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 (22):

Cat. No. Product Name Effect Purity
  • HY-N1370
    Tanshinone IIA sulfonate sodium Inhibitor
    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-100831
    YM-58483 Inhibitor 99.38%
    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)[1][2].
  • HY-W009724
    2-Aminoethyl diphenylborinate Activator 99.86%
    2-Aminoethyl diphenylborinate (2-APB) is a cell-permeable inhibitor of Inositol triphosphate receptor (IP3R). 2-Aminoethyl diphenylborinate also inhibits the store-operated Ca2+ (SOC) channel and activates some TRP channels (V1, V2 and V3). Additionally, 2-Aminoethyl diphenylborinate has inhibitory effects on vasospasm. At high concentrations, it exhibits specific anti-inflammatory and antioxidant effects in neural tissue[1][2][3][4][5].
  • 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[1].
  • HY-100001
    SKF-96365 hydrochloride Inhibitor 99.71%
    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[1][2].
  • HY-100831R
    YM-58483 (Standard) Inhibitor
    YM-58483 (Standard) is the analytical standard of YM-58483. This product is intended for research and analytical applications. 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)[1][2].
  • HY-N1370R
    Tanshinone IIA sulfonate (sodium) (Standard) Inhibitor
    Tanshinone IIA sulfonate (sodium) (Standard) is the analytical standard of Tanshinone IIA sulfonate (sodium). This product is intended for research and analytical applications. 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-20588
    CRAC intermediate 2 Inhibitor 99.45%
    CRAC intermediate 2 is a intermediate compound for CRAC inhibitor synthesis, extracted from patent WO 2013059666A1.
  • HY-122158
    CRAC channel inhibitor-1 Inhibitor
    CRAC channel inhibitor-1 (compound 55) is a CRAC channel inhibitor. CRAC channel inhibitor-1 can be used in immunology-related research[1].
  • HY-111325
    Synta66 Inhibitor
    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-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-114743
    GS 283 Antagonist
    GS 283 is a compound with calcium antagonist and weak histamine and muscarinic receptor blocking activity, with activity in modulating contraction of guinea pig and rat tracheal smooth muscle. GS 283 inhibits contractions induced by carbachol, histamine (guinea pig only), and high H+ in guinea pig and rat tracheal smooth muscle, inhibits Ca2+-induced contractions in guinea pig tracheal smooth muscle, and at high concentrations completely abolishes contractions induced by carbachol in Ca2+-free medium.
  • HY-103310
    MRS1845 Inhibitor 99.69%
    MRS1845 is a selective store-operated calcium (SOC) channel inhibitor with an IC50 of 1.7 μM[1]. MRS1845 is an ORAI1 inhibitor[2][3]. MRS1845 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
  • HY-147005
    piCRAC-1 Inhibitor 98.24%
    piCRAC-1 is a potent, photoinducible Ca2+ release-activated Ca2+ (CRAC) channel inhibitor. piCRAC-1 alleviates thrombocytopenia and hemorrhage[1].
  • HY-20587
    CRAC intermediate 1 Inhibitor 98.46%
    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.
  • HY-12504
    Pyr6 Inhibitor
    Pyr6 is a selective store operated calcium entry (SOCE) inhibitor with an IC50 of 0.49 μM. Pyr6 displays 37-fold higher potency for RBL SOCE than for TRPC3 ROCE[1].
  • 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[1][2].
  • HY-12521
    GSK-5498A Inhibitor
    GSK-5498A is a selective CARC channel inhibitor (IC50: 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[1].
  • HY-P990478
    Anti-Orai1 Antibody
    Anti-Orai1 Antibody is a humanized antibody expressed in CHO cells that targets Orai1. The Anti-Orai1 Antibody has a huIgG2 heavy chain and a huλ light chain, with an predicted molecular weight (MW) of 150 kDa. The isotype control for Anti-Orai1 Antibody can refer to Human IgG2 kappa, Isotype Control (HY-P99002).
  • HY-113618B
    RO2959 monohydrochloride Inhibitor 98.21%
    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[1][2].