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You are here:Home-Inhibitors & Agonists-Membrane Transporter/Ion Channel-CRAC Channel

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The Ca2+ release-activated Ca2+ (CRAC) channel is a highly Ca2+-selective store-operated channel expressed in T cells, mast cells, and various other tissues. CRAC channels regulate critical cellular processes such as gene expression, motility, and the secretion of inflammatory mediators. The identification of Orai1, a key subunit of the CRAC channel pore, and STIM1, the endoplasmic reticulum (ER) Ca2+ sensor, have provided the tools to illuminate the mechanisms of regulation and the pore properties of CRAC channels. Opening of CRAC channels enables the refilling of ER Ca2+ stores and sustains long-lasting Ca2+oscillations and plateau signals, critical for the proliferation of T cells and production of cytokines following antigenic stimulation.

Cat. No. Product Name CAS No. Information
H4361

YM-58483

 		223499-30-7

A store-operated Ca2+ entry blocker and CRAC channel inhibitor with IC50 of 100 nM; 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; potently inhibits IL-2 production and NF-AT-driven promoter activity in Jurkat cells; also inhibits IL-4 and IL-5 production Th2 T cells, prevents antigen-induced inflammatory responses in animal models; orally active.
H4360

GSK-5498A

 		1253186-49-0

GSK-5498A is a potent, selective small molecule blocker of Calcium-Release Activated Calcium (CRAC) channel with IC50 of 1 uM; completely inhibits calcium influx through CRAC channels, inhibits mediator release from mast cells, and pro-inflammatory cytokine release from T-cells from multiple human and rat preparations.

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