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Home >> Signaling Pathways >> DNA Damage/DNA Repair >> IRE1

IRE1

The serine/threonine-protein kinase/endoribonuclease inositol-requiring enzyme 1 (IRE1) is an enzyme that in humans is encoded by the ERN1 gene. IRE1 is an endoplasmic reticulum (ER) transmembrane sensor that activates UPR to maintain ER and cellular function. While mammalian IRE1 promotes cell survive, it can initiate apoptosis via decay of anti-apoptotic microRNAs.

IRE1 activation is initiated by homotypic interactions of the stress-sensing lumenal domain favoring transautophosphorylation of the kinase-extension nuclease (KEN) domain on the cytoplasmic side of the ER membrane.

IRE1/XBP-1 has been shown to regulate a variety of genes in various cell types in response to ER stress, mostly related to ER function and the secretory pathway, although the target genes vary depending on the cell type and nature of the stress stimuli.

Targets for  IRE1

Products for  IRE1

  1. Cat.No. Product Name Information
  2. GC34384 3,6-DMAD hydrochloride 3,6-DMAD hydrochloride, an acridine derivative, is a potent IRE1α-XBP1s pathway inhibitor. 3,6-DMAD hydrochloride promotes IL-6 secretion via the IRE1α-XBP1s pathway. 3,6-DMAD hydrochloride inhibits IRE1α oligomerization and endoribonuclease (RNase) activity. 3,6-DMAD hydrochloride can be used for research of cancer. 3,6-DMAD hydrochloride Chemical Structure
  3. GC14493 4μ8C

    4u8C

    IRE1 Rnase inhibitor, potent and non-toxic

     4μ8C Chemical Structure
  4. GC50366 AMG 18 hydrochloride

    AMG-18 Hydrochloride

     AMG 18 hydrochloride (AMG-18 Hydrochloride) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM. AMG 18 hydrochloride Chemical Structure
  5. GC17139 APY29 IRE1α inhibitor APY29 Chemical Structure
  6. GC33406 B I09 B I09 is an IRE-1 RNase inhibitor, with an IC50 of 1230 nM. B I09 Chemical Structure
  7. GC32857 GSK2850163 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 Chemical Structure
  8. GC34205 GSK2850163 hydrochloride 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 Chemical Structure
  9. GC63513 IRE1α kinase-IN-1 IRE1α kinase-IN-1 is a highly selective IRE1α (ERN1) inhibitor, with an IC50 of 77 nM. IRE1α kinase-IN-1 Chemical Structure
  10. GC64232 IRE1α kinase-IN-2 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 Chemical Structure
  11. GC63785 IXA4 IXA4 is a highly selective, non-toxic IRE1/XBP1s activator that induces endoplasmic reticulum (ER) proteostasis remodeling. IXA4 Chemical Structure
  12. GC64238 KIRA-7 KIRA-7, an imidazopyrazine compound, binds the IRE1α kinase (IC50 of 110 nM) to allosterically inhibit its RNase activity. KIRA-7 Chemical Structure
  13. GC19212 KIRA6

    IRE1 Inhibitor IV, IRE1α Kinase Inhibiting RNase Attenuator 6

     KIRA6 allosterically inhibits IRE1α RNase kinase activity with an IC50 of 0.6 uM. KIRA6 Chemical Structure
  14. GC31879 Kira8

    AMG-18

    Kira8 (AMG-18) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM.

     Kira8 Chemical Structure
  15. GC18303 MKC-3946 MKC-3946 is an inhibitor of inositol-requiring enzyme 1α (IRE1α). MKC-3946 Chemical Structure
  16. GC32889 MKC8866 (IRE-1α inhibitor 1)

    Orin1001

     MKC8866 (IRE-1α inhibitor 1), a salicylaldehyde analog, is a potent, selective IRE1 RNase inhibitor with an IC50 of 0.29μM in human vitro. MKC8866 (IRE-1α inhibitor 1) strongly inhibits Dithiothreitol-induced X-box-binding protein 1-spliced (XBP1s) expression with an EC50 of 0.52μM and unstresses RPMI 8226 cells with an IC50 of 0.14μM. MKC8866 (IRE-1α inhibitor 1) 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 (IRE-1α inhibitor 1) Chemical Structure
  17. GC32910 MKC9989 MKC9989 is a Hydroxy aryl aldehydes (HAA) inhibitor and also inhibits IRE1α with an IC50 of 0.23 to 44 μM. MKC9989 Chemical Structure
  18. GC34111 NSC95682 (6-Bromo-2-hydroxy-3-methoxybenzaldehyde) NSC95682 (6-Bromo-2-hydroxy-3-methoxybenzaldehyde) (NSC95682) is an IRE-1α inhibitor with an IC50 of 0.08 μM, extracted from patent WO 2008154484 A1, IRE-lα inhibitor compound 3-5. NSC95682 (6-Bromo-2-hydroxy-3-methoxybenzaldehyde) Chemical Structure
  19. GC12937 STF 083010

    IRE1 Inhibitor I

     IRE1α endonuclease inhibitor STF 083010 Chemical Structure
  20. GC17651 Sunitinib Sunitinib (SU 11248) is an orally active multi-target receptor tyrosine kinase inhibitor with IC50 values of 80 nM and 2 nM for vascular endothelial growth factor receptor (VEGFR2) and platelet-derived growth factor receptor (PDGFRβ), respectively. Sunitinib Chemical Structure
  21. GC14683 Sunitinib malate

    SU 11248,SU11248,SU-11248,Sunitinib

     A multi-kinase inhibitor Sunitinib malate Chemical Structure
  22. GC48118 Sunitinib-d10 An internal standard for the quantification of sunitinib Sunitinib-d10 Chemical Structure
  23. GC11805 Toyocamycin Toyocamycin is an adenosine analog and an inhibitor of XBP1. Toyocamycin Chemical Structure
  24. GC73484 Z4P Z4P is a BBB-permeable IRE1 inhibitor (IC50: 1.11 μM). Z4P Chemical Structure

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