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IRE1

IRE1 inhibitors block inositol-requiring enzyme 1 (IRE1), a sensor of endoplasmic reticulum stress. In 1993, yeast IRE1 was identified as a transmembrane protein kinase required to induce genes for endoplasmic reticulum resident proteins. The enzyme couples a cytosolic kinase domain to an endoribonuclease (RNase) domain. Studies in 2001 and 2002 showed that IRE1 splices X-box binding protein 1 (XBP1) mRNA, producing an active transcription factor of the unfolded protein response. 4μ8C, STF-083010 and MKC8866 inhibit the RNase activity of IRE1α. KIRA6 and Kira8 bind the kinase site and suppress RNase activity allosterically, whereas APY29 is an ATP-competitive ligand of the kinase domain.

3 Items

  • IXA4
    Cat. No.
    A54705
    CAS No.
    1185329-96-7

    IXA4

    IXA4 is a selective activator of the IRE1/XBP1s signaling pathway. It uniquely stimulates IRE1/XBP1s activation without inducing a global unfolded protein response or engaging other stress-responsive signaling mechanisms, such as the heat shock or oxidative stress responses. IXA4 has been shown to effectively reduce the secretion of amyloid precursor protein (APP), making it a valuable tool for studies aimed at understanding protein homeostasis and cellular stress responses.

    In stock View Details
    1 mg
    $25.00
    5 mg
    $65.00
    All 6 sizes
  • IXA6
    Cat. No.
    A54707
    CAS No.
    1021106-40-0

    IXA6

    IXA6 is a specific activator of IRE1, leading to the activation of XBP1s through the induction of IRE1 RNase activity. This compound plays a crucial role in regulating the unfolded protein response (UPR) and enhancing ER stress signaling pathways. IXA6 is valuable for research into cellular stress responses, protein folding mechanisms, and potential therapeutic interventions in diseases linked to ER dysfunction.

    In stock View Details
    1 mg
    $175.00
    5 mg
    $445.00
    All 3 sizes
  • IXA62
    Cat. No.
    A54711
    CAS No.
    956783-34-9

    IXA62

    IXA62 is an orally active and selective activator of IRE1/XBP1s, exhibiting an EC50 value of 0.31 μM. This compound is shown to reduce Aβ secretion, making it a potential candidate for research into Alzheimer's disease pathology. Additionally, IXA62 enhances glucose-stimulated insulin secretion in rat insulinoma cells, highlighting its applicability in studies of glucose metabolism and diabetes research.

    In stock View Details
    5 mg
    $125.00
    10 mg
    $205.00
    All 4 sizes

3 Items

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