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IRE1 inhibitors block inositol-requiring enzyme 1 (IRE1), a sensor of endoplasmic reticulum stress. In 1993, yeast IRE1 was identified as a transmembrane protein kinase required to induce genes for endoplasmic reticulum resident proteins. The enzyme couples a cytosolic kinase domain to an endoribonuclease (RNase) domain. Studies in 2001 and 2002 showed that IRE1 splices X-box binding protein 1 (XBP1) mRNA, producing an active transcription factor of the unfolded protein response. 4μ8C, STF-083010 and MKC8866 inhibit the RNase activity of IRE1α. KIRA6 and Kira8 bind the kinase site and suppress RNase activity allosterically, whereas APY29 is an ATP-competitive ligand of the kinase domain.
MKC3946 is a potent and soluble IRE1α inhibitor, used for cancer research.
STF-083010 is a specific IRE1α inhibitor. STF-083010 inhibits Ire1 endonuclease activity, without affecting its kinase activity, after endoplasmic reticulum stress.
KIRA6 is an advanced small-molecule IRE1α RNase kinase inhibitor with an IC50 of 0.6 µM. KIRA6 can trigger an apoptotic response.
Synonyms: NSC95682
6-Bromo-2-hydroxy-3-methoxybenzaldehyde (NSC95682) is an IRE-1α inhibitor with an IC50 of 0.08 μM, extracted from patent WO 2008154484 A1, IRE-lα inhibitor compound 3-5.
APY29 inhibits IRE1α autophosphorylation (IC50 = 280 nM) and activates IRE1α RNase activity.
Synonyms: AMG 18
Kira8 (AMG-18) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM.
Synonyms: Vengicide
Toyocamycin (Vengicide) is an adenosine analog produced by Actinomycete, acts as an XBP1 inhibitor, inhibits IRE1α-induced ATP-dependent XBP1 mRNA cleavage, with an IC50 of 80 nM.
Synonyms: IRE1-IN-8866
MKC8866, a salicylaldehyde analog, is a potent, selective IRE1 RNase inhibitor with an IC50 of 0.29 μM in human vitro.
B I09 is an IRE-1 RNase inhibitor, with an IC50 of 1230 nM.
MKC9989 is a Hydroxy aryl aldehydes (HAA) inhibitor and also inhibits IRE1α with an IC50 of 0.23 to 44 μM.
Synonyms: AMG-18 Hydrochloride; AMG18; Kira-8
Kira8 Hydrochloride (AMG-18 Hydrochloride) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM.
Synonyms: Tauroursodeoxycholic acid dihydrate; TUDCA dihydrate; UR 906 dihydrate
Tauroursodeoxycholate (Tauroursodeoxycholic acid; TDUCA) dihydrate is an inhibitor of endoplasmic reticulum (ER) stress that significantly downregulates pro-apoptotic molecules, including caspase-3 and caspase-12. Additionally, it suppresses ERK signaling, contributing to its cytoprotective and anti-apoptotic effects.
KIRA9 is a selective inhibitor of IRE1α, exhibiting an IC50 of 4.8 μM in INS-1 cells. By occupying the ATP-binding site, KIRA9 effectively disrupts endoplasmic reticulum (ER)-localized mRNA decay and inhibits apoptosis associated with ER stress. This compound serves as a valuable tool for studying the unfolded protein response and its implications in various cellular stress-related diseases.
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3-Ethoxy-5,6-dibromosalicylaldehyde is a selective non-competitive inhibitor of IRE1, including IRE1α, with an IC50 of approximately 0.12 μM for human IRE1α-cyto. This compound effectively inhibits XBP-1 splicing and induces apoptosis in various cellular contexts. It has been shown to upregulate TXNIP mRNA expression while downregulating TXN expression levels. Additionally, 3-ethoxy-5,6-dibromosalicylaldehyde exhibits promising anticancer activity against pancreatic cancer and significantly inhibits the replication of chikungunya virus, making it a valuable tool for research in apoptosis and viral biology.
