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-169939
    1ACTA
    		Inhibitor
    1ACTA is an IRE1α S-Nitrosylation inhibtor, maintaining the endoplasmic reticulum stress response under nitrosative stress.
    1ACTA
  • 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-173497
    IRE1-IN-2
    		Inhibitor
    IRE1-IN-2 (compound G15) is a potent IRE1 inhibitor. IRE1-IN-2 inhibits FFA-induced lipid accumulation with an IC50 of 2.06 μM.
    IRE1-IN-2
  • 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
  • HY-103248R
    Toyocamycin (Standard)
    		Inhibitor
    DL-Aspartic acid (Standard) is the analytical standard of DL-Aspartic acid. This product is intended for research and analytical applications. DL-Aspartic acid (DL-Asp-OH) is a kind of biological materials or organic compounds that are widely used in life science research.
    Toyocamycin (Standard)
  • HY-145418
    IRE1α kinase-IN-3
    		Inhibitor
    IRE1α kinase-IN-3 (compound 2) is a potent IRE1α inhibitor with an Ki of 480 nM. IRE1α kinase-IN-3 is the ATP-competitive ligands of IRE1α.
    IRE1α kinase-IN-3
  • HY-18510
    IRE1α kinase-IN-7
    		Inhibitor
    IRE1α kinase-IN-7 (compound 4) is an IRE1α kinase inhibitor. IRE1α kinase-IN-7 can be used for research of endoplasmic reticulum stress-related diseases.
    IRE1α kinase-IN-7
  • HY-169763
    D-F07
    		Inhibitor
    D-F07 is a prodrug with an aldehyde shielding group and an IRE-1 inhibitor that induces Apoptosis. D-F07 has antitumor activity.
    D-F07
  • HY-129348
    IRE1α kinase-IN-10
    		Inhibitor
    IRE1α kinase-IN-10 (GP29) is an IRE1α kinase inhibitor. IRE1α kinase-IN-10 can be used for the research of endoplasmic reticulum stress-related diseases.
    IRE1α kinase-IN-10
  • HY-107371R
    6-Bromo-2-hydroxy-3-methoxybenzaldehyde (Standard)
    		Inhibitor
    6-Bromo-2-hydroxy-3-methoxybenzaldehyde (Standard) (NSC95682 (Standard)) is the analytical standard of 6-Bromo-2-hydroxy-3-methoxybenzaldehyde (HY-107371). This product is intended for research and analytical applications. 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 (Standard)
  • HY-107400R
    B I09 (Standard)
    		Inhibitor
    B I09 (Standard) is the analytical standard of B I09 (HY-107400). This product is intended for research and analytical applications. B I09 is an IRE-1 RNase inhibitor, with an IC50 of 1230 nM.
    B I09 (Standard)
  • HY-10255AS1
    Sunitinib-d4
    		Inhibitor
    Sunitinib-d4 is the deuterium labeled Sunitinib. 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-d<sub>4</sub>
  • HY-104040R
    MKC8866 (Standard)
    		Inhibitor
    MKC8866 (Standard) is the analytical standard of MKC8866 (HY-104040). This product is intended for research and analytical applications. 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 (Standard)
  • HY-10255AR
    Sunitinib (Standard)
    		Inhibitor
    Sunitinib (Standard) is the analytical standard of Sunitinib. This product is intended for research and analytical applications. 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 (Standard)
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Cat. No. Product Name / Synonyms Application Reactivity