| Description |
A cell-permeable pyridofuropyrimidine compound that selectively inhibits mammalian type III PtdInsP kinase (IC 50 = 33 nM and >5 µM using murine PIKfyve and yeast Fab1, respectively), while exhibiting much reduced activity against p110α (IC 50 = 3.3 µM) and little activity against type IIγ PtdInsP kinase even at concentrations as high as 10 µM. Shown to block serum-induced PtdIns(3,5)P 2 production in NIH3T3 cells (80% inhibition at 800 nM) and disrupt cellular endosomal transport in a reversible manner.
|
