Catalog No.
Product Name
Application
Product Information
Citations
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IRE1α inhibitor
MKC3946 is a potent and soluble IRE1α inhibitor, used for cancer research.- Shengji Li, .et al. , Cancer Gene Ther, 2025, Aug;32(8):884-898 PMID: 40634594
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IRE-1α inhibitor
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. -
IRE1 Rnase inhibitor
4μ8C is a potent and selective IRE1 Rnase inhibitor with IC50 of 76 nM.- Gideon Ong, .et al. , Cell Death Dis, 2024, Apr 18;15(4):276 PMID: 38637497
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IRE1α inhibitor
STF-083010 is a specific IRE1α inhibitor. STF-083010 inhibits Ire1 endonuclease activity, without affecting its kinase activity, after endoplasmic reticulum stress.- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
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mono-selective IRE1α inhibitor
Kira8 (AMG-18) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM. -
XBP1 inhibitor
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. -
IRE1α inhibitor
Kira8 Hydrochloride (AMG-18 Hydrochloride) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM. -
Endoplasmic Reticulum Stress Inhibitor
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. -
IRE1 Inhibitor
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. -
IRE1 Inhibitor
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. -
IRE1/XBP1s Activator
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. -
IRE1α Inhibitor
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. -
IRE1/XBP1s Activator
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 Inhibitor
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. -
IRE1α Inhibitor
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. -
IRE1α Inhibitor
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. -
IRE1/XBP1s Activator
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. -
IRE1 Inhibitor
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 Knase Inhibitor
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. -
IRE1α Inhibitor
PAIR2 is a selective inhibitor targeting the kinase domain of human IRE1α, exhibiting a Ki value of 8.8 nM. This compound effectively occupies the ATP-binding site, partially inhibiting IRE1α's ribonuclease activity while preserving Xbp1 mRNA splicing. PAIR2 also promotes the differentiation of B cells into plasma cells, prevents IRE1α-induced apoptosis, and restores Fgfr2 mRNA expression in AT2 cells. With its ability to reach steady-state concentrations in lung tissues of Mus musculus, PAIR2 is a valuable tool for exploring the role of the IRE1α signaling pathway in conditions such as pulmonary fibrosis. -
IRE1 Inhibitor
GSK2850163 hydrochloride is a selective inhibitor of inositol-requiring enzyme-1 alpha (IRE1α), effectively targeting its kinase and RNase activities, with IC50 values of 20 nM and 200 nM, respectively. This compound is instrumental in research focused on endoplasmic reticulum stress responses and the unfolded protein response, making it a valuable tool for studying various pathophysiological conditions, including cancer and neurodegenerative diseases. -
IRE1 Inhibitor
IRE1α kinase-IN-6 is a potent inhibitor of IRE1α, exhibiting an IC50 value of 4.4 nM. This compound effectively disrupts the activity of the inositol-requiring enzyme 1α, playing a critical role in the unfolded protein response. IRE1α kinase-IN-6 is utilized in research to study cellular stress responses, apoptosis, and various pathophysiological conditions associated with dysregulated protein homeostasis. -
IRE1α Inhibitor
IRE1α-IN-2 is a selective inhibitor of IRE1α, demonstrating an IC50 greater than 200 nM for the splicing of XBP1 mRNA. This compound plays a significant role in the study of the unfolded protein response and its implications in cancer research. It is valuable for elucidating the functions of IRE1α in cellular stress pathways and potential therapeutic interventions. -
IRE1α Inhibitor
IRE1a-IN-1 is a potent inhibitor of IRE1α, exhibiting an IC50 of less than 100 nM for XBP1 mRNA. This compound plays a significant role in the regulation of the unfolded protein response and is linked to cancer research. It is ideal for studies investigating the therapeutic potential of targeting IRE1α in various cancer types, providing insights into cellular stress responses and tumor biology. -
IRE1α Inhibitor
IRE1α kinase-IN-9 is a potent inhibitor of IRE1α, demonstrating an average IC50 value of less than 0.1 μM. This compound is valuable for investigating diseases linked to the unfolded protein response and regulated IRE1-dependent decay (RIDD). Its effectiveness in modulating IRE1α activity makes it a significant tool for research in cellular stress responses and related therapeutic applications. -
