KIRA6

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KIRA6

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Cat No: 19151

Biochemicals - Kinase Inhibitors

The IRE1 pathway is a component of the unfolded protein response that senses unfolded proteins via an ER luminal domain that becomes oligomerized during stress. It is associated with promoting cell survival through the activity of the IRE1α RNase, whos...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

N-[4-[8-amino-3-(1,1-dimethylethyl)imidazo[1,5-a]pyrazin-1-yl]-1-naphthalenyl]-N'-[3-(trifluoromethyl)phenyl]-urea

Correlated keywords:

IRE1a IRE1alpha IRE1? endoplasmic recticulum unfolded portein response kinase inhibiting RNase attentuator IRE-1a IRE-1alpha IRE-1? IRE1-a IRE1-alpha IRE1-? KIRA-6

Product Overview:
The IRE1 pathway is a component of the unfolded protein response that senses unfolded proteins via an ER luminal domain that becomes oligomerized during stress. It is associated with promoting cell survival through the activity of the IRE1α RNase, whose activity upregulates proteins that enhance ER protein folding and quality control. However, under high ER stress, the IRE1α RNase becomes hyperactive and is less discriminant in its substrate specificity, endonucleolytically cleaving many additional mRNAs that localize to the ER membrane, leading to cell proliferation blocks, inflammation, and apoptosis. KIRA6 is an ATP-competitive IRE1α kinase inhibiting RNase attenuator (KIRA) that allosterically inhibits IRE1α RNase kinase activity (IC50 = 0.6 µM) and prevents oligomerization.{30935} It has been shown to inhibit IRE1α in vivo and to promote cell survival under ER stress.{30935} At 20 µg/ml, KIRA6 is reported to preserve photoreceptor functional viability in rat models of ER stress-induced retinal degeneration.{30935} At 5 mg/kg, it has also been shown to preserve pancreatic β cells, increase insulin, and reduce hyperglycemia in Akita diabetic mice.{30395}

Size	1 mg
Shipping	dry ice
CAS Number	1589527-65-0
Molecular Formula	C₂₈H₂₅F₃N₆O
SMILES	NC1=NC=CN2C1=C(C3=C(C=CC=C4)C4=C(NC(NC5=CC(C(F)(F)F)=CC=C5)=O)C=C3)N=C2C(C)(C)C
Molecular Weight	518,5
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2922.19
UNSPSC code	12352100

Technical File

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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.