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D-F07 is an IRE-1 inhibitor that functions as a prodrug with an aldehyde shielding group. It induces apoptosis and exhibits significant antitumor activity. D-F07 is valuable for research applications investigating cellular stress responses and apoptotic pathways in cancer models.
IXA4 is a selective activator of the IRE1/XBP1s signaling pathway. It uniquely stimulates IRE1/XBP1s activation without inducing a global unfolded protein response or engaging other stress-responsive signaling mechanisms, such as the heat shock or oxidative stress responses. IXA4 has been shown to effectively reduce the secretion of amyloid precursor protein (APP), making it a valuable tool for studies aimed at understanding protein homeostasis and cellular stress responses.
Synonyms: GSK163
GSK2850163 is a selective inhibitor of inositol-requiring enzyme-1 alpha (IRE1α), effectively blocking both IRE1α kinase and RNase activities with IC50 values of 20 nM and 200 nM, respectively. This compound is a valuable tool in research focusing on the unfolded protein response and its associated cellular stress pathways. GSK2850163 has potential applications in the study of various diseases, including cancer and neurodegenerative disorders, where IRE1α activity plays a critical role.
IXA6 is a specific activator of IRE1, leading to the activation of XBP1s through the induction of IRE1 RNase activity. This compound plays a crucial role in regulating the unfolded protein response (UPR) and enhancing ER stress signaling pathways. IXA6 is valuable for research into cellular stress responses, protein folding mechanisms, and potential therapeutic interventions in diseases linked to ER dysfunction.
IRE1α kinase-IN-1 is a selective inhibitor of IRE1α (ERN1), exhibiting an IC50 of 77 nM. It demonstrates a remarkable 100-fold selectivity for IRE1α over the IRE1β isoform. This compound effectively inhibits ER stress-induced oligomerization and autophosphorylation of IRE1α, as well as its RNase activity with an IC50 of 80 nM. IRE1α kinase-IN-1 is valuable for research applications related to ER stress and associated signaling pathways.
G-5758 is a selective inhibitor of IRE1α, demonstrating an IC50 of 38 nM as determined by the XBP1s luciferase reporter cell assay. This compound exhibits good tolerability in vivo, remaining effective in rats at oral dosages up to 500 mg/kg. G-5758 is useful for research applications related to multiple myeloma, providing insights into the cellular stress response and potential therapeutic avenues for hematologic malignancies.
KIRA-7 is an imidazopyrazine compound that functions as an allosteric inhibitor of IRE1α kinase, exhibiting an IC50 of 110 nM. By inhibiting the RNase activity of IRE1α, KIRA-7 demonstrates significant anti-fibrotic effects. This reagent is valuable for research focusing on cellular stress responses and the unfolded protein response.
IXA62 is an orally active and selective activator of IRE1/XBP1s, exhibiting an EC50 value of 0.31 μM. This compound is shown to reduce Aβ secretion, making it a potential candidate for research into Alzheimer's disease pathology. Additionally, IXA62 enhances glucose-stimulated insulin secretion in rat insulinoma cells, highlighting its applicability in studies of glucose metabolism and diabetes research.
Z4P is a potent inhibitor of IRE1, exhibiting an IC50 of 1.13 μM and capable of penetrating the blood-brain barrier. This compound demonstrates significant anti-tumor activity and, when used in combination with Temozolomide, effectively inhibits glioblastoma growth and recurrence. Z4P serves as a valuable tool in cancer research, particularly in studies focused on targeting the unfolded protein response in tumor cells.
IRE1α kinase-IN-2 is a selective inhibitor of IRE1α kinase, exhibiting an EC50 of 0.82 μM and an IC50 for autophosphorylation of 3.12 μM. This compound effectively inhibits XBP1 mRNA splicing in wild-type cell lines, making it a valuable tool for investigating the unfolded protein response and endoplasmic reticulum stress pathways. It is suited for research applications focusing on cellular stress responses and therapeutic strategies targeting related diseases.
