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

IRE1

Inositol requiring enzyme 1

IRE1

Related Products

PDF 0.39 MB

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-124646
    KIRA-7
    		Inhibitor 99.09%
    KIRA-7, an imidazopyrazine compound, binds the IRE1α kinase (IC50 of 110 nM) to allosterically inhibit its RNase activity. KIRA-7 has an anti-fibrotic effect.
    KIRA-7
  • HY-12399
    MKC9989
    		Inhibitor 98.33%
    MKC9989 is a Hydroxy aryl aldehydes (HAA) inhibitor and also inhibits IRE1α with an IC50 of 0.23 to 44 μM.
    MKC9989
  • HY-18509
    IRE1α kinase-IN-2
    		Inhibitor 99.24%
    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-153773
    Z4P
    		Inhibitor 98.29%
    Z4P is a BBB-penetrable 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-155068
    FC-116
    		Inhibitor 98.04%
    FC-11 is a tubulin inhibitor. FC-116 inhibits the proliferation of colorectal cancer (CRC) cells, with IC50 values of 4.52 nM for HCT116 cells and 18.69 nM for CT26 cells. FC-11 can induce ER stress to generate excess ROS, leading to mitochondrial damage, thereby promoting apoptosis in colorectal cancer (CRC) cells by targeting microtubules. FC-116 exerts potent anti-tumor effects in vivo. FC-11 can be used for the study of colorectal cancer.
    FC-116
  • HY-107371
    6-Bromo-2-hydroxy-3-methoxybenzaldehyde
    		Inhibitor 99.96%
    6-Bromo-2-hydroxy-3-methoxybenzaldehyde (NSC95682) (Compound 3-5) is a selective and potent IRE-1α inhibitor with an IC50 value of 0.08 μM. 6-Bromo-2-hydroxy-3-methoxybenzaldehyde can be used for research on diseases associated with the unfolded protein response (UPR), such as cancer and autoimmune diseases.
    6-Bromo-2-hydroxy-3-methoxybenzaldehyde
  • HY-10255AS
    Sunitinib-d10
    		Inhibitor 99.89%
    Sunitinib-d10 (SU 11248-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 and PDGFRβ, respectively. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
    Sunitinib-d<sub>10</sub>
  • HY-178946
    IA107
    		Inhibitor 98.14%
    IA107 is a potent, selective, and allosteric IRE1α RNase (IC50 = 16 nM (non phosphorylated), IC50 = 9 nM (phosphorylated)) inhibitor. IA107 can inhibit endoplasmic reticulum stress-induced XBP1 mRNA splicing and protein expression, and has no cytotoxicity.
    IA107
  • HY-10255R
    Sunitinib Malate (Standard)
    		Inhibitor
    Sunitinib (Malate) (Standard) is the analytical standard of Sunitinib (Malate). This product is intended for research and analytical applications. 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 (Standard)
  • 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-114368A
    Kira8 Hydrochloride
    		Inhibitor 98.03%
    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-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-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-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-123996
    3-Ethoxy-5,6-dibromosalicylaldehyde
    		Inhibitor
    3-ethoxy-5,6-dibromosalicylaldehyde is a potent, non-competitive, selective IRE1 (including IRE1α) inhibitor (IC50s: ∼0.12 μM for hIRE1α-cyto; 6 μM for yeast Ire1). 3-ethoxy-5,6-dibromosalicylaldehyde inhibits XBP-1 splicing. 3-ethoxy-5,6-dibromosalicylaldehyde induces Apoptosis. 3-ethoxy-5,6-dibromosalicylaldehyde upregulates the mRNA expression level of TXNIP, while downregulating the expression level of TXN. 3-ethoxy-5,6-dibromosalicylaldehyde exhibits anticancer activity against pancreatic cancer. 3-ethoxy-5,6-dibromosalicylaldehyde significantly inhibits chikungunya virus replication.
    3-Ethoxy-5,6-dibromosalicylaldehyde
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity