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

CRAC Channel (钙释放激活钙通道)

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 相关产品 (12):

目录号 产品名 作用方式 纯度
  • HY-100001
    SKF-96365 hydrochloride Inhibitor 99.51%
    SKF-96365 hydrochloride 是一种有效的 TRP channel 阻滞剂和 SOCE (store-operated Ca2+ entry) 抑制剂。SKF-96365 hydrochloride 可显著抑制豚鼠离体心脏 hERG、hKCNQ1/hKCNE1、hKir2.1 和 hKv4.3 电流,显著延长 QTc 间期。SKF-96365 hydrochloride 通过诱导结直肠癌细胞的细胞周期阻滞和凋亡 (apoptosis) 而显示出强大的抗肿瘤活性。
  • HY-100831
    YM-58483 Inhibitor 99.78%
    YM-58483 (BTP2) 是一种有效的 CRAC channels 抑制剂,能够抑制 Ca2+ 信号。YM-58483 阻断钙池操纵的阳离子内流 (SOCE)。
  • HY-101942
    Zegocractin Inhibitor 99.96%
    Zegocractin (CM-4620) 是一种钙离子释放激活通道 (CRAC channel) 的抑制剂,其对 Orai1/STIM1Orai2/STIM1IC50 值分别为 119 nM 和 895 nM。
  • HY-N1370
    Tanshinone IIA sulfonate sodium Inhibitor ≥98.0%
    Tanshinone IIA sulfonate sodium 是 tanshinone IIA 的衍生物,为 SOCE 的抑制剂,用于心血管疾病的研究。
  • HY-111325
    Synta66 Inhibitor ≥98.0%
    Synta66 是钙离子通道 Orai (CRAC 的核心) 的抑制剂,主要用于神经疾病的研究。
  • HY-103310
    MRS1845 Inhibitor 99.27%
    MRS1845 是一种选择性钙池调控钙离子通道 (SOC) 抑制剂,IC50 为 1.7 μM。MRS1845 是一种 ORAI1 抑制剂。
  • HY-12521
    GSK-5498A Inhibitor 98.14%
    GSK-5498A 是一种选择性的钙释放激活钙通道 (CARC) 抑制剂 (IC50,1 μM);抑制肥大细胞介质释放和 T 细胞促炎性细胞因子的释放。
  • HY-113618B
    RO2959 monohydrochloride Inhibitor 99.02%
    RO2959 monohydrochloride 是一种有效的选择性 CRAC 通道抑制剂,IC50 为 402 nM。RO2959 monohydrochloride 是由 Orai1/Stim1 通道介导的钙存储进入 (SOCE) 的有效阻滞剂,IC50 为 25 nM。RO2959 monohydrochloride 还是人 IL-2 产生的有效抑制剂,有效阻断 T 细胞受体触发的基因表达和 T 细胞功能途径。
  • HY-113618A
    RO2959 hydrochloride Inhibitor
    RO2959 hydrochloride 是一种有效的选择性 CRAC 通道抑制剂,IC50 为 402 nM。RO2959 hydrochloride 是由 Orai1/Stim1 通道介导的钙存储进入 (SOCE) 的有效阻滞剂,IC50 为 25 nM。RO2959 hydrochloride 还是人 IL-2 产生的有效抑制剂,有效阻断 T 细胞受体触发的基因表达和 T 细胞功能途径。
  • HY-20588
    CRAC intermediate 2 Inhibitor 99.96%
    CRAC intermediate 2是摘自专利WO 2013059666A1中用于CRAC系列抑制剂合成的中间体。
  • HY-112913
    SOCE inhibitor 1 Inhibitor
    SOCE inhibitor 1是钙库调控的钙通道抑制剂,IC50为4.4 μM。
  • HY-20587
    CRAC intermediate 1 Inhibitor 98.0%
    CRAC intermediate 1是从专利WO 2010122089摘取出的关键中间体,用于CRAC离子通道系列化合物的合成。
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