NF-κB/IκB

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  1. Antioxidant Agent

    Chrysoeriol is a natural flavonoid known for its antioxidant properties. This compound exhibits significant anti-inflammatory activity by inhibiting critical signaling pathways, including JAK2/STAT3, IκB/p65, and NF-κB. Due to its robust biological activities, chrysoeriol is valuable in research applications focused on inflammation and oxidative stress-related conditions.
  2. Endogenous Metabolite

    Stachydrine is an endogenous metabolite that primarily functions in promoting blood circulation and alleviating blood stasis, particularly noted in the traditional Chinese herb Leonurus heterophyllus. This compound has been shown to inhibit the NF-κB signaling pathway, suggesting its potential role in modulating inflammatory processes. Stachydrine is valuable for research applications focused on cardiovascular health and inflammation.
  3. Vitamin E

    γ-Tocotrienol is an active form of vitamin E that primarily targets the signaling pathway of NF-κB and P-glycoprotein (P-gp). It demonstrates significant biological activity by reversing multidrug resistance (MDR) in breast cancer cells, enhancing the efficacy of chemotherapeutic agents. Additionally, γ-tocotrienol serves as a radioprotective agent, effectively mitigating bone marrow radiation damage associated with targeted radionuclide treatments. Research applications include cancer therapy and protection against radiation-induced injury.
  4. ACAT Inhibitor

    ACAT-IN-7 is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor. This compound effectively inhibits ACAT activity, resulting in altered lipid metabolism and subsequent reduction in cholesterol esterification. ACAT-IN-7 is of particular interest in research exploring its potential role in inflammatory processes, as it inhibits NF-κB mediated transcription, which is crucial for various cellular responses.
  5. ACAT Inhibitor

    ACAT-IN-2 is a selective inhibitor of acyl-Coenzyme A:cholesterol acyltransferase (ACAT). This compound effectively inhibits the NF-κB mediated transcriptional process, making it a valuable tool for research in cholesterol metabolism and inflammatory pathways. ACAT-IN-2 is primarily utilized in studies investigating dyslipidemia and its associated diseases, contributing to a deeper understanding of lipid regulation and associated pathophysiology.
  6. ACAT Inhibitor

    ACAT-IN-10 is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor that provides valuable insights into lipid metabolism. This compound is particularly useful in studying the regulation of cholesterol esters and their implications in various diseases, including atherosclerosis and metabolic disorders. Additionally, ACAT-IN-10 exhibits weak inhibition of NF-κB-mediated transcription, making it a potential tool for investigating inflammatory pathways.
  7. ACAT Inhibitor

    ACAT-IN-4 hydrochloride is a selective acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor. It disrupts cholesterol esterification, leading to a reduction in lipid accumulation in cells. This compound has significant implications for research in atherosclerosis, inflammation, and lipid metabolism, particularly through its ability to inhibit NF-κB mediated transcription.
  8. ACAT Inhibitor

    ACAT-IN-9 is a selective acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor that effectively disrupts the synthesis of cholesteryl esters. By inhibiting ACAT activity, ACAT-IN-9 also attenuates NF-κB mediated transcription, which plays a critical role in inflammation and immune responses. This compound is utilized in research focusing on lipid metabolism, cardiovascular diseases, and inflammation pathways.
  9. ACAT Inhibitor

    ACAT-IN-4 is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor that effectively impedes ACAT activity. This compound has been shown to inhibit NF-κB mediated transcription, making it a valuable tool for studying cholesterol metabolism and inflammatory responses. ACAT-IN-4 is suitable for research applications focusing on lipid regulation, atherosclerosis, and other related cardiovascular conditions.
  10. ACAT Inhibitor

    ACAT-IN-10 dihydrochloride is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor. This compound exhibits weak inhibition of NF-κB mediated transcription, highlighting its potential role in modulating inflammatory processes. It is primarily utilized in research focused on lipid metabolism and its implications in various diseases, including atherosclerosis and metabolic disorders. ACAT-IN-10 dihydrochloride serves as a valuable tool for investigating the biochemical pathways regulated by ACAT activity.
  11. ACAT Inhibitor

