binds the ATP-binding site of PKR and blocks autophosphorylation with an IC50 value of 186-210 nM.{25323} PKR Inhibitor protects human neuroblastoma cells against cell damage triggered by tunicamycin-mediated endoplasmic reticulum stress.{25321} It also prevents phosphorylation of Fas-associated protein with a death domain (FADD) in neuroblastoma cells, preventing FADD-dependent activation of caspases and apoptosis.{25319} Intraperitoneal administration of PKR inhibitor in rats reduces phosphorylation of PKR and eIF2α in the brain.{25320} Similar administration in mice enhances long-term memory storage, including contextual and auditory long-term fear memories.{25322}

Size	1 mg
Shipping	dry ice
CAS Number	608512-97-6
Molecular Formula	C₁₃H₈N₄OS
SMILES	O=C1NC2=CC=C3C(SC=N3)=C2/C1=C/C4=CNC=N4
Molecular Weight	268,3
Formulation	A crystalline solid
Purity	≥95%
Custom Code	2922.19
UNSPSC code	12352100

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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.

Accreditations
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.