1. Signaling Pathways
  2. Membrane Transporter/Ion Channel
  3. CRAC Channel

CRAC Channel

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.

STIM1 proteins span through the membrane of the ER, are competent in sensing luminal Ca 2+ concentration, and in turn, are responsible for relaying the signal of Ca2+ store-depletion to pore-forming Orai1 proteins in the plasma membrane. A direct interaction of STIM1 and Orai1 allows for the re-entry of Ca2+ from the extracellular space. CRAC channels are critical for lymphocyte function and immune responses. A driving force in the quest for CRAC channel drugs has been the immunocompromised phenotype displayed by humans and mice with null or loss-of-function mutations in STIM1 or Orai1, suggesting that CRAC channel inhibitors could be useful therapeutics for autoimmune or inflammatory conditions.

CRAC Channel Related Products (12):

Cat. No. Product Name Effect Purity
  • HY-100001
    SKF-96365 hydrochloride
    Inhibitor 99.51%
    SKF-96365 hydrochloride is a potent TRP channel blocker and a store-operated Ca2+ entry (SOCE) inhibitor. SKF-96365 hydrochloride significantly inhibits hERG, hKCNQ1/hKCNE1, hKir2.1 and hKv4.3 current, and significantly prolongs the QTc interval in isolated guinea pig hearts. SKF-96365 hydrochloride exhibits potent anti-neoplastic activity by inducing cell-cycle arrest and apoptosis in colorectal cancer cells.
  • HY-100831
    YM-58483
    Inhibitor 99.78%
    YM-58483 (BTP2) is the first selective and potent inhibitor of CRAC channels and subsequent Ca2+ signals. YM-584832 is a blocker of store-operated Ca2+ entry (SOCE).
  • HY-101942
    Zegocractin
    Inhibitor 99.96%
    Zegocractin (CM-4620) is a calcium-release activated calcium-channel (CRAC channel) inhibitor, with IC50s of 119 nM and 895 nM for Orai1/STIM1 and Orai2/STIM1 channels, respectively.
  • HY-N1370
    Tanshinone IIA sulfonate sodium
    Inhibitor ≥98.0%
    Tanshinone IIA sulfonate (sodium) is a derivative of tanshinone IIA, which acts as an inhibitor of store-operated Ca2+ entry (SOCE), and is used to treat cardiovascular disorders.
  • HY-111325
    Synta66
    Inhibitor ≥98.0%
    Synta66 is an inhibitor of store-operated calcium entry channel Orai, which forms the pore of the CRAC channel, and used for the research of neurological disease.
  • HY-103310
    MRS1845
    Inhibitor 99.27%
    MRS1845 is a selective store-operated calcium (SOC) channel inhibitor with an IC50 of 1.7 μM. MRS1845 is an ORAI1 inhibitor.
  • HY-12521
    GSK-5498A
    Inhibitor 98.14%
    GSK-5498A is a selective small molecule blocker of CARC (IC50, 1 μM); inhibits mediator release from mast cells, and pro-inflammatory cytokine release from T-cells in a variety of species.
  • HY-113618B
    RO2959 monohydrochloride
    Inhibitor 99.02%
    RO2959 monohydrochloride is a potent and selective CRAC channel inhibitor with an IC50 of 402 nM. RO2959 monohydrochloride is a potent blocker of store operated calcium entry (SOCE) mediated by Orai1/Stim1 channels with an IC50 of 25 nM. RO2959 monohydrochloride is also a potent inhibitor of human IL-2 production, and potently blocks T cell receptor triggered gene expression and T cell functional pathways.
  • HY-113618A
    RO2959 hydrochloride
    Inhibitor
    RO2959 hydrochloride is a potent and selective CRAC channel inhibitor with an IC50 of 402 nM. RO2959 hydrochloride is a potent blocker of store operated calcium entry (SOCE) mediated by Orai1/Stim1 channels with an IC50 of 25 nM. RO2959 hydrochloride is also a potent inhibitor of human IL-2 production, and potently blocks T cell receptor triggered gene expression and T cell functional pathways.
  • HY-20588
    CRAC intermediate 2
    Inhibitor 99.96%
    CRAC intermediate 2 is a intermediate compound for CRAC inhibitor synthesis, extracted from patent WO 2013059666A1.
  • HY-112913
    SOCE inhibitor 1
    Inhibitor 99.73%
    SOCE inhibitor 1 is a store-operated calcium entry (SOCE) inhibitor with an IC50 of 4.4 μM.
  • HY-20587
    CRAC intermediate 1
    Inhibitor 98.0%
    CRAC intermediate 1 is a key intermediate in the chemical synthesis of a series of CRAC channel inhibitors, detailed information can be found in Patent WO 2010122089 A1, intermediate 9.
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