5-Quinoxalin-6-ylmethylene-thiazolidine-2,4-dione Pink solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A cell-permeable thiazolidinedione compound that acts as a potent, selective, and ATP-competitive inhibitor of phosphatidylinositol 3-kinase g (PI 3-Kg) (Ki = 7.8 nM; IC50 = 8 nM, 60 nM, 270 nM, 300 nM for p110-g, a, b and d-isoforms, respectively). Does not affect the activity of a wide panel of kinases, receptors, enzymes, and ion channels even at concentrations as high as 1 µM. 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). Also shown to exhibit in vivo efficacy in reducing neutrophil chemotaxis in murine peritonitis and arthritis models. Purity: ≥90% by HPLC. CAS 648450-29-7. Ref.: Barber, D.F., et al. 2005. Nat. Med. 11, 933. Camps, M., et al. 2005. Nat. Med. 11, 936. |
