IRE1

Cat. No.

A54714

CAS No.

2771006-54-1

PAIR2

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.

Cat. No.

A54715

CAS No.

2319838-09-8

GSK2850163 hydrochloride

Synonyms: GSK163 (hydrochloride)

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.

Cat. No.

A54716

CAS No.

2715123-88-7

IRE1α kinase-IN-6

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.

Cat. No.

A54717

CAS No.

3033375-24-2

IRE1a-IN-2

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.

Cat. No.

A54718

CAS No.

3033375-01-5

IRE1a-IN-1

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.

Cat. No.

A54719

CAS No.

1338933-30-4

IRE1α kinase-IN-9

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.

Cat. No.

A54720

CAS No.

2771006-45-0

IRE1α kinase-IN-4

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.

Cat. No.

A54721

CAS No.

1338933-29-1

IRE1α kinase-IN-8

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.

Cat. No.

A54722

CAS No.

2011754-00-8

BDM44768

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.

Cat. No.

A54723

CAS No.

2196076-49-8

1ACTA

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.

Cat. No.

A54724

CAS No.

2226511-77-7

3,6-DMAD dihydrochloride

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.

Cat. No.

A54725

CAS No.

2771006-47-2

IRE1α kinase-IN-5

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.

Cat. No.

A54726

CAS No.

2416223-41-9

IRE1α kinase-IN-3

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.

Cat. No.

A54727

CAS No.

1414938-22-9

IRE1α kinase-IN-7

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.

Cat. No.

A54728

CAS No.

1415050-59-7

IRE1α kinase-IN-10

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.

Cat. No.

A54729

CAS No.

1157857-37-8

DSA8

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.

Cat. No.

A54730

CAS No.

2309519-81-9

GSK2850163 (S enantiomer)

Synonyms: GSK163 (S enantiomer)

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.