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Catalog No.
Product Name
Application
Product Information
Citations
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HCV NS5B Polymerase Inhibitor
HCV NS5B polymerase-IN-3 is a potent inhibitor of the hepatitis C virus (HCV) NS5B polymerase, demonstrating significant antiviral activity. In the Huh7 replicon cell line, it exhibits an EC50 value of 0.23 μM while maintaining a favorable cytotoxicity profile. This compound is relevant for research applications focused on HCV replication and drug development strategies targeting hepatitis C. -
HCV Polymerase Inhibitor
VCH-916 free base is a non-nucleoside inhibitor targeting the NS5B polymerase of Hepatitis C virus (HCV). This compound demonstrates potent antiviral activity, making it a valuable tool for research on HCV replication. It is primarily utilized in studies focused on developing effective treatments for Hepatitis C and understanding the viral mechanisms of polymerase function. -
DNA Gyrase/Topoisomerase IV Inhibitor
Topoisomerase Inhibitor 6 is a dual irreversible inhibitor targeting DNA gyrase and topoisomerase IV, demonstrating a minimum inhibitory concentration (MIC) of 0.06 μg/mL against fluoroquinolone-resistant Staphylococcus aureus. This compound functions by obstructing the DNA strand break-reunion process, thereby causing lethal DNA damage. It holds potential for the study of Gram-positive bacterial infections, including those caused by S. aureus and Streptococcus pneumoniae. -
Topoisomerase II Inhibitor
NBTI 5463 is an inhibitor of bacterial type II topoisomerases, specifically targeting topoisomerase II. This compound exhibits potent antibacterial activity by inhibiting GyrA and TopoIV in Pseudomonas aeruginosa and Escherichia coli. By binding to topoisomerase II, NBTI 5463 disrupts DNA cleavage and religation, thereby obstructing bacterial DNA replication and transcription. This compound holds promise for advancing research on Gram-negative bacterial infections. -
Topoisomerase II Inhibitor
(-)-BO 2367 is a potent topoisomerase II inhibitor, exhibiting significant antibacterial and antitumor properties. It demonstrates IC50 values of 3.8 μM against the DNA relaxation activity of L1210 topoisomerase II and 0.5 μM and 1 μM against the supercoiling activities of Escherichia coli and Micrococcus luteus gyrases, respectively. This compound is valuable for research applications in cancer biology and microbial resistance studies, facilitating further exploration of therapeutic interventions. -
Adenylate Cyclase Inhibitor
MANT-GppNHp is a competitive inhibitor of adenylate cyclase (AC) that serves as a fluorescently labeled GTP analogue. It specifically interacts with the hydrophobic pocket adjacent to the AC catalytic site through its MANT group, effectively obstructing the binding of ATP. This compound is valuable for investigating diseases characterized by elevated AC activity, such as cholera, and offers insights into cellular signaling pathways. -
PNP Inhibitor
Immucillin-G is a potent inhibitor of purine nucleoside phosphorylase (PNP), a key enzyme in purine metabolism. By inhibiting PNP, Immucillin-G effectively reduces urate levels, making it valuable for research into metabolic disorders, particularly hyperuricemia. Its role in modulating purine metabolism provides significant insights for studies related to gout and metabolic diseases. -
Cytosolic Thymidine Kinase/Mitochondrial Enzyme Inhibitor
Ap5dT is an inhibitor of cytosolic thymidine kinase and mitochondrial enzymes, exhibiting inhibition constants (Kis) of 0.12 μM and 0.50 μM, respectively. This compound is relevant for research on acute myelocytic leukemia, facilitating investigations into thymidine metabolism and its implications in cancer biology. Its selective inhibition properties make Ap5dT a valuable tool for studying metabolic pathways involved in cellular proliferation. -
Guanylate Kinases Inhibitor
Guanosine 3',5'-bisdiphosphate (ppGpp) acts as a specific inhibitor of guanylate kinases, affecting GTP biosynthesis in chloroplasts. By inhibiting plastid and mitochondrial guanylate kinase activity, ppGpp is crucial for understanding metabolic regulation and signaling processes in plant systems. This reagent is valuable for research applications involving nucleotide metabolism and signaling pathways. -
eIF4E Inhibitor
eIF4E-IN-1 is a potent inhibitor of the eIF4E protein, which plays a critical role in regulating protein synthesis and cell proliferation. This compound effectively targets and inhibits immunosuppressive components, including immune checkpoint proteins such as PD-1, PD-L1, LAG3, TIM3, and IDO. eIF4E-IN-1 demonstrates promising biological activity in the modulation of immune responses, making it a valuable tool for research applications in cancer and infectious disease therapies. -
MNK1/MNK2 Inhibitor
HD202A is a selective dual inhibitor of MNK1 and MNK2, exhibiting IC50 values of 6.09 nM and 8.06 nM, respectively. This compound effectively inhibits the MNK-eIF4E signaling pathway, leading to downregulation of perilipin 2 and SCD1, while upregulating adipose triglyceride lipase and PPARγ coactivator 1α. HD202A enhances mitochondrial fatty acid oxidation, redox homeostasis, and demonstrates significant effects on metabolic health, including suppression of body weight gain, reduction in hepatic lipid accumulation, and improvement in glucose tolerance and insulin sensitivity. These properties make HD202A a valuable tool for researching metabolic dysfunction-associated steatotic liver disease. -
eIF4A Inhibitor
