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

IRE1

Inositol requiring enzyme 1

IRE1

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Inositol-requiring enzyme 1 (IRE1) is a bifunctional serine/threonine kinase and endoribonuclease that is a major mediator of the unfolded protein response (UPR) during endoplasmic reticulum (ER) stress. It represents a potential therapeutic target for a number of diseases associated with endoplasmic reticulum stress.

IRE1 is the only identified ER stress sensor in yeast and essential for UPR in animals and plants. As an ER transmembrane protein, IRE1 monitors ER homeostasis through an ER luminal stress-sensing domain and triggers UPR through a cytoplasmic kinase domain and an RNase domain. Upon ER stress, IRE1 RNase is activated through conformational change, autophosphorylation, and higher order oligomerization. Mammalian IRE1 initiates diverse downstream signaling of the UPR either through unconventional splicing of the transcription factor Xbp-1 or and through posttranscriptional modifications via Regulated IRE1-Dependent Decay (RIDD) of multiple substrates.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-U00460
    3,6-DMAD hydrochloride
    		Inhibitor 99.50%
    3,6-DMAD hydrochloride, an acridine derivative, is a potent IRE1α-XBP1s pathway inhibitor. 3,6-DMAD hydrochloride promotes IL-6 secretion via the IRE1α-XBP1s pathway. 3,6-DMAD hydrochloride inhibits IRE1α oligomerization and endoribonuclease (RNase) activity. 3,6-DMAD hydrochloride can be used for research of cancer.
    3,6-DMAD hydrochloride
  • HY-W014605
    Diphenylcyclopropenone
    		Activator 99.86%
    Diphenylcyclopropenone (Diphencyprone) is a potent hapten acting as a topical immunomodulatory agent, which induces an allergic contact dermatitis. Diphenylcyclopropenone induces an increase of cell-surface thiols in cells of a human monocytic cell line, THP-1. Diphenylcyclopropenone acts on the autoreactive T-lymphocytes within the follicular milieu to induce Apoptosis. Diphenylcyclopropenone can be used for alopecia areata research.
    Diphenylcyclopropenone
  • HY-153773
    Z4P
    		Inhibitor 99.32%
    Z4P is a BBB-penatrable IRE1 inhibitor with an IC50 of 1.13 μM. Z4P in combination with Temozolomide (HY-17364) inhibits the growth and recurrence of glioblastoma and has anti-tumor activity.
    Z4P
  • HY-161672
    G-5758
    		Inhibitor 98.91%
    G-5758 is an orally available IRE1α inhibitor with an IC50 of 38 nM for XBP1s. G-5758 is well tolerated in multiple myeloma models (KMS-11) at oral doses up to 500 mg/kg in rats. G-5758 exhibits pharmacodynamics comparable to that of induced IRE1 knockdown.
    G-5758
  • HY-18509
    IRE1α kinase-IN-2
    		Inhibitor 98.50%
    IRE1α kinase-IN-2 is a potent IRE1α kinase inhibitor, with an EC50 of 0.82 μM. IRE1α kinase-IN-2 inhibits IRE1α kinase autophosphorylation (IC50=3.12 μM). IRE1α kinase-IN-2 inhibits XBP1 mRNA splicing in the WT cell lines.
    IRE1α kinase-IN-2
  • HY-107371
    6-Bromo-2-hydroxy-3-methoxybenzaldehyde
    		Inhibitor 99.96%
    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.
    6-Bromo-2-hydroxy-3-methoxybenzaldehyde
  • HY-10255AS
    Sunitinib-d10
    		Inhibitor 99.89%
    Sunitinib-d10 is a deuterium labeled Sunitinib. Sunitinib is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2/KDR/Flk-1 and PDGFRβ, respectively[1]. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation[2].
