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IRE1

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.

  • 4μ8C
    T636314003-96-4
    4μ8C (IRE1 Inhibitor III)(IC50=76 nM) is an effective and specific IRE1 Rnase inhibitor.
    • $43
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  • GSK2850163 (S enantiomer)
    T98482309519-81-9In house
    GSK2850163 (S enantiomer) is the inactive enantiomer of GSK2850163. GSK2850163 is an novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1a).
    • $117
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  • B I09
    T148471607803-67-7In house
    B I09, an IRE-1 RNase inhibitor with an IC50 of 1230 nM, inhibits splicing of XBP1 mRNA in human WaC3 cells and expression of xbp-1 in LPS-stimulated B cells. B I09 can be used to simulate the defects of XBP-1 in CLL cells., an IRE-1 RNase inhibitor with an IC50 of 1230 nM, inhibits splicing of XBP1 mRNA in human WaC3 cells and expression of xbp-1 in LPS-stimulated B cells. B I09 can be used to simulate the defects of XBP-1 in CLL cells., an IRE-1 RNase inhibitor with an IC50 of 1230 nM, inhibits splicing of XBP1 mRNA in human WaC3 cells and expression of xbp-1 in LPS-stimulated B cells. B I09 can be used to simulate the defects of XBP-1 in CLL cells.
    • $44
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  • GSK2850163
    T114882121989-91-9In house
    GSK2850163 is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α) which can inhibit RNase activity and IRE1α kinase activity (IC50s: 200 and 20 nM).
    • $64
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  • APY29
    T36541216665-49-4
    APY29 is an allosteric modulator of IRE1α; inhibits IRE1α autophosphorylation (IC50 = 280 nM) and activates IRE1α RNase activity.
    • $36
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  • STF-083010
    T6681307543-71-1
    STF-083010 is a selective inhibitor of the IRE1α endonuclease.
    • $47
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  • KIRA6
    TQ00761589527-65-0
    KIRA6 is an effective inhibitor of IRE1α RNase kinase (IC50: 0.6 μM). It can trigger an apoptotic response.
    • $39
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  • Sunitinib
    T0374L557795-19-4
    Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase (RTK) inhibitor that inhibits VEGFR2 and PDGFRβ (IC50=80/2 nM). Sunitinib has antitumor activity and can be used for the treatment of kidney cancer and gastrointestinal tumors.
    • $53
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  • MKC9989
    T120711338934-20-5
    MKC9989 is an inhibitor of Hydroxy aryl aldehydes (HAA). MKC9989 also inhibits IRE1α with an IC50 of 0.23 to 44 μM.
    • $79
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  • Sunitinib Malate
    T0374341031-54-7
    Sunitinib Malate (Sunitinib) is an indolinone-based tyrosine kinase inhibitor. It blocks the tyrosine kinase activities of VEGFR2, PDGFRβ (IC50: 80/2 nM), and c-kit.
    • $37
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  • IRE1α kinase-IN-1
    T95642328097-41-0
    IRE1α kinase-IN-1 is a highly selective IRE1α (ERN1) inhibitor, with an IC50 of 77 nM. It displays 100-fold selectivity for IRE1α over the IRE1β isoform. It inhibits ER stress-induced IRE1α oligomerization and autophosphorylation, and also inhibits IRE1α RNase activity (IC50=80 nM)
    • $147
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  • 6-Bromo-2-hydroxy-3-methoxybenzaldehyde
    T748320035-41-0
    6-Bromo-2-hydroxy-3-methoxybenzaldehyde (NSC-95682) is an inhibitor of IRE-1α (IC50 : 0.08 μM).
    • $39
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  • Toyocamycin
    T17143606-58-6
    Toyocamycin (Vengicide) is an adenosine analog produced by Actinomycete, acts as an XBP1 inhibitor, inhibits IRE1α-induced ATP-dependent XBP1 mRNA cleavage (IC50: 80 nM). Toyocamycin induces apoptosis.
    • $39
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  • IRE1α kinase-IN-9
    T790631338933-30-4
    IRE1α kinase-IN-9 (compound 2) is a potent inhibitor of IRE-1α, demonstrating an average IC50 value of less than 0.1 μM. It is suitable for research into diseases linked to the unfolded protein response or regulated IRE1-dependent decay (RIDD) [1].
    • $1,520
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  • IXA6
    T625681021106-40-0
    IXA6 is a novel IRE1/XBP1s agonist with potential vasoprotective activity that activates IRE1-XBP1s signaling and XBP1s transcriptional response, which can be used to study neurodegenerative diseases such as Parkinson's disease and Alzheimer's disease.
    • $299
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  • IXA4
    T93491185329-96-7
    IXA4 is a highly selective, nontoxic activator of IRE1/XBP1s and reduces APP secretion by activating IRE1. IXA4-stimulated IRE1 activation also enhanced pancreatic function.
    • $34
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  • MKC8866
    T155941338934-59-0
    MKC8866 is a selective IRE1 RNase inhibitor (IC50: 0.29 μM in human vitro). MKC8866 inhibits IRE1 RNase in breast cancer cells leading to the decreased production of pro-tumorigenic factors and it can inhibit prostate cancer (PCa) tumor growth.
    • $80
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  • IRE1α kinase-IN-8
    T790621338933-29-1
    IRE1α kinase-IN-8, a benzoheterocyclecarboxaldehyde derivative, serves as a potent inhibitor of IRE-1α. This compound is utilized in research pertaining to diseases linked to the unfolded protein response and regulated IRE1-dependent decay (RIDD) [1].
    • $1,520
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  • Kira8
    T11762L1630086-20-2
    Kira8 (AMG-18) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity (IC50: 5.9 nM).
    • $89
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  • MKC3946
    TQ01011093119-54-0
    MKC3946 is an effective and soluble IRE1α inhibitor which triggered modest growth inhibition in multiple myeloma cell lines.
    • $61
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