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

IRE1

Inositol requiring enzyme 1

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-N3000A
    6-Methoxydihydrosanguinarine hydrochloride
    Activator
    6-Methoxydihydrosanguinarine hydrochloride is an alkaloid with activity across multiple cancer cell types. 6-Methoxydihydrosanguinarine hydrochloride activates IRE1/JNK signaling, blocks Akt/mTOR and PI3K/AKT/mTOR pathways, reduces expression of Cdc25C, CyclinB1, Cdc2, YAP/TAZ, Survivin, GPX4, and EGFR, upregulates IRE1 and DR5, and activates JNK and caspases. 6-Methoxydihydrosanguinarine hydrochloride induces apoptosis, G2/M phase arrest, DNA damage, ROS generation, lipid peroxidation, ferroptosis, autophagy, and suppresses cancer cell growth. 6-Methoxydihydrosanguinarine hydrochloride disruptes the biofilm formation of Candida albicans (C. albicans). 6-Methoxydihydrosanguinarine hydrochloride can be used for the research of non-small cell lung cancer, hepatocellular carcinoma, melanoma, colon carcinoma, ovarian cancer and breast cancer.
    6-Methoxydihydrosanguinarine hydrochloride
  • 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-18903
    DSA8
    Modulator
    DSA8 is a type II kinase inhibitor with IRE1 RNase modulating activity. DSA8 can be used for the research of cancer, metabolic disease, suah as diabetes.
    DSA8
  • HY-U00459A
    GSK2850163 (S enantiomer)
    GSK2850163 S enantiomer is the inactive enantiomer of GSK2850163. GSK2850163 is an inositol-requiring enzyme-1 alpha (IRE1a) inhibitor.
    GSK2850163 (S enantiomer)
  • HY-W018161R
    Hexadecanedioic acid (Standard)
    Hexadecanedioic acid (Thapsic acid) (Standard) is the analytical standard of Hexadecanedioic acid (HY-W018161). This product is intended for research and analytical applications. Hexadecanedioic acid is an orally active metabolite produced by B. uniformis. Hexadecanedioic acid inhibits IRE1α-XBP1s-mediated flipogenesis and ferroptosis. Hexadecanedioic acid downregulates XBP1 and Hrd1 expression, activates the Nrf2/SLC7A11/GPX4 pathway. Hexadecanedioic acid can be used for the research of metabolic-associated fatty liver disease.
    Hexadecanedioic acid (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)
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity