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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. 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.
Signaling Pathways | Target | TargetMol
Cat. No. Product name CAS No. Purity Chemical Structure
T62568 IXA6 1021106-40-0 98.63%
IXA6
IXA6 is a novel IRE1/XBP1s agonist with potential vasoprotective activity that activates IRE1-XBP1s signaling and XBP1s transcriptional response, which can be us...
T79062 IRE1α kinase-IN-8 1338933-29-1 98%
IRE1α kinase-IN-8
IRE1α kinase-IN-8, a benzoheterocyclecarboxaldehyde derivative, serves as a potent inhibitor of IRE-1α. This compound is utilized in research pertaining to disea...
T79063 IRE1α kinase-IN-9 1338933-30-4 98%
IRE1α kinase-IN-9
IRE1α kinase-IN-9 (compound 2) is a potent inhibitor of IRE-1α, demonstrating an average IC50 value of less than 0.1 μM. It is suitable for research into disease...
TQ0101 MKC3946 1093119-54-0 99.97%
MKC3946
MKC3946 is an effective and soluble IRE1α inhibitor which triggered modest growth inhibition in multiple myeloma cell lines.
T12071 MKC9989 1338934-20-5 99.52%
MKC9989
MKC9989 is an inhibitor of Hydroxy aryl aldehydes (HAA). MKC9989 also inhibits IRE1α with an IC50 of 0.23 to 44 μM.
T15594 MKC8866 1338934-59-0 99.28%
MKC8866
MKC8866 is a selective IRE1 RNase inhibitor (IC50: 0.29 μM in human vitro). MKC8866 inhibits IRE1 RNase in breast cancer cells leading to the decreased productio...
T14847 B I09 1607803-67-7 99.23%
B I09
B I09, an IRE-1 RNase inhibitor with an IC50 of 1230 nM, inhibits splicing of XBP1 mRNA in human WaC3 cells and expression of xbp-1 in LPS-stimulated B cells. B ...
T9564 IRE1α kinase-IN-1 2328097-41-0 99.18%
IRE1α kinase-IN-1
IRE1α kinase-IN-1 is a highly selective IRE1α (ERN1) inhibitor, with an IC50 of 77 nM. It displays 100-fold selectivity for IRE1α over the IRE1β isoform. It inhi...
T9349 IXA4 1185329-96-7 98.69%
IXA4
IXA4 is a highly selective, nontoxic activator of IRE1/XBP1s and reduces APP secretion by activating IRE1. IXA4-stimulated IRE1 activation also enhanced pancreat...
T6363 4μ8C 14003-96-4 98.61%
4μ8C
4μ8C (IRE1 Inhibitor III)(IC50=76 nM) is an effective and specific IRE1 Rnase inhibitor.
T11488 GSK2850163 2121989-91-9 98.44%
GSK2850163
GSK2850163 is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α) which can inhibit RNase activity and IRE1α kinase activity (IC50s: 200 and 20 nM).
T9848 GSK2850163 (S enantiomer) 2309519-81-9 98.40%
GSK2850163 (S enantiomer)
GSK2850163 (S enantiomer) is the inactive enantiomer of GSK2850163. GSK2850163 is an novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1a).
T0374L Sunitinib 557795-19-4 98.38%
Sunitinib
Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase (RTK) inhibitor that inhibits VEGFR2 and PDGFRβ (IC50=80/2 nM). Sunitinib has antitumor activit...
T0374 Sunitinib Malate 341031-54-7 98.23%
Sunitinib Malate
Sunitinib Malate (Sunitinib) is an indolinone-based tyrosine kinase inhibitor. It blocks the tyrosine kinase activities of VEGFR2, PDGFRβ (IC50: 80/2 nM), and c-...
T17143 Toyocamycin 606-58-6 98.17%
Toyocamycin
Toyocamycin (Vengicide) is an adenosine analog produced by Actinomycete, acts as an XBP1 inhibitor, inhibits IRE1α-induced ATP-dependent XBP1 mRNA cleavage (IC50...
T11762L Kira8 1630086-20-2 98.07%
Kira8
Kira8 (AMG-18) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity (IC50: 5.9 nM).
T7483 6-Bromo-2-hydroxy-3-methoxybenzaldehyde 20035-41-0 98%
6-Bromo-2-hydroxy-3-methoxybenzaldehyde
6-Bromo-2-hydroxy-3-methoxybenzaldehyde (NSC-95682) is an inhibitor of IRE-1α (IC50 : 0.08 μM).
