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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.
Cat. No. Product name CAS No. Purity Chemical Structure
T14847 B I09 1607803-67-7 98%
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 ...
TQ0101 MKC3946 1093119-54-0 98%
MKC3946 is an effective and soluble IRE1α inhibitor which triggered modest growth inhibition in multiple myeloma cell lines.
T9564 IRE1α kinase-IN-1 2328097-41-0 98%
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...
T6681 STF-083010 307543-71-1 98%
STF-083010 is a selective inhibitor of the IRE1α endonuclease.
T6363 4μ8C 14003-96-4 98%
4μ8C(IC50=76 nM) is an effective and specific IRE1 Rnase inhibitor.
T11488 GSK2850163 2121989-91-9 98%
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%
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%
Sunitinib, a multi-targeted RTK inhibitor, is targeting PDGFRβ and VEGFR2 (Flk-1) with IC50 of 2 nM and 80 nM and also inhibits c-Kit.
T0374 Sunitinib Malate 341031-54-7 98%
Sunitinib is an indolinone-based tyrosine kinase inhibitor. It blocks the tyrosine kinase activities of VEGFR2, PDGFRβ (IC50: 80/2 nM), and c-kit.
T17143 Toyocamycin 606-58-6 98%
Toyocamycin is an adenosine analog produced by Actinomycete, acts as an XBP1 inhibitor, inhibits IRE1α-induced ATP-dependent XBP1 mRNA cleavage (IC50: 80 nM). To...
T11762L Kira8 1630086-20-2 98%
Kira8 is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity (IC50: 5.9 nM).
T9349 IXA4 1185329-96-7 98%
IXA4 is a highly selective, nontoxic activator of IRE1/XBP1s and reduces APP secretion by activating IRE1. IXA4-stimulated IRE1 activation also enhanced pancreat...
T3654 APY29 1216665-49-4 98%
APY29 is an allosteric modulator of IRE1α; inhibits IRE1α autophosphorylation (IC50 = 280 nM) and activates IRE1α RNase activity.
TQ0076 KIRA6 1589527-65-0 98%
KIRA6 is an effective inhibitor of IRE1α RNase kinase (IC50: 0.6 µM). It can trigger an apoptotic response.
T12071 MKC9989 1338934-20-5 98%
MKC9989 is an inhibitor of Hydroxy aryl aldehydes (HAA). MKC9989 also inhibits IRE1α with an IC50 of 0.23 to 44 μM.
T7483 6-Bromo-2-hydroxy-3-methoxybenzaldehyde 20035-41-0 98%
6-Bromo-2-hydroxy-3-methoxybenzaldehyde is an inhibitor of IRE-1α (IC50 : 0.08 μM).
T15594 MKC8866 1338934-59-0 98%
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 ...
MKC3946
TQ0101
MKC3946 is an effective and soluble IRE1α inhibitor which triggered modest growth inhibition in multiple myeloma cell lines.
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...
STF-083010
T6681
STF-083010 is a selective inhibitor of the IRE1α endonuclease.
4μ8C
T6363
4μ8C(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, a multi-targeted RTK inhibitor, is targeting PDGFRβ and VEGFR2 (Flk-1) with IC50 of 2 nM and 80 nM and also inhibits c-Kit.
Sunitinib Malate
T0374
Sunitinib is an indolinone-based tyrosine kinase inhibitor. It blocks the tyrosine kinase activities of VEGFR2, PDGFRβ (IC50: 80/2 nM), and c-kit.
Toyocamycin
T17143
Toyocamycin is an adenosine analog produced by Actinomycete, acts as an XBP1 inhibitor, inhibits IRE1α-induced ATP-dependent XBP1 mRNA cleavage (IC50: 80 nM). To...
Kira8
T11762L
Kira8 is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity (IC50: 5.9 nM).
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...
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.
MKC9989
T12071
MKC9989 is an inhibitor of Hydroxy aryl aldehydes (HAA). MKC9989 also inhibits IRE1α with an IC50 of 0.23 to 44 μM.
6-Bromo-2-hydroxy-3-methoxybenzaldehyde
T7483
6-Bromo-2-hydroxy-3-methoxybenzaldehyde is an inhibitor of IRE-1α (IC50 : 0.08 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...