YM-58483 is a potent store-operated Ca2+ entry blocker and CRAC channel inhibitor with IC50 of 100 nM.
YM-58483 inhibits Ca(2+) influx through SOC channels without affecting the TCR signal transduction cascade in Jurkat cells, inhibits thapsigargin-induced sustained Ca(2+) influx (IC50=100 nM), and 30-fold less potent against Cav channels.
YM-58483 potently inhibits IL-2 production and NF-AT-driven promoter activity in Jurkat cells.
YM-58483 also inhibits IL-4 and IL-5 production Th2 T cells, prevents antigen-induced inflammatory responses in animal models; orally active.