    ACAT-IN-6 is a potent acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor. This compound effectively inhibits NF-κB mediated transcription, making it a valuable tool for studying lipid metabolism and inflammatory pathways. ACAT-IN-6 is useful in research applications focused on cholesterol homeostasis and related diseases.
  12. ACAT Inhibitor

    ACAT-IN-3 is an inhibitor of acyl-Coenzyme A:cholesterol acyltransferase (ACAT), targeting the cholesterol esterification pathway. This compound effectively inhibits NF-κB-mediated transcription, making it a valuable tool in studying pathways associated with inflammation and lipid metabolism. Its application in research may help elucidate the role of ACAT in various disease models, particularly those related to atherosclerosis and other metabolic disorders.
  13. ACAT Inhibitor

    ACAT-IN-5 is a selective inhibitor of acyl-Coenzyme A:cholesterol acyltransferase (ACAT), a key enzyme involved in cholesterol metabolism. By inhibiting ACAT activity, ACAT-IN-5 has been shown to modulate NF-κB mediated transcription, thereby influencing inflammatory pathways and lipid metabolism. This reagent is vital for research applications exploring cholesterol homeostasis, atherosclerosis, and related metabolic disorders.
  14. Flavonoid

    Chrysin-7-O-glucuronide is a flavonoid that targets α-glucosidase and α-amylase, exhibiting inhibitory activity with IC50 values of 612.13 and 980.73 μg/mL, respectively. This compound is known to suppress NF-κB signaling and possesses free radical scavenging abilities, functioning as a protectant for tight junctions and alleviating intestinal mucosal barrier injury. Chrysin-7-O-glucuronide is relevant for research focused on type 2 diabetes and the impacts of severe acute pancreatitis on intestinal health.
  15. CYP3A4 Inhibtior

    Curcumenol is a potent inhibitor of CYP3A4, exhibiting an IC50 value of 12.6 μM. This bioactive compound, derived from Curcuma zedoaria, demonstrates neuroprotective, anti-inflammatory, anti-tumor, and hepatoprotective activities. In studies, Curcumenol suppresses Akt-mediated NF-κB activation and inhibits the p38 MAPK signaling pathway in LPS-stimulated BV-2 microglial cells, making it a valuable tool for research in neuroinflammation and cancer therapy.
  16. NF-κB/MAPKs Inhibitor

    Tetrahydropiperine is a selective inhibitor of NF-κB and MAPKs, while simultaneously activating the PI3K/Akt/mTOR pathway. This compound effectively reduces the production of pro-inflammatory cytokines, including TNF-α, IL-6, and nitric oxide, by inhibiting the nuclear translocation of NF-κB and the phosphorylation of ERK, JNK, and p38 MAPKs. Additionally, Tetrahydropiperine mitigates excessive autophagy, offering neuroprotective benefits against oxidative damage. Its diverse biological activities make it valuable for research focused on inflammatory conditions, such as endotoxemia and arthritis, as well as neurological disorders, including ischemic stroke.
  17. Anti-oxidant, Aromatase Inhibitor, Anabolic Agent

    5-Methyl-7-methoxyisoflavone is an orally active antioxidant that primarily functions as an aromatase inhibitor. This compound disrupts testosterone metabolic pathways, making it useful in various anabolic applications. It exhibits enhanced potency in increasing muscle mass and endurance compared to other anabolic agents. Additionally, 5-Methyl-7-methoxyisoflavone supports fat loss, contributes to the maintenance of low cholesterol levels, and aids in strengthening bone density. The compound also acts as an inhibitor of NF-κB, further expanding its potential therapeutic applications.
  18. 11β-hydroxysteroid dehydrogenase 1 Inhibitor

