Catalog No.
Product Name
Application
Product Information
Citations
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eIF4E Inhibitor
eIF4E-IN-4 is a selective inhibitor of eukaryotic initiation factor 4E (eIF4E), demonstrating a biochemical activity value of 95 nM. This compound effectively inhibits cap-dependent mRNA translation, exhibiting an IC50 value of 2.5 μM. eIF4E-IN-4 is valuable for research applications related to breast cancer, colon cancer, and head and neck cancer, providing insights into the role of eIF4E in malignancies. -
eIF4A Inhibitor
eIF4A3-IN-6 is a selective inhibitor of eukaryotic initiation factor 4A (eIF4A), specifically targeting eIF4AI and eIF4AII. This compound exhibits significant biological activity in disrupting eIF4A-mediated processes, making it a valuable tool for studying eIF4A-dependent diseases, particularly in cancer research. The potential applications of eIF4A3-IN-6 extend to elucidating the role of eIF4A in oncogenic mechanisms and therapeutic interventions. -
GCN2-targeting Agent
AMG-34 is a selective GCN2-targeting agent that exhibits an IC50 of 0.395 μM for GCN2, along with IC50 values of 0.010 μM for PERK, 1.07 μM for HR and PKR, and greater than 10 μM for other targets. This compound is instrumental in research focused on the cellular stress response and the role of GCN2 in regulating protein synthesis. Its inhibitory activity makes it a valuable tool for studies exploring the therapeutic potential of modulating the integrated stress response. -
MNK1/2 Inhibitor
MNK1/2-IN-7 is a selective inhibitor of MNK1 and MNK2, primarily targeting the MNK/eIF4E signaling pathway. This compound exhibits potent anticancer activity by effectively inhibiting the phosphorylation of eIF4E, which contributes to reduced cancer cell proliferation. Additionally, MNK1/2-IN-7 demonstrates favorable hERG safety profiles, making it a valuable tool for research applications in oncology, particularly in combination therapies with agents like Ibrutinib. -
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. -
SIRT1/2 Inhibitor
Sirt1/2-IN-1 is a selective inhibitor of SIRT1 and SIRT2, exhibiting IC50 values of 1.81 and 2.10 µg/mL, respectively, while also inhibiting SIRT3 with an IC50 of 20.5 µg/mL. This compound induces hyperacetylation of α-tubulin, with an IC50 of 32.05 µg/mL, demonstrating its potential for modulating protein acetylation. Sirt1/2-IN-1 is particularly relevant in cancer research, showcasing significant anticancer activity that supports its use in investigating therapeutic strategies targeting sirtuin pathways. -
HDAC Inhibitor
HDAC-IN-54 is a potent histone deacetylase (HDAC) inhibitor, exhibiting IC50 values of 25 nM for human HDAC1, 66 nM for HDAC2, 6.5 nM for HDAC3, and 281 nM for HDAC6. This compound effectively induces acetylation of α-tubulin and histone H3, promoting cancer cell apoptosis, particularly in synergy with cisplatin. HDAC-IN-54 is relevant for research applications in head and neck cancer, ovarian cancer, and tongue squamous cell carcinoma. -
Nucleoside Metabolite
(R)-b-Aminoisobutyric acid is a nucleoside metabolite that serves as an effective amino donor. It plays a significant role in various biochemical pathways, making it valuable for studies on amino acid metabolism and nucleoside synthesis. This compound can be used in research applications focused on metabolic disorders and the regulation of nucleoside levels within cells. -
Nucleoside Metabolite
3,4-Dihydroxyphenylpyruvic acid is a nucleoside metabolite that plays a crucial role in the biosynthesis of catecholamines. This compound exhibits antioxidant properties and is involved in the regulation of cellular stress responses. Its applications in research include studying metabolic disorders and neurodegenerative diseases, as well as investigating its potential therapeutic effects in various biological contexts. -
Ribonucleoside Analog
4-Thiouridine is a ribonucleoside analog that serves as a valuable tool in RNA analysis and mRNA labeling. It effectively inhibits rRNA synthesis, leading to a nucleolar stress response, which can be utilized to study cellular stress mechanisms and RNA processing pathways. This compound is essential for researchers investigating RNA dynamics and the regulation of gene expression. -
Oligonucleotide Enhancer
UNC10217938A is a 3-deazapteridine analog that functions as an oligonucleotide enhancer. It effectively modulates intracellular trafficking and promotes the release of oligonucleotides from endosomes, leading to enhanced biological activity. This compound is particularly useful in research applications involving the optimization of antisense and siRNA oligonucleotide efficacy. -
Adenine Nucleoside Analogue
N-6-Methyl-2-deoxyadenosine (m6dA) is an adenine nucleoside analogue that targets nuclear processes and DNA replication machinery. It functions as a multifaceted epigenetic regulator, influencing transcription, DNA damage response, cell cycle progression, transposon silencing, and nucleosome organization in both prokaryotic and eukaryotic systems. Additionally, m6dA plays a crucial role in mitochondrial epigenetic inheritance and is implicated in fear extinction memory in murine models. Dysregulated levels of N-6-Methyl-2-deoxyadenosine have been associated with various cancers, making it a valuable reagent for research into glioblastoma, triple-negative breast cancer, and conditioned fear responses. -
Queuine Precursor
preQ1 dihydrochloride is a modified guanine-derived nucleobase that serves as a precursor in the biosynthesis of queuine. This compound demonstrates a high-affinity interaction with the aptamer of the preQ1 riboswitch, making it valuable for research in RNA biology and gene regulation. Its unique properties support studies aimed at understanding nucleobase metabolism and the role of queuine in cellular processes. -
