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.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V77328 | 3,6-DMAD hydrochloride | 3,6-DMAD HCl is an acridine analogue and a potent inhibitor of the IRE1α-XBP1s pathway. | |
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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. |
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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. |
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V75796 | GSK2850163 (S enantiomer) | 2309519-81-9 | GSK2850163 S enantiomer is the inactive enantiomer of GSK2850163. |
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V52037 | GSK2850163 hydrochloride | 2319838-09-8 | GSK2850163 HCl is a novel inhibitor of myo-inositol-requiring enzyme-1α (IRE1α). |
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V75790 | IRE1α kinase-IN-1 | 2328097-41-0 | IRE1α kinase-IN-1 is a selective inhibitor of IRE1α (ERN1) with IC50 of 77 nM. |
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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. |
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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. |
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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. |
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V75793 | IRE1α kinase-IN-6 | 2715123-88-7 | IRE1α kinase-IN-6 is a potent inhibitor of IRE1α with IC50 of 4.4 nM. |
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V75795 | IRE1α kinase-IN-7 | 1414938-22-9 | IRE1α kinase-IN-7 (compound 4) is an IRE1α inhibitor. |
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V75788 | IRE1α kinase-IN-8 | 1338933-29-1 | IRE1α kinase-IN-8 is a benzoheterocyclic carboxaldehyde analogue and a potent inhibitor of IRE-1α. |
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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. |
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V3379 | IXA-4 | 1185329-96-7 | IXA4 is a selective, non-toxic activator of IRE1/XBP1s. |
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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. |
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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. |
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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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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. |
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V75791 | PAIR2 | 2771006-54-1 | PAIR2 is a potent and specific partial antagonist of IRE1α RNase. |
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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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