eIF4A-IN-1 is a selective inhibitor of eIF4A, a key protein involved in the regulation of mRNA translation. This compound effectively reduces protein synthesis in cancer cells by disrupting the initiation of translation, thereby providing a valuable tool for investigating tumor biology. eIF4A-IN-1 is applicable in studies focused on cancer therapeutics and understanding the mechanisms of tumorigenesis. -
eIF4A Inhibitor
eIF4A3-IN-5 is a potent inhibitor of eukaryotic initiation factor 4A (eIF4A), specifically targeting eIF4AI and eIF4AII. This compound demonstrates significant potential for investigating eIF4A-dependent diseases, particularly in the context of cancer research. Its ability to modulate eIF4A activity makes it a valuable tool for studying mechanisms of protein synthesis and their implications in tumorigenesis. -
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. -
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. -
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. -
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 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. -
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. -
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. -
D-DT Inhibitor
RGB097 is a potent inhibitor of D-dopachrome tautomerase (D-DT), demonstrating an IC50 value of 0.5 µM. This compound exhibits significant biological activity and has potential applications in cancer research, particularly in elucidating the role of D-DT in oncogenesis and tumor progression. -
MIF Inhibitor
MIF-IN-5 is a potent and reversible inhibitor of macrophage migration inhibitory factor (MIF), exhibiting a competitive mechanism of action. With an IC50 of 4.8 μM and a Ki value of 3.3 μM, it effectively disrupts MIF's biological activity. This compound is valuable for research applications involving inflammation, immune response modulation, and potential therapeutic strategies targeting various diseases associated with MIF dysregulation. -
MIF Inhibitor
HTS05585 is a selective inhibitor of macrophage migration inhibitory factor (MIF), demonstrating a Kd value of 0.29 μM via microscale thermophoresis and 0.32±0.01 μM confirmed by isothermal titration calorimetry. This compound effectively inhibits the release of pro-inflammatory cytokines, including TNF-α, IL-6, and IL-1β, from LPS-stimulated macrophages. HTS05585 is a valuable tool for studying inflammation-related diseases, particularly in the context of sepsis research. -
MIF tautomerase Inhibitor
TE-11 is a potent MIF tautomerase inhibitor, exhibiting an IC50 value of 5.63 μM. This compound effectively ameliorates CD-like colitis and reduces migration of MIF-induced eosinophils and neutrophils. Additionally, TE-11 prevents M1 polarization and the associated metabolic reprogramming, making it a valuable tool for research in inflammatory and autoimmune disorders. -
HDAC Inhibitor
2-Propylpent-4-ynoic acid, a histone deacetylase (HDAC) inhibitor, exhibits an IC50 of 0.5 mM against human HDAC. This compound induces P-glycoprotein function and has been associated with teratogenicity, fetal growth inhibition, and neurotoxicity. Notably, the S-enantiomer demonstrates more significant teratogenic effects compared to its R-enantiomer and other analogs. 2-Propylpent-4-ynoic acid is relevant in research focused on the mechanisms underlying colon cancer and neural tube defects, including exencephaly. -
PARP-1 Inhibitor
L-2286 is a potent orally active inhibitor of PARP-1. This compound demonstrates significant biological activity by alleviating carotid artery remodeling, reducing oxidative stress and inflammation in spontaneously hypertensive rats, while also providing neuroprotective effects in the dorsal hippocampus. L-2286 is applicable in research focused on hypertension and its associated vascular and neurological complications. -
HCV Inhibitor
Roseoside is a potent inhibitor targeting the HCV NS5A/B replicase, demonstrating an IC50 of 20 μM. This compound effectively interferes with HCV RNA replication in vitro and exhibits antibacterial properties against both Gram-positive and Gram-negative bacteria, as well as antifungal activity against Candida albicans. Roseoside serves as a valuable research tool for investigating bacterial infections, candidiasis, and Hepatitis A and C virus mechanisms, while demonstrating no cytotoxic effects in human systems. -
Topoisomerase Inhibitor
(±)-10-Hydroxycamptothecin is a potent topoisomerase I inhibitor known for its significant anticancer properties. This indole alkaloid demonstrates a broad spectrum of biological activity, making it a valuable reagent in cancer research. Its ability to interfere with DNA replication makes it a critical compound for studies focused on targeted therapies and drug resistance mechanisms in cancer cells. -
Topoisomerase II Inhibitor
Pixantrone is a potent topoisomerase II inhibitor and DNA intercalator, demonstrating significant anti-tumor activity. This compound interferes with DNA replication and transcription processes, making it valuable for cancer research. Its application spans various oncology studies, particularly in evaluating therapeutic effects against different tumor types. -
HDAC2 Inhibitor
HDAC2-IN-3 is a selective HDAC2 inhibitor with an IC50 of 14 nM, capable of crossing the blood-brain barrier. This compound effectively upregulates histone acetylation levels both in cultured cells and in vivo, and has been shown to enhance long-term potentiation (LTP) in the hippocampus. HDAC2-IN-3 is valuable for research applications focused on neurodegenerative disorders, particularly Alzheimer's disease.
