GSK-5498A is a selective CARC channel inhibitor ( IC 50 : 1 μM). GSK-5498A inhibits mediators release from mast cells and pro-inflammatory cytokines release from T cells. GSK-5498A can be used in the research of inflammatory disorders
In Vitro
GSK-5498A (1 and 10 μM) inhibits calcium influx through CRAC channels in human embryonic kidney cells. GSK-5498A (1 nM-10 μM) inhibits the thapsigargin-evoked fluorescence signal (pIC 50 : 6.3) in Jurkat cells, measured using the calcium sensitive dye: Fluo4-AM. GSK-5498A (1 nM-10 μM) evokes concentration-dependent inhibition of Cytostim-evoked interferon-γ and IL-5 production in PBMCs. GSK-5498A (1 μM-10 μM) inhibits degranulation of rat tissue-resident mast cells. GSK-5498A (10 nM-10 μM) inhibits mouse and rat T-cell cytokine (IL-2) release. GSK-5498A (0-10 μM) shows high selectivity for CRAC channels over other ion channels, enzymes and G-protein coupled receptors. MCE has not independently confirmed the accuracy of these methods. They are for reference only.