Biochem/physiol Actions

Reversible: no

Product competes with ATP.

Target IC₅₀: 250 nM against PI 3-Kγ

Primary TargetPI 3-Kγ

Cell permeable: yes

General description

A cell-permeable thiazolidinedione compound that acts as a potent and ATP-competitive inhibitor of PI 3-Kγ (K_i = 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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Bilancio, A., et al. 2006. Blood107, 642.Camps, M., et al. 2005. Nat. Med.11, 936.

Packaging

Packaged under inert gas

5 mg in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Irritant (B)