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JAK Inhibitor I

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    JAK Inhibitor I
  • JAK Inhibitor I
Cat No: 15146
Biochemicals - Kinase Inhibitors
Cayman

Janus-associated kinases (JAKs) are cytoplasmic tyrosine kinases that are required for activating the signaling of certain cytokines and growth factor receptors.{19346,20362} JAK1 mostly activates IL-6, whereas JAK1 and JAK3 trigger IL-2 and IL-4 and J...

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Territorial Availability: Available through Bertin Technologies only in France
Synonyms:
  • 2-(1,1-dimethylethyl)-9-fluoro-1,6-dihydro-7H-benz[h]imidazo[4,5-f]isoquinolin-7-one
Correlated keywords:
  • JAKs janus-associated kinases CMP 6 Pyridone 6 tyrosine cytokine JAK1 JAK2 JAK3 inhibitors inhibits inhibitions I one 1 pyridine tetracycle ATP binds binding binder cleft JAK-1 JAK-2 JAK-3 1 2 3 two three interleukins ILs CMPs 6 siz CMP-6 CMP6 pyridone-6 pyridone6 pan-JAK pan
Product Overview:
Janus-associated kinases (JAKs) are cytoplasmic tyrosine kinases that are required for activating the signaling of certain cytokines and growth factor receptors.{19346,20362} JAK1 mostly activates IL-6, whereas JAK1 and JAK3 trigger IL-2 and IL-4 and JAK1 and JAK2 stimulates IFN-γ. JAK Inhibitor I is a pyridine-containing tetracycle that interferes with JAK kinase activity by interacting within the ATP-binding cleft. It inhibits JAK1, 2, and 3 with IC50 values of 15, 1, and 5 nM, respectively, while displaying significantly weaker affinities (IC50s = 130 nM - > 10 μM) for other protein tyrosine kinases.{24837} It was shown to block IL-2 and IL-4-dependent proliferation of mouse T-cell lymphoma cells with IC50 values of 50-100 nM.{24837} In a mouse model of atopic dermatitis, JAK Inhibitor I, supplied at 2 mg encapsulated in a PLGA nanoparticle, was shown to suppress IFN-γ/STAT1, IL-2/STAT5, and IL-4/STAT6 signaling pathways.{24838}
Size 500 µg
Shipping dry ice
CAS Number 457081-03-7
Molecular Formula C18H16FN3O
SMILES O=C1NC=CC2=C1C(C=C(F)C=C3)=C3C4=C2NC(C(C)(C)C)=N4
Molecular Weight 309,3
Formulation A crystalline solid
Purity ≥98%
Custom Code 2922.19
UNSPSC code 12352100

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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.

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