CRAC Channel
Calcium release-activated channels; Ca2+ release-activated Ca2+ channels
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.
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CRAC Channel Related Products (24)
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Antibodies (5)
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2-Aminoethyl diphenylborinate
0 ImagesSynonyms: 2-APB2-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.
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SKF-96365 (hydrochloride)
0 ImagesSKF-96365 hydrochloride is a TRPC channel antagonist and store-operated calcium entry (SOCE) inhibitor. SKF-96365 hydrochloride reduces calcium ion influx by inhibiting the activity and expression of TRPC6, STIM1 and Orai1. SKF-96365 hydrochloride inhibits voltage-gated sodium current (cardiac INa/NaV1.5) and slows myocardial conduction. SKF-96365 hydrochloride inhibits phosphorylation/activation of CaMKIIγ and suppresses the downstream AKT signaling pathway. SKF-96365 hydrochloride induces G2/M phase cell cycle arrest, apoptosis and cytoprotective autophagy in colorectal cancer cells. SKF-96365 hydrochloride alleviates allergic rhinitis symptoms by reducing inflammatory cytokine levels. SKF-96365 hydrochloride reduces intracellular calcium overload, inhibits Homer1 expression, prevents nuclear damage and suppresses apoptosis. SKF-96365 hydrochloride inhibits the growth of colorectal cancer xenografts in nude mice. SKF-96365 hydrochloride is applicable to research related to allergic rhinitis, colorectal cancer, Parkinson's disease, persistent spontaneous nociception and hyperalgesia.
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Zegocractin
0 ImagesSynonyms: CM-4620Zegocractin (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.
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Synta66
0 ImagesSynta66 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.
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MRS1845
0 ImagesMRS1845 is a selective store-operated calcium (SOC) channel inhibitor with an IC50 of 1.7 μM. MRS1845 is an ORAI1 inhibitor. 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.
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RO2959 monohydrochloride
0 ImagesRO2959 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.
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Pyr6
0 ImagesSynonyms: N-[4-[3,5-Bis(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-3-fluoro-4-pyridinecarboxamidePyr6 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.
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GSK-5498A
0 ImagesGSK-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.
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SKF-96365
0 ImagesSKF-96365 is a TRPC channel antagonist and store-operated calcium entry (SOCE) inhibitor. SKF-96365 reduces calcium ion influx by inhibiting the activity and expression of TRPC6, STIM1 and Orai1. SKF-96365 inhibits voltage-gated sodium current (cardiac INa/NaV1.5) and slows myocardial conduction. SKF-96365 inhibits phosphorylation/activation of CaMKIIγ and suppresses the downstream AKT signaling pathway. SKF-96365 induces G2/M phase cell cycle arrest, apoptosis and cytoprotective autophagy in colorectal cancer cells. SKF-96365 alleviates allergic rhinitis symptoms by reducing inflammatory cytokine levels. SKF-96365 reduces intracellular calcium overload, inhibits Homer1 expression, prevents nuclear damage and suppresses apoptosis. SKF-96365 inhibits the growth of colorectal cancer xenografts in nude mice. SKF-96365 is applicable to research related to allergic rhinitis, colorectal cancer, Parkinson's disease, persistent spontaneous nociception and hyperalgesia.
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SOCE inhibitor 1
0 ImagesSOCE inhibitor 1 (Compound 39) is a store-operated calcium entry (SOCE) inhibitor with an IC50 of 4.4 μM. SOCE inhibitor 1 has a good stability in plasma.
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RO2959 hydrochloride
0 ImagesRO2959 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.
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Anti-Orai1 Antibody
0 ImagesCat. No.: HY-P990478Purity: 99.16%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).
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CRAC intermediate 2
0 ImagesCRAC intermediate 2 (the starting compound in example 23) is an intermediate. CRAC intermediate 2 can be used in the research of CRAC inhibitors.
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GS 283
0 ImagesCat. No.: HY-114743CAS No.: 149440-36-8GS 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.
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Tanshinone IIA sulfonate sodium (Standard)
0 ImagesSynonyms: Sodium Tanshinone IIA sulfonate (Standard); Tanshinone IIA sodium sulfonate (Standard)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.
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GSK-5503A
0 ImagesCat. No.: HY-103071CAS No.: 1253186-46-7GSK-5503A is a calcium-release activated calcium (CRAC) channel blocker. GSK-5503A effectively inhibits stromal interaction molecule 1 (STIM1) mediated Orai1 and Orai3 currents in vitro. GSK-5503A can be used for the research of asthma and allergic disorders.
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CRAC channel inhibitor-1
0 ImagesCat. No.: HY-122158CAS No.: 903591-53-7CRAC channel inhibitor-1 (compound 55) is a CRAC channel inhibitor. CRAC channel inhibitor-1 can be used in immunology-related research.
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