Mononucleotide
2'-Deoxyguanosine 5'-monophosphate disodium is a nucleotide analog targeting cellular processes associated with guanine. This mononucleotide serves as a key reactant in studies of self-assembly in solution and the nucleation and growth of G-quadruplex structures. In addition, it plays a role in nucleophilic trapping and reductive alkylation, making it valuable for research on oxidative stress and DNA synthesis. As a precursor to guanosine triphosphate (GTP), it is essential for various biochemical assays and applications in nucleic acid research. -
Purine Nucleoside Analog
4-Thiothymidine is a purine nucleoside analog that exhibits significant antitumor activity, particularly against indolent lymphoid malignancies. Its primary mechanisms include the inhibition of DNA synthesis and the induction of apoptosis, making it a valuable compound for cancer research. This analog is essential for studies focused on the development of targeted therapies and the understanding of cellular responses to nucleoside analogs in oncological contexts. -
Isonuclear Anhydride Derivative
N-Methylisatoic anhydride is an isonuclear anhydride derivative that serves as a highly selective reagent for 2'-OH acylation of RNA. This compound is conjugated with biotin and a disulfide linker, facilitating the capture of RNA from complex biological mixtures containing both RNA and DNA. Its unique properties make it a valuable tool in RNA manipulation and isolation for various research applications. -
Purine Nucleoside Analog
5-Bromouridine is a purine nucleoside analog that exhibits significant antitumor activity, particularly against indolent lymphoid malignancies. Its anticancer effects are primarily attributed to the inhibition of DNA synthesis and the induction of apoptosis. This compound is an important tool for research applications in cancer biology and therapeutic development. -
Nucleoside Analog
Bz-OMe-rA is a nucleoside analog that primarily targets cellular nucleoside metabolism. It exhibits potential biological activity as an inhibitor of nucleoside transporters and may influence RNA synthesis and processing. Bz-OMe-rA is utilized in research to study nucleoside analogs in therapeutic applications, including antiviral and anticancer strategies. -
Purine Nucleoside Analog
2'-Deoxy-2'-fluoro-5-iodouridine is a purine nucleoside analog that exhibits significant antitumor activity, particularly against indolent lymphoid malignancies. Its mechanism of action involves the inhibition of DNA synthesis and the induction of apoptosis, making it a valuable tool for cancer research. This compound is relevant in studies focused on cancer therapeutics and the development of novel treatment strategies targeting nucleoside metabolism. -
Cytidine Analog
2’-Fluoro-2’-deoxy-ara-C(Bz)-3’-phosphoramidite is a cytidine analog that inhibits DNA methyltransferases, thereby influencing gene expression and cellular metabolism. This compound demonstrates significant anti-metabolic and anti-tumor activities, making it a valuable tool in cancer research and epigenetic studies. Its unique structure allows for incorporation into nucleic acids, facilitating investigations into gene regulation and therapeutic development. -
Nucleoside Analog
5'(E)-VP-2'-OMe-U phosphoramidite is a nucleoside analog utilized as a monomer in oligonucleotide synthesis. This reagent is instrumental in generating modified nucleic acids, enabling the study of RNA structure and function. Its unique properties make it suitable for applications in biological research, including probe design and therapeutic development. -
Nucleoside Antimetabolite/Analog
2′-Deoxy-2′-fluoroadenosine is a fluorinated nucleoside analog that functions as an antimetabolite, displaying significant antitumor and antiviral properties. It disrupts DNA replication in cancer and viral cells upon incorporation, hindering their proliferation. This compound is particularly valuable for synthesizing 2′-Deoxy-2′-fluoro-modified oligonucleotides hybridized with RNA. Additionally, 2′-Deoxy-2′-fluoroadenosine can be converted by E. coli purine nucleoside phosphorylase (PNP) into the cytotoxic agent 2-fluoroadenine (FAde), demonstrating promising in vivo efficacy against tumors with E. coli PNP expression. -
Purine Nucleoside Analog
5-Methoxyuridine is a purine nucleoside analog that exhibits significant antitumor activity, particularly against indolent lymphoid malignancies. Its anticancer mechanisms primarily involve the inhibition of DNA synthesis and the induction of apoptosis, making it a valuable tool for cancer research. This compound can be utilized in studies focusing on nucleoside metabolism and the therapeutic potential of nucleoside analogs in oncology. -
Immunosuppressive Agent
6-Thioguanosine is a potent immunosuppressive agent and an active metabolite of Azathioprine. It functions by inhibiting nucleotide synthesis, leading to the suppression of lymphocyte proliferation. This compound is primarily utilized in research applications related to transplantation, autoimmune disorders, and cancer therapy, where modulation of the immune response is critical. -
Thymidine Phosphorylase Inhibitor
KIN59 (5’-O-Tritylinosine) is a potent allosteric inhibitor of thymidine phosphorylase, effectively impacting cellular proliferation. This compound demonstrates the ability to inhibit FGF2-stimulated cell growth and reduces the expression of phosphorylated FGFR1 and Akt in FGF2-stimulated cells. KIN59 showcases significant anti-tumor activity, making it valuable for research in cancer therapeutics and cell signaling pathways.
