A pyridine-containing tetracycle that interferes with JAK kinase activity interacting within the ATP-binding cleft (IC50s = 15

JAK Inhibitor I – 5 mg

Brand:
Cayman
CAS:
457081-03-7
Storage:
-20
UN-No:
Non-Hazardous - /

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}  

 

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Description

A pyridine-containing tetracycle that interferes with JAK kinase activity interacting within the ATP-binding cleft (IC50s = 15, 1, and 5 nM for JAK1, 2, and 3, respectively); block IL-2 and IL-4-dependent proliferation of mouse T-cell lymphoma cells (IC50s = 50-100 nM)

Formal name: 2-(1,1-dimethylethyl)-9-fluoro-1,6-dihydro-7H-benz[h]imidazo[4,5-f]isoquinolin-7-one

Synonyms:  CMP 6|Janus-Associated Kinase Inhibitor I|Pyridone 6

Molecular weight: 309.3

CAS: 457081-03-7

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|JAK Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cell Biology|Cell Signaling|JAK Signaling||Research Area|Epigenetics, Transcription, & Translation|Transcription Factors||Research Area|Immunology & Inflammation|Adaptive Immunity

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