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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
3,6-DMAD hydrochloride V77328 3,6-DMAD hydrochloride 3,6-DMAD HCl is an acridine analogue and a potent inhibitor of the IRE1α-XBP1s pathway.
4μ8C (IRE1 Inhibitor III) 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.
G-5758 V88687 G-5758 2413455-99-7 G-5758 is an orally available IRE1α inhibitor with an IC50 of 38 nM for XBP1s.
GSK2850163 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.
GSK2850163 (S enantiomer) V75796 GSK2850163 (S enantiomer) 2309519-81-9 GSK2850163 S enantiomer is the inactive enantiomer of GSK2850163.
GSK2850163 hydrochloride V52037 GSK2850163 hydrochloride 2319838-09-8 GSK2850163 HCl is a novel inhibitor of myo-inositol-requiring enzyme-1α (IRE1α).
IRE1a-IN-1 V88689 IRE1a-IN-1 IRE1a-IN-1 (Compound 10) is an IRE1α inhibitor with IC50 of less than 100 nM for XBP1 mRNA.
IRE1a-IN-2 V88688 IRE1a-IN-2 IRE1a-IN-2 (Compound 30) is an IRE1α inhibitor with IC50 greater than 200 nM for XBP1 mRNA.
IRE1α kinase-IN-1 V75790 IRE1α kinase-IN-1 2328097-41-0 IRE1α kinase-IN-1 is a selective inhibitor of IRE1α (ERN1) with IC50 of 77 nM.
IRE1α kinase-IN-2 V75789 IRE1α kinase-IN-2 1414938-21-8 IRE1α kinase-IN-2 is a potent IRE1α kinase inhibitor (antagonist) with EC50 of 0.82 μM.
IRE1α kinase-IN-4 V75797 IRE1α kinase-IN-4 2771006-45-0 IRE1α kinase-IN-4 (compound 6) is a potent inhibitor of IRE1α with Ki of 140 nM.
IRE1α kinase-IN-5 V75792 IRE1α kinase-IN-5 2771006-47-2 IRE1α kinase-IN-5 (compound 7) is a potent IRE1α inhibitor (antagonist) with Ki of 98 nM.
IRE1α kinase-IN-6 V75793 IRE1α kinase-IN-6 2715123-88-7 IRE1α kinase-IN-6 is a potent inhibitor of IRE1α with IC50 of 4.4 nM.
IRE1α kinase-IN-7 V75795 IRE1α kinase-IN-7 1414938-22-9 IRE1α kinase-IN-7 (compound 4) is an IRE1α inhibitor.
IRE1α kinase-IN-8 V75788 IRE1α kinase-IN-8 1338933-29-1 IRE1α kinase-IN-8 is a benzoheterocyclic carboxaldehyde analogue and a potent inhibitor of IRE-1α.
IRE1α kinase-IN-9 V75794 IRE1α kinase-IN-9 1338933-30-4 IRE1α kinase-IN-9 (compound 2) is a potent inhibitor of IRE-1α with average IC50 <0.1 μM.
IXA-4 V3379 IXA-4 1185329-96-7 IXA4 is a selective, non-toxic activator of IRE1/XBP1s.
KIRA6 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.
Kira8 (AMG-18) 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.
MKC3946 V3985 MKC3946 1093119-54-0 MKC3946 (MKC-3946) is a potent and soluble IRE1α RNase inhibitor that has potential anticancer activity.
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