YM-58483 (BTP2)

YM-58483/BTP2 is a blocker of store-operated Ca2+ entry (SOCE), which regulates the activation of non-excitable cells such as lymphocytes.

YM-58483 (also known as BTP2) is a selective SOCE blocker that inhibits anti-CD3 antibody-induced sustained Ca2+ influx in Jurkat T cells. YM-58483 does not cross-react with voltage-operated Ca2+ entry, K+ channels, or Cl− channels. It suppresses the CRAC, TRPC3, and TRPC5 channels, and also facilitates the TRPM4 channel. YM-58483 suppresses cytokine production (IL-2, IL-4, IL-5, IFN-, etc.) and proliferation in T cells in vitro. YM-58483 inhibits the spleen cell proliferation associated with MLR by suppressing NF-AT activation via sustained influx of extracellular Ca2+. YM-58483 potently inhibits IL-2 production and NF-AT-driven promoter activity, but not AP-1-driven promoter activity in Jurkat cells.