GSK2656157

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GSK2656157

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Cat No: 17372

Biochemicals - Small Molecule Inhibitors

GSK2656157 is an inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK; IC50 = 0.9 nM).{32772,32773} It is selective for PERK over a panel of additional kinases.{32772} GSK2656157 blocks both stress-induced PERK autophosphorylati...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

1-[5-(4-amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-4-fluoro-2,3-dihydro-1H-indol-1-yl]-2-(6-methyl-2-pyridinyl)-ethanone

Correlated keywords:

PKR elF2a ATF-4 anti-tumor J7741 J774-1 protein kinase R like endoplasmic reticulum kinase GSK 2656157

Product Overview:
GSK2656157 is an inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK; IC50 = 0.9 nM).{32772,32773} It is selective for PERK over a panel of additional kinases.{32772} GSK2656157 blocks both stress-induced PERK autophosphorylation and eIF2α substrate phosphorylation and decreases levels of ATF4 and CHOP in multiple cell lines.{32772} It is orally bioavailable, suppressing PERK autophosphorylation in mouse pancreas and inhibiting the growth of multiple human tumor xenografts in mice.{32772,32773} GSK2656157 inhibits caspase 1 activation in macrophage-like J774.1 cells, preventing LPS-induced IL-1β production, through its effects on the PERK/eIF2α pathway.{32771}

Size	5 mg
Shipping	dry ice
CAS Number	1337532-29-2
Molecular Formula	C₂₃H₂₁FN₆O
SMILES	NC1=NC=NC2=C1C(C3=CC=C4C(CCN4C(CC5=CC=CC(C)=N5)=O)=C3F)=CN2C
Molecular Weight	416,5
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2932.99
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.

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.