YM-201636 is a potent, selective PIKfyve inhibitor with IC50 of 33 nM, does not inhibit type Iiγ/Iα PtdInsP kinases even at 10 uM (p110α IC50=3.3 uM).
YM-201636 shows insensitivity against yeast orthologue of PIKfyve, Fab1; significantly decreases the production of PtdIns(3,5)P2 by 80% in serum-starved NIH3T3 cells with no effect on serum-stimulated PKB Ser 473 phosphorylation at 0.8 uM.
YM-201636 inhibits basal and insulin-activated 2-deoxyglucose uptake withIC50 of 54 nM.
YM-201636 significantly reduces retroviruses budding from cells; blocks the continuous recycling of the tight junction proteins claudin-1 and claudin-2 in MDCK cells.
