1. Signaling Pathways
  2. Cell Cycle/DNA Damage
  3. IRE1


The serine/threonine-protein kinase/endoribonuclease inositol-requiring enzyme 1 (IRE1) is an enzyme that in humans is encoded by the ERN1 gene. IRE1 is an endoplasmic reticulum (ER) transmembrane sensor that activates UPR to maintain ER and cellular function. While mammalian IRE1 promotes cell survive, it can initiate apoptosis via decay of anti-apoptotic microRNAs.

IRE1 activation is initiated by homotypic interactions of the stress-sensing lumenal domain favoring transautophosphorylation of the kinase-extension nuclease (KEN) domain on the cytoplasmic side of the ER membrane.

IRE1/XBP-1 has been shown to regulate a variety of genes in various cell types in response to ER stress, mostly related to ER function and the secretory pathway, although the target genes vary depending on the cell type and nature of the stress stimuli.

IRE1 Related Products (14):

Cat. No. Product Name Effect Purity
  • HY-15845
    STF-083010 Inhibitor >98.0%
    STF-083010 is a specific IRE1α inhibitor. STF-083010 inhibits Ire1 endonuclease activity, without affecting its kinase activity, after endoplasmic reticulum stress.
  • HY-19707
    4μ8C Inhibitor 98.95%
    4μ8C (IRE1 Inhibitor III) is a small-molecule inhibitor of IRE1α.
  • HY-19708
    KIRA6 Inhibitor 98.75%
    KIRA6, an advanced small-molecule IRE1α RNase kinase inhibitor with an IC50 of 0.6 µM. KIRA6 can trigger an apoptotic response.
  • HY-17537
    APY29 Inhibitor 99.54%
    APY29 is an allosteric modulator of IRE1α which inhibits IRE1α autophosphorylation with IC50 of 280 nM and activates IRE1α RNase activity.
  • HY-104040
    MKC8866 Inhibitor 98.38%
    MKC8866, a salicylaldehyde analog, is a potent, selective IRE1 RNase inhibitor with an IC50 of 0.29 μM in human vitro. MKC8866 strongly inhibits DTT-induced X-box-binding protein 1-spliced (XBP1s) expression with an EC50 of 0.52 μM and unstresses RPMI 8226 cells with an IC50 of 0.14 μM. MKC8866 inhibits IRE1 RNase in breast cancer cells leading to the decreased production of pro-tumorigenic factors and it can inhibits prostate cancer (PCa) tumor growth .
  • HY-103248
    Toyocamycin Inhibitor
    Toyocamycin (Vengicide) is an adenosine analog produced by Actinomycete, acts as an XBP1 inhibitor, inhibits IRE1α-induced ATP-dependent XBP1 mRNA cleavage, with an IC50 of 80 nM. Toyocamycin (Vengicide) induces apoptosis. Toyocamycin (Vengicide) shows no effect on IRE1α auto-phosphorylation.
  • HY-19710
    MKC3946 Inhibitor 99.77%
    MKC3946 is a potent and soluble IRE1α inhibitor, used for cancer research.
  • HY-U00459
    GSK2850163 Inhibitor 98.50%
    GSK2850163 is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α) which can inhibit IRE1α kinase activity and RNase activity with IC50s of 20 and 200 nM, respectively.
  • HY-12399
    MKC9989 Inhibitor 98.61%
    MKC9989 is a Hydroxy aryl aldehydes (HAA) inhibitor and also inhibits IRE1α with an IC50 of 0.23 to 44 μM.
  • HY-107371
    6-Bromo-2-hydroxy-3-methoxybenzaldehyde Inhibitor 99.87%
    6-Bromo-2-hydroxy-3-methoxybenzaldehyde (NSC95682) is an IRE-1α inhibitor with an IC50 of 0.08 μM, extracted from patent WO 2008154484 A1, IRE-lα inhibitor compound 3-5.
  • HY-114368
    Kira8 Inhibitor 99.74%
    Kira8 is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM.
  • HY-U00460
    3,6-DMAD hydrochloride Inhibitor >98.0%
    3,6-DMAD hydrochloride is a inhibitor of the IRE1α-XBP1 pathway of the unfolded protein response.
  • HY-107400
    B I09 Inhibitor
    B I09 is an IRE-1 RNase inhibitor, with an IC50 of 1230 nM.
  • HY-U00459B
    GSK2850163 hydrochloride Inhibitor
    GSK2850163 hydrochloride is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α) which can inhibit IRE1α kinase activity and RNase activity with IC50s of 20 and 200 nM, respectively.
Isoform Specific Products

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