AS1938909 is a SHIP2 inhibitor that works by increasing Akt phosphorylation, glucose consumption, and glucose uptake in L6 myotubes, specifically upregulating the GLUT1 gene.
LAS191859 is a CRTH2 DP2 antagonist with IC50 values of 7.6, 9.58, 14 and 15.5nM for recombinant guinea pig, human, rat and mouse CRTH2 DP2 receptors, respectively. LAS191859 has a residence time half-life of 21h at CRTh2 that translates into a long-lasti
AS1940477 is p38 MAPK inhibitor. AS1940477 inhibited the enzymatic activity of recombinant p38α and β isoforms but showed no effect against other 100 protein kinases including p38γ and δ isoforms. In human peripheral blood mononuclear cells, AS1940477 inhibited lipopolysaccharide (LPS)- or phytohemagglutinin A (PHA)-induced production of proinflammatory cytokines, including TNFα, IL-1β, and IL-6 at low concentrations (LPS TNFα, IC(50)=0.45n M; PHA TNFα, IC(50)=0.40 nM). In addition, equivalent concentrations of AS1940477 that inhibited cytokine production also inhibited TNFα- and IL-1 β-induced production of IL-6, PGE(2), and MMP-3 in human synovial stromal cells. AS1940477 was also found to potently inhibit TNF production in whole blood (IC(50)=12 nM) and effectively inhibited TNFα production induced by systemically administered LPS in rats at less than 0.1mg kg (ED(50)=0.053 mg kg) with an anti-inflammatory effect lasting for 20h after oral administration. Overall, this stu......