IRE1

Inositol-requiring enzyme 1 (IRE1) is a resident transmembrane ER protein with both kinase and endonuclease domains. Both yeast (IRE) and mammalian (IRE1α) homologs are involved in the degradation of misfolded proteins, as part of the unfolded protein response (UPR).

Products
Background
Literature
Gene Data

Inhibitors

Cat No Product Name / Activity
4479 4μ8C
Inhibits IRE1α endoribonuclease activity
6009 B I09
IRE1 endonuclease inhibitor; cell permeable
4509 STF 083010
Inhibits IRE1α endonuclease activity

Other

Cat No Product Name / Activity
1227 Apigenin
Protein kinase inhibitor; promotes IRE1 activity
4865 APY 29
Inhibits IRE1α autophosphorylation; activates IRE1α endoribonuclease activity
3603 Kaempferol
MCU activator; also promotes IRE1 activity
1125 Quercetin
Non-selective PI 3-kinase inhibitor; promotes IRE1 endonuclease activity

Inositol-requiring enzyme 1 (IRE1), also known as endoplasmic reticulum to nucleus signaling 1 (ERN1), is a resident transmembrane ER protein with both kinase and endonuclease domains. Both yeast (IRE1) and mammalian (IRE1α) homologs are involved in the degradation of misfolded proteins, as part of the unfolded protein response (UPR). IRE1 (yeast) is involved in the endonucleolytic cleavage of HAC1 mRNA, whereas IRE1α (human) catalyzes the splicing of X-box binding protein (XBP) 1 mRNA. XBP1 mRNA splicing triggers upregulation of genes involved in the ERAD pathway, induction of XBP1 expression and the synthesis of ER chaperones.

Under normal conditions, IRE1 is maintained in an inactive state due to the binding of B-cell immunoglobulin binding protein (BiP) to its luminal domain. However, the accumulation of unfolded proteins within the ER induces ER stress, causing BiP to detach from IRE1. Following BiP detachment, IRE1 undergoes dimerization and autophosphorylation through the actions of IRE1 kinase domains. Activation of IRE1 endonuclease and kinase domains may also occur by direct binding of unfolded proteins to IRE1.

Literature for IRE1

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New Product Guide (Spring/Summer 2017)

Our new product guide highlights over 130 new products added to the Tocris Bioscience range during the first half of 2017.

  • 7-TM Receptors
  • Enzymes
  • Enzyme-Linked Receptors
  • Ion Channels
  • Nuclear Receptors
  • Transporters
  • Apoptosis
  • Cell Metabolism
  • Epigenetics
  • Fluorescent Imaging
  • Signal Transduction
  • Stem Cells

IRE1 Gene Data

Species Gene Symbol Gene Accession No. Protein Accession No.
Human ERN1 NM_001433 O75460
Rat Ern1 NM_001191926 NP_001178855
Mouse Ern1 NM_023913 Q9EQY0