    Lunularin is a selective inhibitor of 11β-hydroxysteroid dehydrogenase 1, exhibiting an IC50 of 45.44 μM for human and 17.39 μM for rat enzymes. This compound has been shown to modulate gene expression by upregulating Sirt1 and Hmox1 in liver tissue, while also reducing food intake, body weight gain, and blood glucose levels in high-fat diet mice. Furthermore, Lunularin displays anti-cancer properties by inhibiting cell proliferation and colony formation in renal and colon cancer cell lines, along with suppression of LPS-induced NF-κB pathway activation. This reagent is valuable for research in obesity, cancer biology, inflammation, and metabolic disorders.
  19. ACAT Inhibitor

    ACAT-IN-8 is a selective inhibitor of acyl-Coenzyme A:cholesterol acyltransferase (ACAT), a key enzyme involved in intracellular cholesterol esterification. By inhibiting ACAT, this compound modulates lipid metabolism and significantly impacts NF-κB mediated transcription. ACAT-IN-8 is useful for research applications related to cardiovascular diseases, metabolic disorders, and inflammation, providing insights into cholesterol-related pathways and their regulation.
  20. NF-κB Inhibitor

    (R)-(+)-Anatabine is an NF-κB inhibitor that acts to lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). As the less active R-enantiomer of Anatabine, it retains the ability to modulate α4β2 nAChR activity. This compound exhibits anti-inflammatory properties and is being investigated for its potential applications in the treatment of neurodegenerative disorders.
  21. 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.
  22. Calcium Channel Inhibitor

    Nothofagin is a dihydrochalcone that acts as a calcium channel inhibitor. By blocking calcium influx, it downregulates NF-κB translocation, providing a mechanism to modulate inflammatory responses. This compound exhibits antioxidant properties and has potential applications in research related to septic responses and vascular inflammation.
  23. Proatherosclerotic Peptide Hormone

    GIP (22-51) human is a potent proatherosclerotic peptide hormone targeting the NF-κB signaling pathway. This 30-amino acid peptide promotes the expression of matrix metalloproteinase-8 (MMP-8) and induces proinflammatory and proatherosclerotic protein expression. Additionally, GIP (22-51) human elevates intracellular free calcium levels in THP-1-derived macrophages, making it a valuable tool for atherosclerosis research.
  24. Cationic Lipid

    H1L1A1B3 is an ionizable cationic lipid designed for the formation of lipid nanoparticles (LNPs) to effectively deliver circular RNA (circRNA). This lipid exhibits superior transfection efficiency, yielding a fourfold enhancement in circRNA delivery to lung cancer cells compared to conventional lipids. Additionally, H1L1A1B3 activates the NF-κB/IRF immune signaling pathways, making it a valuable tool for enhancing RNA therapeutic applications in research.
  25. MALT1 Inhibitor

    Z-VRPR-FMK is an irreversible inhibitor of the MALT1 protein. It effectively inhibits the growth and invasion of diffuse large B-cell lymphoma by blocking MALT1-induced NF-κB activation and matrix metalloproteinase (MMP) expression. This makes Z-VRPR-FMK a valuable tool for research investigating the role of MALT1 in oncogenesis and therapeutic strategies targeting NF-κB pathways.
  26. Proteasomal Degrader

    (S,R,S)-AHPC-Boc derivative 1 is a selective proteasomal degrader that targets MALT1. By recruiting the E3 ubiquitin ligase CRBN, it forms a ternary complex with MALT1, facilitating its ubiquitination and subsequent proteasomal degradation. This compound inhibits the NF-κB signaling pathway by disrupting the CBM complex, which may induce apoptosis in ABC-DLBCL cells. (S,R,S)-AHPC-Boc derivative 1 is valuable for the investigation of MALT1-dependent cancers, particularly diffuse large B-cell lymphoma (DLBCL).
  27. MALT1 Inhibitor

    MALT1-IN-5 is a potent inhibitor of the MALT1 protease, targeting the NF-κB signaling pathway. This compound has demonstrated significant biological activity in disrupting MALT1-dependent signaling processes. MALT1-IN-5 is primarily utilized in cancer research to investigate the role of MALT1 in tumorigenesis and its potential as a therapeutic target.
  28. MALT1 Inhibitor

