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-10255A
    Sunitinib
    		Inhibitor 99.04%
    Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
    Sunitinib
  • HY-19707
    4μ8C
    		Inhibitor 99.95%
    4μ8C (IRE1 Inhibitor III) is a small-molecule inhibitor of IRE1α.
    4μ8C
  • HY-104040
    MKC8866
    		Inhibitor 99.95%
    MKC8866, a salicylaldehyde analog, is a potent, selective IRE1 RNase inhibitor with an IC50 of 0.29 μM in human vitro. MKC8866 strongly inhibits Dithiothreitol-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.
    MKC8866
  • 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.
    STF-083010
  • HY-139214
    IXA4
    		Inhibitor 98.83%
    IXA4 is a highly selective, non-toxic IRE1/XBP1s activator. IXA4 activates IRE1/XBP1s signaling without globally activating the unfolded protein response (UPR) or other stress-responsive signaling pathways (e.g., the heat shock response or oxidative stress response). IXA4 reduces secretion of APP through IRE1 activation.
    IXA4
  • HY-176040
    IXA62
    		Inhibitor 99.88%
    IXA62 is an orally active and selective IRE1/XBP1s activator (EC50 = 0.31 μM) that reduces Aβ secretion. IXA62 enhances glucose-stimulated insulin secretion from rat insulinoma cells.
    IXA62
  • HY-174991
    CPD-2828
    		Inhibitor
    CPD-2828 is an orally active and selective IRE1α inhibitor with an IC50 value of 1.2 μM. CPD-2828 is promising for research of endoplasmic reticulum stress-related diseases (e.g., cancer, neurodegenerative diseases).
    CPD-2828
  • HY-170849
    Nur77 modulator 4
    Nur77 modulator 4 (Compound 15h) is a Nur77 inducer with a KD of 0.477 μM. Nur77 modulator 4 significantly induces Nur77 expression and apoptosis, showing excellent growth inhibition in HepG2 and MCF-7 cells, with an IC50 of less than 5 μM. Nur77 modulator 4 activates Nur77-mediated ER stress through the PERK-ATF4 and IRE1 signaling pathways, thereby inducing cell apoptosis. Nur77 modulator 4 can be used in cancer research applications .
    Nur77 modulator 4
  • HY-103248
    Toyocamycin
    		Inhibitor 99.78%
    Toyocamycin (Vengicide) is an adenosine analog produced by Streptomyces diastatochromogenes, acts as an XBP1 inhibitor. Toyocamycin blocks RNA synthesis and ribosome function, and induces apoptosis. Toyocamycin affects IRE1α-XBP1 pathway, and inhibits XBP1 mRNA cleavage with an IC50 value of 80 nM with affecting IRE1α auto-phosphorylation. Toyocamycin specifically inhibits CDK9 with an IC50 value of 79 nM.
    Toyocamycin
  • HY-19708
    KIRA6
    		Inhibitor 99.86%
    KIRA6 is an advanced small-molecule IRE1α RNase kinase inhibitor with an IC50 of 0.6 µM. KIRA6 can trigger an apoptotic response.
    KIRA6
  • HY-10255
    Sunitinib Malate
    		Inhibitor 99.86%
    Sunitinib Malate (SU 11248 Malate) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib Malate, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
    Sunitinib Malate
  • HY-114368
    Kira8
    		Inhibitor 98.90%
    Kira8 (AMG-18) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM.
    Kira8
  • HY-U00459
    GSK2850163
    		Inhibitor 98.25%
    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.
    GSK2850163
  • HY-17537
    APY29
    		Inhibitor 99.90%
    APY29, an ATP-competitive inhibitor, is an allosteric modulator of IRE1α which inhibits IRE1α autophosphorylation by binding to the ATP-binding pocket with IC50 of 280 nM. APY29 acts as a ligand that allosterically activates IRE1α adjacent RNase domain.
    APY29
  • HY-19710
    MKC3946
    		Inhibitor 99.21%
    MKC3946 is a potent IRE1α inhibitor, used for cancer research.
    MKC3946
  • HY-107400
    B I09
    		Inhibitor 99.35%
    B I09 is an IRE-1 RNase inhibitor, with an IC50 of 1230 nM.
    B I09
  • HY-139212
    IXA6
    		Activator 99.29%
    IXA6 is a novel IRE1/XBP1s activator, and can induce IRE1 RNase activity.
    IXA6
  • HY-19696B
    Tauroursodeoxycholate dihydrate
    		Inhibitor 99.96%
    Tauroursodeoxycholate dehydrate is an orally active taurine conjugate of Ursodeoxycholic acid (HY-13771). Tauroursodeoxycholate dehydrate inhibits caspase-3/7, Apoptosis, IRE1α/TRAF2/NF-κB, prevents JNK phosphorylation, inhibits ROS generation, and activates Akt signaling. Tauroursodeoxycholate dehydrate prevents cataract formation, reduces renal tubular damage in type 2 diabetic mice, reduces I/R injury in liver, and inhibits intestinal inflammation and barrier disruption in nonalcoholic fatty liver disease.
    Tauroursodeoxycholate dihydrate
  • HY-136735
    IRE1α kinase-IN-1
    		Inhibitor 98.94%
    IRE1α kinase-IN-1 is a highly selective IRE1α (ERN1) inhibitor, with an IC50 of 77 nM. IRE1α kinase-IN-1 displays 100-fold selectivity for IRE1α over the IRE1β isoform. IRE1α kinase-IN-1 inhibits ER stress-induced IRE1α oligomerization and autophosphorylation, and also inhibits IRE1α RNase activity (IC50=80 nM).
    IRE1α kinase-IN-1
  • HY-161672
    G-5758
    		Inhibitor 98.91%
    G-5758 is a selective and orally effective IRE1α inhibitor with an IC50 of 38 nM (detected by the XBP1s luciferase reporter cell assay). G-5758 is still well tolerated in rats at oral doses up to 500 mg/kg. G-5758 can be used in the research of multiple myeloma.
    G-5758
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity