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.
货号:ajcx18116
CAS:N/A
分子式:C12H6N3O2S•K
分子量：295.4
溶解度:DMF: 3 mg/ml,DMSO: 5 mg/ml,DMSO:PBS (pH 7.2) (1:10): 0.1 mg/ml
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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. PI3Kγ is a class 1B PI3K that is composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit, whereas PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits. AS-605240 is an orally active inhibitor of PI3-kinase γ that suppresses joint inflammation in mouse models of rheumatoid arthritis. It inhibits human recombinant PI3Kγ, α, β, and δ in an ATP-competitive manner with IC50 values of 8, 60, 270, and 300 nM, respectively. 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 .