    Sunitinib-d<sub>10</sub>
  • HY-145425
    PAIR2
    		Antagonist
    PAIR2 is a potent and selective partial antagonist of IRE1α RNase. PAIR2 can completely occupy IRE1α’s ATP-binding site in cells and block the ability of a potent KIRA to inhibit XBP1 splicing.
    PAIR2
  • HY-114368A
    Kira8 Hydrochloride
    		Inhibitor
    Kira8 Hydrochloride (AMG-18 Hydrochloride) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM.
    Kira8 Hydrochloride
  • 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.
    GSK2850163 hydrochloride
  • HY-142659
    IRE1α kinase-IN-6
    		Inhibitor
    IRE1α kinase-IN-6 is a potent IRE1α inhibitor with an IC50 value of 4.4 nM.
    IRE1α kinase-IN-6
  • HY-158393
    IRE1a-IN-2
    		Inhibitor
    IRE1a-IN-2 (Compound 30) is an IRE1α inhibitor, with an IC50 of over than 200 nM for XBP1 mRNA. IRE1a-IN-2 can be used for the research of cancer.
    IRE1a-IN-2
  • HY-158386
    IRE1a-IN-1
    		Inhibitor
    IRE1a-IN-1 (Compound 10) is an IRE1α inhibitor, with an IC50 of less than 100 nM for XBP1 mRNA. IRE1a-IN-1 can be used for the research of cancer.
    IRE1a-IN-1
  • HY-153475
    IRE1α kinase-IN-9
    		Inhibitor
    IRE1α kinase-IN-9 (compound 2) is a potent IRE-1α inhibitor，exhibits an average IC50 value of <0.1 μM. IRE1α kinase-IN-9 can be used for research in diseases associated with the unfolded protein response or with regulated IRE1-dependent decay (RIDD).
    IRE1α kinase-IN-9
  • HY-145422
    KIRA9
    		Inhibitor
    KIRA9 is a potent IRE1 inhibitor (IC50=4.8 μM in INS-1 cells). KIRA9 is able to fully engage the ATP-binding site of IRE1α. KIRA9 can block ER-localized mRNA decay and apoptosis.
    KIRA9
  • HY-145419
    IRE1α kinase-IN-4
    		Inhibitor
    IRE1α kinase-IN-4 (compound 6) is a potent IRE1α inhibitor with an Ki of 140 nM. IRE1α kinase-IN-4 is the ATP-competitive ligands of IRE1α.
    IRE1α kinase-IN-4
  • HY-153474
    IRE1α kinase-IN-8
    		Inhibitor
    IRE1α kinase-IN-8, a benzoheterocyclecarboxaldehyde derivative, is a potent IRE-1α inhibitor. IRE1α kinase-IN-8 can be used for research in diseases associated with the unfolded protein response or with regulated IRE1-dependent decay (RIDD).
    IRE1α kinase-IN-8
  • HY-114611
    BDM44768
    BDM44768 is an inhibitior of IDE. BDM44768 exacerbates ER stress-induced IRE1 activation and promotes lipid accumulation in hepatocytes. BDM44768 potentiates activation of the IRE1 pathway in the liver and exacerbates liver lipid accumulation in an acute mice model of ER stress.
    BDM44768
  • HY-U00460B
    3,6-DMAD dihydrochloride
    		Inhibitor
    3,6-DMAD dihydrochloride, an acridine derivative, is a potent IRE1α-XBP1s pathway inhibitor. 3,6-DMAD dihydrochloride promotes IL-6 secretion via the IRE1α-XBP1s pathway. 3,6-DMAD dihydrochloride inhibits IRE1α oligomerization and endoribonuclease (RNase) activity. 3,6-DMAD dihydrochloride can be used for research of cancer.
    3,6-DMAD dihydrochloride
  • HY-145420
    IRE1α kinase-IN-5
    		Inhibitor
    IRE1α kinase-IN-5 (compound 7) is a potent IRE1α inhibitor with an Ki of 98 nM. IRE1α kinase-IN-5 is the ATP-competitive ligands of IRE1α.
    IRE1α kinase-IN-5
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity