5-(2,2-Difluoro-benzo[1,3]dioxol-5-ylmethylene)-thiazolidine-2,4-dione Off-white solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A cell-permeable thiazolidinedione compound that acts as a potent and ATP-competitive inhibitor of PI 3-Kg (Ki = 180 nM; IC50 = 250 nM). Exhibits great selectivity over PI 3-Ka (IC50 = 4.5 µM), PI 3-Kb and d (IC50 > 20 µM), and shows little effect towards a large panel of receptors, unrelated enzymes, ion channels, and 38 commonly studied kinases. Shown to block MCP-1-mediated monocyte chemotaxis in vitro and exhibit better in vivo efficacy than LY294002 (Cat. No. 440202 and 440204) in blocking RANTES- or thioglycollate-induced peritoneal neutrophil recruitment by oral administration in a murine peritonitis model. Purity: ≥98% by HPLC. CAS 648449-76-7. Ref.: Bilancio, A., et al. 2006. Blood 107, 642. Camps, M., et al. 2005. Nat. Med. 11, 936. |
