Inhibition of N-terminal His6-tagged recombinant full length human p110beta/untagged recombinant full length human p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate measured after 80 mins by transcreener fluorescence polarization assay
Inhibition of recombinant human full-length His-tagged PI3K p110gamma expressed in baculovirus expression system using PIP2 as substrate measured after 80 mins by transcreener fluorescence polarization assay
Inhibition of N-terminal His6-tagged recombinant full length human p110delta/untagged recombinant full length human p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate measured after 80 mins by transcreener fluorescence polarization assay
Inhibition of PI3Kdelta in human whole blood assessed as reduction in anti-IgM-stimulated CD69 expression on B-cells preincubated for 60 mins followed by anti-IgM stimulation and measured after overnight incubation by flow cytometry
Inhibition of PI3Kdelta in rat whole blood assessed as reduction in anti-IgD-stimulated CD86 expression on B-cells preincubated for 60 mins followed by anti-IgD stimulation and measured after overnight incubation by flow cytometry
Inhibition of PI3Kgamma in human whole blood assessed as reduction in anti-IgE-stimulated CD63 expression in basophils preincubated for 30 mins followed by anti-IgE stimulation
Inhibition of PI3Kdelta in human whole blood assessed as reduction in fMLP-stimulated CD63 expression in basophils preincubated for 30 mins followed by fMLP stimulation
Ex vivo inhibition of anti-IgD-induced B cell activation in Wistar rat assessed as CD86 expression at 1 mg/kg, po pretreated for 2 hrs followed by anti-IgD stimulation and measured after overnight incubation by flow cytometry relative to control
Antiarthritic activity in po dosed type2 collagen-induced Wistar rat arthritis model assessed as reduction in hind paw volume administered twice daily for 7 days and measured daily during compound dosing by plethysmometry
Glutathione reactivity in human liver microsomes assessed as GSH-adduct formation at 1 uM measured after 30 mins in presence of NADPH generating system
Inhibition of KC/GRO-induced neutrophil migration in Wistar rat air pouch model at 10 mg/kg, po pretreated for 0.5 hrs followed by KC/GRO-stimulation and measured after 4 hrs by flow cytometry relative to control