Fluprostenol is a metabolically stable analog of PGF2alpha with potent FP receptor agonist activity. Fluprostenol is the optically active enantiomer of fluprostenol and would be expected to have twice the potency as the racemic mixture. Fluprostenol inhibits PGF2alpha binding to human and rat FP receptors with IC50...

m-3M3FBS is an activator of phospholipase C (PLC) that stimulates superoxide generation, increase in cytoplasmic calcium, and inositol phosphate formation in human neutrophils when used at a concentration of 15-50 µM. It stimulates cytoplasmic calcium increases in several cell lines and, at 25 µM in vitro, promotes...

Astemizole is a non-sedating antihistamine that antagonizes the histamine H1 receptor with a Ki value of 4.4 nM. It is considerably less potent at muscarinic acetylcholine receptors (Ki = 2.4 µM). Astemizole is also a potent blocker of ether-a-go-go-related gene (ERG) potassium channels (IC50 = ~1 nM) that has been...

BMS 345541 is a cell permeable inhibitor of the IkappaB kinases IKKalpha and IKKbeta (IC50s = 4 and 0.3 µM). It is without effect against a panel of other serine/threonine and tyrosine kinases at 100 µM. BMS 345541 inhibits signaling through nuclear factor-kappaB (NF-kappaB) both in cells and in vivo, showing...