IRE1

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.For many disorders connected to endoplasmic reticulum stress, it represents a possible therapeutic target.

IRE1 is the only identified ER stress sensor in yeast and essential for UPR in animals and plants.As an ER transmembrane protein, IRE1 controls UPR via a cytoplasmic kinase domain and an RNase domain and maintains ER homeostasis via an ER luminal stress-sensing domain. Through conformational change, autophosphorylation, and higher order oligomerization in response to ER stress, IRE1 RNase is activated. The unusual splicing of the transcription factor Xbp-1 or posttranscriptional alterations via Regulated IRE1-Dependent Decay (RIDD) of various substrates are two ways whereby mammalian IRE1 starts diverse downstream signals of the UPR.

IRE1 related products

Structure Cat No. Product Name CAS No. Product Description
V77328 3,6-DMAD hydrochloride
V1952 4μ8C (IRE1 Inhibitor III) 14003-96-4 4μ8C(also known as IRE1 Inhibitor III) is a potent and selective IRE1 Rnase inhibitor (IC50 = 76 nM) with the potential for metabolic diseases.
V3537 GSK2850163 2121989-91-9 GSK2850163 is a novel and potent 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.
V75796 GSK2850163 (S enantiomer) 2309519-81-9
V52037 GSK2850163 hydrochloride 2319838-09-8
V75790 IRE1α kinase-IN-1 2328097-41-0
V75789 IRE1α kinase-IN-2 1414938-21-8
V75797 IRE1α kinase-IN-4 2771006-45-0
V75792 IRE1α kinase-IN-5 2771006-47-2
V75793 IRE1α kinase-IN-6 2715123-88-7
V75795 IRE1α kinase-IN-7 1414938-22-9
V75788 IRE1α kinase-IN-8 1338933-29-1
V75794 IRE1α kinase-IN-9 1338933-30-4
V3379 IXA-4 1185329-96-7 IXA-4 is a highly selective, non-toxic IRE1/XBP1s activator.
V23244 KIRA6 1589527-65-0 KIRA6 (KIRA-6) is a novel, potent and ATP-competitive allosteric IRE1α inhibitor (IC50 of 0.6 µM) with anti-inflammatory and immune-modulating properties.
V32447 Kira8 (AMG-18) 1630086-20-2 Kira8 (AMG18; Kira-8; AMG-18) is a potent and allosteric inhibitor of IRE1α kinase-inhibiting rnase attenuator (kira) with antifibrotic effects.
V3985 MKC3946 1093119-54-0 MKC3946 (MKC-3946) is a potent and soluble IRE1α RNase inhibitor that has potential anticancer activity.
V5105 NSC95682 20035-41-0 NSC95682 (6-Bromo-2-hydroxy-3-methoxybenzaldehyde),extracted from patent WO 2008154484 A1, IRE-lα inhibitor compound 3-5, is a novel and potent IRE-1α inhibitor with an IC50of 0.08 μM.
V75791 PAIR2 2771006-54-1
V1900 STF-083010 307543-71-1 STF-083010 (formerly IRE1 Inhibitor I) is a novel and specific small-molecule inhibitor of IRE1α endonuclease.
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