AS-<wbr/>605240 (potassium salt)

AS-605240 (potassium salt)

CAT N°: 9000980
Price:

From 48.00 40.80

Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of PI at the three position to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3.{8039,12235,13740} PI3K? is a class 1B PI3K that is composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit, whereas PI3K?, ?, and ? are class 1A enzymes composed of p110 and p85 subunits.{14518} AS-605240 is an orally active inhibitor of PI3-kinase ? that suppresses joint inflammation in mouse models of rheumatoid arthritis.{13338} It inhibits human recombinant PI3K?, ?, ?, and ? in an ATP-competitive manner with IC50 values of 8, 60, 270, and 300 nM, respectively.{13338} AS-605240 inhibits C5a-mediated phosphorylation of protein kinase B in RAW 264 cells with an IC50 value of 90 nM. In vivo, AS-605240 reduced RANTES-induced peritoneal neutrophil recruitment in a mouse model of leukocyte chemotaxis with an ED50 value of 9.1 mg/kg. AS-605240 (potassium salt) has improved solubility compared to AS-605240 (Item No. 10007707).

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