PI 3-Kδ/γ Inhibitor XV, SW-14

A cell permeable, ATP competitive tolyl quinazolinone inhibitor of PI 3-Kδ/γ that displays 70-fold selectivity over PI 3-Kβ and 900-fold selectivity over PI 3-Kα in enzymatic assays with an IC₅₀ = 9 nM for PI3Kδ and 21 nM for PI 3-Kγ and in a cell-based assay with an EC₅₀ = 132 nM for PI 3-Kδ and 4.5 nM for PI 3-K γ. It elicits an inflammatory marker suppression effect in co-cultures of HUVEC and PBMCs stimulated with lipopolysacharide. Additionally, TNFα production decreases dose-dependently in the same cell lines treated with 370 nM to 10 µM of compound. SW14 exhibits a stronger effect compared to that of PI 3-Kδ inhibition (SW30) or pan-PI 3-K inhibition with different anti-inflammatory profile. In contrast to PI 3-Kα/β it also shows very little anti-proliferative effects even at the highest dose tested (10 µM) in HUVEC culture only.

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

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

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

Toxicity: Standard Handling (A)