A cell-permeable thiazolidinedione compound that acts as a potent and ATP-competitive inhibitor of PI 3-Kγ (Ki = 180 nM; IC50 = 250 nM). Exhibits great selectivity over PI 3-Kα (IC50 = 4.5 µM), PI 3-Kβ and δ (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.
5 mg in Plastic ampoule
Packaged under inert gas
Cell permeable: yes
Target IC50: 250 nM against PI 3-Kγ
Product competes with ATP.
Toxicity: Irritant (B)
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Bilancio, A., et al. 2006. Blood107, 642.
Camps, M., et al. 2005. Nat. Med.11, 936.
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany