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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V104881 | 1ACTA | 2196076-49-8 | 1ACTA is an IRE1α S-nitrosation inhibitor that maintains the ER stress response under nitrosative stress. |
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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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V110395 | 3-Ethoxy-5,6-dibromosalicylaldehyde | 20041-64-9 | 3-Ethoxy-5,6-dibromosalicylaldehyde is a potent, non-competitive, selective inhibitor of IRE1 (including IRE1α) (IC50: ~0.12 μM (hIRE1α-cyto); 6 μM (yeast Ire1)). |
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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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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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V111773 | DSA8 | 1157857-37-8 | DSA8 is a type II kinase inhibitor with IRE1 ribonuclease regulatory activity. |
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V88687 | G-5758 | 2413455-99-7 | G-5758 is an orally available IRE1α inhibitor with an IC50 of 38 nM for XBP1s. |
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V110361 | G1167 | G1167 is an IRE1 ligand that can be used to synthesize PROTACs, such as G6374. | |
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V110335 | G6374 | G6374 is an IRE1 PROTAC degrader with a DC50 value of 0.04 μM. | |
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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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V116496 | IA107 | IA107 is a potent, selective allosteric inhibitor of IRE1α RNase (IC50 = 16 nM (non-phosphorylated), IC50 = 9 nM (phosphorylated)). | |
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V88689 | IRE1a-IN-1 | 3033375-01-5 | IRE1a-IN-1 (Compound 10) is an IRE1α inhibitor with IC50 of less than 100 nM for XBP1 mRNA. |
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V88688 | IRE1a-IN-2 | 3033375-24-2 | IRE1a-IN-2 (Compound 30) is an IRE1α inhibitor with IC50 greater than 200 nM for XBP1 mRNA. |
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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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