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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
TQ0076 KIRA6 KIRA6 is an effective inhibitor of IRE1α RNase kinase (IC50: 0.6 µM). It can trigger an apoptotic response.
T0374L Sunitinib 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.
T11762L Kira8 Kira8 is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity (IC50: 5.9 nM).
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-kit.
T9349 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...
T17143 Toyocamycin 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...
T7483 6-Bromo-2-hydroxy-3-methoxybenzaldehyde 6-Bromo-2-hydroxy-3-methoxybenzaldehyde is an inhibitor of IRE-1α (IC50 : 0.08 μM).
T12071 MKC9989 MKC9989 is an inhibitor of Hydroxy aryl aldehydes (HAA). MKC9989 also inhibits IRE1α with an IC50 of 0.23 to 44 μM.
TQ0101 MKC3946 MKC3946 is an effective and soluble IRE1α inhibitor which triggered modest growth inhibition in multiple myeloma cell lines.
T3654 APY29 APY29 is an allosteric modulator of IRE1α; inhibits IRE1α autophosphorylation (IC50 = 280 nM) and activates IRE1α RNase activity.
T6363 4μ8C 4μ8C(IC50=76 nM) is an effective and specific IRE1 Rnase inhibitor.
T6681 STF-083010 STF-083010 is a selective inhibitor of the IRE1α endonuclease.
T15594 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...
KIRA6
TQ0076
KIRA6 is an effective inhibitor of IRE1α RNase kinase (IC50: 0.6 µM). It can trigger an apoptotic response.
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.
Kira8
T11762L
Kira8 is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity (IC50: 5.9 nM).
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.
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...
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). T...
6-Bromo-2-hydroxy-3-methoxybenzaldehyde
T7483
6-Bromo-2-hydroxy-3-methoxybenzaldehyde is an inhibitor of IRE-1α (IC50 : 0.08 μM).
MKC9989
T12071
MKC9989 is an inhibitor of Hydroxy aryl aldehydes (HAA). MKC9989 also inhibits IRE1α with an IC50 of 0.23 to 44 μM.
MKC3946
TQ0101
MKC3946 is an effective and soluble IRE1α inhibitor which triggered modest growth inhibition in multiple myeloma cell lines.
APY29
T3654
APY29 is an allosteric modulator of IRE1α; inhibits IRE1α autophosphorylation (IC50 = 280 nM) and activates IRE1α RNase activity.
4μ8C
T6363
4μ8C(IC50=76 nM) is an effective and specific IRE1 Rnase inhibitor.
STF-083010
T6681
STF-083010 is a selective inhibitor of the IRE1α endonuclease.
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 producti...