Description: Fiboflapon (GSK2190915) is an orally available and effective 5-lipoxygenase-activating protein (FLAP) inhibitor that binds FLAP with a titer of 2.9 nM and inhibition of LTB4 in human blood with an IC50 of 76 nM. Target: FLAP. Smiles:...

GSK2190915 is a selective inhibitor of human 5-lipoxygenase-activating protein (FLAP, IC50 = 2.9 nM). It is selective for FLAP over 5-, 12-, and 15-lipoxygenase, leukotriene A4 (LTA4) hydrolase, LTC4 synthase, COX-1, and COX-2 (IC50s = >10 µm for all). GSK2190915 inhibits production of LTB4 induced by the calcium...