5-(6-キノキサリニルメチレン)-2,4-チアゾリジンジオン

プロパティ

安全情報

説明

PI 3-Kγ Inhibitor is a cell-permeable thiazolidinedione compound that acts as a potent, selective, and ATP-competitive inhibitor of PI 3-kinase γ (PI 3-Kγ) (K_i = 7.8 nM; IC₅₀ = 8 nM, 60 nM, 270 nM, 300 nM for p110-γ, α, β and δ-isoforms, respectively). PI 3-Kγ Inhibitor does not affect the activity of a wide panel of kinases, receptors, enzymes, and ion channels even at concentrations as high as 1 μM. It selectively blocks MCP-1-, but not CSF-1-, dependent Akt phosphorylation and chemotaxis in primary Pik3cg+/+ murine monocytes and in a human monocytic cell line THP-1 (IC₅₀ = 181 nM). PI 3-Kγ Inhibitor has also been shown to exhibit efficacy in reducing neutrophil chemotaxis in murine peritonitis and arthritis models.