General description

A cell permeable, ATP-competitive and selective tolyl quinazolinone inhibitor of PI 3-Kδ (IC₅₀ = 7 nM, 1300 nM, 85000 nM, and 740 nM for PI 3-Kδ PI 3-Kγ PI 3-Kα and PI 3-Kβ, respectively) in an enzymatic assay with an EC₅₀ = 16 nM for PI 3-Kδ and 2.7 µM for PI 3-Kγ in a cell based assay. It elicits an inflammatory marker suppression effect in co-cultures of HUVEC and PBMCs under superantigen stimulated conditions. This compound, at concentrations between 370 nM and 10 µM, leads to a dose-dependent decrease in E-selectin expression. Furthermore, it is not cytotoxic to HUVEC cells.

A cell permeable, ATP-competitive and selective tolyl quinazolinone inhibitor of PI 3-Kδ (IC₅₀ = 7 nM, 1300 nM, 85000 nM, and 740 nM for PI 3-Kδ, PI 3-Kγ PI 3-Kα and PI 3-Kβ, respectively) in an enzymatic assay with an EC₅₀ = 16 nM for PI 3-Kδ and 2.7 µM for PI 3-Kγ in a cell based assay. It elicits an inflammatory marker suppression effect in co-cultures of HUVEC and PBMCs under superantigen stimulated conditions. This compound, at concentrations between 370 nM and 10 µM, leads to a dose-dependent decrease in E-selectin expression. Furthermore, it is not cytotoxic to HUVEC cells.

Legal Information

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

Other Notes

Williams, O., et al. 2010. Chem Biol.17, 123.

Packaging

5 mg in Glass bottle

Reconstitution

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

Warning

Toxicity: Regulatory Review (Z)