IRE1α Inhibitor
IRE1α kinase-IN-4 is a selective inhibitor of IRE1α, exhibiting a Ki of 140 nM. This compound acts as an ATP-competitive ligand, effectively blocking the kinase activity of IRE1α. Its biological activity makes it a valuable tool for research in cellular stress responses and the unfolded protein response pathway. -
IRE-1α Inhibitor
IRE1α kinase-IN-8 is a potent inhibitor of IRE-1α, a key regulator of the unfolded protein response. This compound is primarily utilized in research focused on diseases linked to endoplasmic reticulum stress and the regulation of IRE1-dependent decay (RIDD). Its application may provide valuable insights into therapeutic strategies for conditions associated with protein misfolding and cellular stress responses. -
IDE Inhibitor
BDM44768 is a selective inhibitor of insulin-degrading enzyme (IDE). This compound has been shown to exacerbate endoplasmic reticulum (ER) stress-induced IRE1 activation, leading to increased lipid accumulation in hepatocytes. BDM44768 serves as a valuable tool in research focused on metabolic disorders and liver function, particularly in models of ER stress and related lipid dysregulation. -
IRE1α Inhibitor
1ACTA is an inhibitor of IRE1α S-nitrosylation, effectively preserving the endoplasmic reticulum stress response during nitrosative stress conditions. This compound is essential for studying the regulatory mechanisms of the unfolded protein response (UPR) and its implications in cellular stress responses. It is widely utilized in research investigating pathways related to neurodegeneration, cancer, and metabolic disorders. -
IRE1α-XBP1s Inhibitor
3,6-DMAD dihydrochloride is a potent inhibitor of the IRE1α-XBP1s signaling pathway, specifically targeting IRE1α oligomerization and endoribonuclease (RNase) activity. This compound has been shown to promote IL-6 secretion, implicating its role in inflammatory responses. 3,6-DMAD dihydrochloride is a valuable tool for cancer research, particularly in studies focusing on cellular stress responses and their implications in tumor biology. -
IRE1α Inhibitor
IRE1α kinase-IN-5 is a potent inhibitor of IRE1α, with a Ki value of 98 nM. This ATP-competitive ligand disrupts the activity of IRE1α, a key mediator in the unfolded protein response pathway. Its inhibition of IRE1α activity supports research into cellular stress responses and potential therapeutic targets in diseases linked to dysregulated protein homeostasis. -
IRE1α Inhibitor
IRE1α kinase-IN-3 is a potent inhibitor of the inositol-requiring enzyme 1 alpha (IRE1α) with an inhibitory constant (Ki) of 480 nM. This compound acts as an ATP-competitive ligand, selectively targeting IRE1α to modulate its kinase activity. IRE1α kinase-IN-3 is valuable for studying the role of IRE1α in the unfolded protein response and related cellular processes, making it a useful tool for research in stress responses and related diseases. -
IRE1α Inhibitor
IRE1α kinase-IN-7 is a selective inhibitor of the IRE1α kinase. This compound is valuable for studying endoplasmic reticulum stress-related diseases, as it modulates the IRE1α signaling pathway. Research applications include investigating cellular responses to stress and potential therapeutic avenues in disorders linked to ER stress. -
IRE1α Kinase Inhibitor
IRE1α kinase-IN-10 is a specific inhibitor of the IRE1α kinase, a key regulator in the unfolded protein response and endoplasmic reticulum stress signaling pathways. This compound is designed for use in research focused on investigating endoplasmic reticulum stress-related diseases, providing insights into cellular stress responses and potential therapeutic strategies. Its application may enhance the understanding of IRE1α's role in various pathological conditions, including neurodegenerative diseases and metabolic disorders. -
IRE1 RNase Modulator
DSA8 is an IRE1 RNase modulator that functions as a type II kinase inhibitor. It is an effective tool for studying pathways involved in cancer and metabolic diseases, including diabetes. DSA8's ability to modulate IRE1 activity makes it valuable for investigating the unfolded protein response and its implications in various diseases. -
IRE1
GSK2850163 (S enantiomer) is an inactive enantiomer of GSK2850163, specifically targeting inositol-requiring enzyme-1 alpha (IRE1α). This compound serves as a valuable tool in research focused on the unfolded protein response and endoplasmic reticulum stress pathways. Investigating the activity of this enantiomer can provide insights into cellular mechanisms and potential therapeutic strategies in diseases characterized by dysregulated IRE1α signaling.
