A potent and selective inhibitor of PI3Kδ (Ki = 79 pM); has >1

GSK2292767 – 10 mg

Brand:
Cayman
CAS:
1254036-66-2
Storage:
-20
UN-No:
De Minimis - 3077 / 9

GSK2292767 is a potent and selective inhibitor of phosphatidylinositol 3-kinase δ (PI3Kδ; Ki = 79 pM).{32991} It has >1,000-fold selectivity for PI3Kδ over isoforms PI3Kα, PI3Kβ, and PI3Kγ with Ki values of 501, 630, and 501 nM, respectively. GSK2292767 is >100-fold selective for PI3Kδ over a panel of 250 kinases. It inhibits IFN-γ and IL-2 production (IC50s = 1.9 and 3.16 nM, respectively) in a human lung parenchyma assay. GSK2292767 also protects against eosinophil recruitment (ED50 = 35 μg/kg) in the brown Norway rat acute ovalbumin model of Th2-driven lung inflammation.  

 

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Description

A potent and selective inhibitor of PI3Kδ (Ki = 79 pM); has >1,000-fold selectivity for PI3Kδ over isoforms PI3Kα, PI3Kβ, and PI3Kγ (Kis = 501, 630, and 501 nM, respectively); >100-fold selective for PI3Kδ over a panel of 250 kinases; inhibits IFNγ and IL-2 production (IC50s = 1.9 and 3.16 nM, respectively) in a human lung parenchyma assay; protects against eosinophil recruitment (ED50 = 35 μg/kg) in the brown Norway rat acute ovalbumin model of Th2-driven lung inflammation,

Formal name: rel-N-[5-[4-[5-[[(2R,6S)-2,6-dimethyl-4-morpholinyl]methyl]-2-oxazolyl]-1H-indazol-6-yl]-2-methoxy-3-pyridinyl]-methanesulfonamide

Synonyms: 

Molecular weight: 512.6

CAS: 1254036-66-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|PI3K||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Immunology & Inflammation|Adaptive Immunity||Research Area|Immunology & Inflammation|Allergy||Research Area|Immunology & Inflammation|Innate Immunity

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