T6681 STF-083010 307543-71-1 97.53%
STF-083010
STF-083010 is a selective inhibitor of the IRE1α endonuclease.
T3654 APY29 1216665-49-4 96.57%
APY29
APY29 is an allosteric modulator of IRE1α; inhibits IRE1α autophosphorylation (IC50 = 280 nM) and activates IRE1α RNase activity.
TQ0076 KIRA6 1589527-65-0 100%
KIRA6
KIRA6 is an effective inhibitor of IRE1α RNase kinase (IC50: 0.6 μM). It can trigger an apoptotic response.
IXA6
T62568
IXA6 is a novel IRE1/XBP1s agonist with potential vasoprotective activity that activates IRE1-XBP1s signaling and XBP1s transcriptional response, which can be us...
IRE1α kinase-IN-8
T79062
IRE1α kinase-IN-8, a benzoheterocyclecarboxaldehyde derivative, serves as a potent inhibitor of IRE-1α. This compound is utilized in research pertaining to disea...
IRE1α kinase-IN-9
T79063
IRE1α kinase-IN-9 (compound 2) is a potent inhibitor of IRE-1α, demonstrating an average IC50 value of less than 0.1 μM. It is suitable for research into disease...
MKC3946
TQ0101
MKC3946 is an effective and soluble IRE1α inhibitor which triggered modest growth inhibition in multiple myeloma cell lines.
MKC9989
T12071
MKC9989 is an inhibitor of Hydroxy aryl aldehydes (HAA). MKC9989 also inhibits IRE1α with an IC50 of 0.23 to 44 μM.
MKC8866
T15594
MKC8866 is a selective IRE1 RNase inhibitor (IC50: 0.29 μM in human vitro). MKC8866 inhibits IRE1 RNase in breast cancer cells leading to the decreased productio...
B I09
T14847
B I09, an IRE-1 RNase inhibitor with an IC50 of 1230 nM, inhibits splicing of XBP1 mRNA in human WaC3 cells and expression of xbp-1 in LPS-stimulated B cells. B ...
IRE1α kinase-IN-1
T9564
IRE1α kinase-IN-1 is a highly selective IRE1α (ERN1) inhibitor, with an IC50 of 77 nM. It displays 100-fold selectivity for IRE1α over the IRE1β isoform. It inhi...
IXA4
T9349
IXA4 is a highly selective, nontoxic activator of IRE1/XBP1s and reduces APP secretion by activating IRE1. IXA4-stimulated IRE1 activation also enhanced pancreat...
4μ8C
T6363
4μ8C (IRE1 Inhibitor III)(IC50=76 nM) is an effective and specific IRE1 Rnase inhibitor.
GSK2850163
T11488
GSK2850163 is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α) which can inhibit RNase activity and IRE1α kinase activity (IC50s: 200 and 20 nM).
GSK2850163 (S enantiomer)
T9848
GSK2850163 (S enantiomer) is the inactive enantiomer of GSK2850163. GSK2850163 is an novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1a).
Sunitinib
T0374L
Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase (RTK) inhibitor that inhibits VEGFR2 and PDGFRβ (IC50=80/2 nM). Sunitinib has antitumor activit...
Sunitinib Malate
T0374
Sunitinib Malate (Sunitinib) is an indolinone-based tyrosine kinase inhibitor. It blocks the tyrosine kinase activities of VEGFR2, PDGFRβ (IC50: 80/2 nM), and c-...
Toyocamycin
T17143
Toyocamycin (Vengicide) is an adenosine analog produced by Actinomycete, acts as an XBP1 inhibitor, inhibits IRE1α-induced ATP-dependent XBP1 mRNA cleavage (IC50...
Kira8
T11762L
Kira8 (AMG-18) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity (IC50: 5.9 nM).
6-Bromo-2-hydroxy-3-methoxybenzaldehyde
T7483
6-Bromo-2-hydroxy-3-methoxybenzaldehyde (NSC-95682) is an inhibitor of IRE-1α (IC50 : 0.08 μM).
STF-083010
T6681
STF-083010 is a selective inhibitor of the IRE1α endonuclease.
APY29
T3654
APY29 is an allosteric modulator of IRE1α; inhibits IRE1α autophosphorylation (IC50 = 280 nM) and activates IRE1α RNase activity.
KIRA6
TQ0076
KIRA6 is an effective inhibitor of IRE1α RNase kinase (IC50: 0.6 μM). It can trigger an apoptotic response.
TargetMol