    NVS-MALT1 is an allosteric inhibitor of the MALT1 protein, disrupting its activity and providing a valuable tool for studying MALT1-mediated signaling pathways. This compound demonstrates the ability to modulate NF-κB activation and enhance apoptosis in cancer cells, making it relevant for research in oncology and immune response. It is particularly useful in investigations focusing on B-cell lymphoma and other MALT1-associated diseases.
  29. MALT1 Inhibitor

    RGT-068A is a selective and orally bioavailable inhibitor of MALT1 (Mucosa-associated lymphoid tissue lymphoma translocation protein 1). This compound demonstrates potent inhibitory activity against MALT1, which is essential for NF-κB signaling in various hematological malignancies and inflammatory diseases. RGT-068A serves as a valuable tool for research into therapeutic strategies targeting MALT1 in cancer and autoimmune disorders.
  30. NF-κB Inhibitor

    SEMBL is a potent inhibitor of NF-κB, specifically targeting NF-κB-DNA binding to disrupt its transcriptional activity. This compound effectively reduces the secretion of NF-κB-dependent inflammatory cytokines and diminishes cancer cell migration and invasion by decreasing matrix metalloproteinase (MMP) expression. SEMBL is valuable for research in anticancer therapies and the study of inflammation-related pathways.
  31. CHI3L1 Inhibitor

    CHI3L1-IN-5 is a selective inhibitor of CHI3L1, exhibiting a KD value of 6 μM. This compound enhances astrocytic clearance by rejuvenating lysosomal function and promoting Aβ uptake, while simultaneously mitigating neuroinflammation through inhibition of the NF-κB pathway. CHI3L1-IN-5 is valuable for investigating its potential therapeutic applications in Alzheimer's disease research.
  32. Stimulator

    Erinacine C is a potent activator of the Nrf2 signaling pathway and an inhibitor of the NF-κB signaling pathway. This compound demonstrates significant antioxidant, neuroprotective, and anti-inflammatory properties, making it a valuable tool in research focused on oxidative stress and neurodegenerative diseases. Its biological activities support studies aimed at exploring therapeutic strategies for conditions associated with inflammation and cellular damage.
  33. Stable Isotope

    Stachydrine-d6 is a deuterated form of Stachydrine, a compound known for its role in promoting blood circulation and alleviating blood stasis, particularly in the traditional Chinese herb Leonurus heterophyllus. This stable isotope can be used in tracing studies and metabolic research due to its labeled nature. Additionally, Stachydrine exhibits inhibitory effects on the NF-κB signaling pathway, highlighting its potential in studies related to inflammation and immunity.
  34. Secondary Metabolite

    Moniliphenone is a secondary metabolite derived from the endophytic fungus Penicillium chrysogenum. This compound exhibits notable anti-inflammatory properties and effectively inhibits TNF-α-stimulated NF-κB activation, making it a valuable tool for exploring pathways involved in inflammation. Its applications in research can aid in understanding the molecular mechanisms of inflammatory diseases and developing potential therapeutic strategies.
  35. Stable Isotope

    D-Ribose (mixture of isomers)-13C5 is a stable isotope-labeled form of D-Ribose, which serves as a crucial sugar moiety in adenosine triphosphate (ATP) production. It functions as an energy enhancer and is commonly employed in metabolic therapy for conditions such as chronic fatigue syndrome and cardiac energy metabolism. Additionally, D-Ribose is involved in protein glycation and can stimulate NF-κB-dependent inflammation through the receptor for advanced glycation end-products (RAGE). This makes it a valuable tool for research in metabolic and inflammatory pathways.
  36. NF-κB Nuclear Accumulation Inhibitor

    Cyclo(his-pro) TFA is a cyclic dipeptide that functions as an NF-κB nuclear accumulation inhibitor. This compound is capable of crossing the blood-brain barrier, making it valuable for studying its effects on various inflammatory and stress-related pathways. Its ability to modulate NF-κB activity supports research in neuroinflammation and other related conditions.
  37. PI3K/PIKK Inhibitor

    PI3K/PIKK-IN-2 is a potent inhibitor of the phosphoinositide 3-kinase (PI3K) and phosphoinositide-dependent kinase (PIKK) pathways. This compound demonstrates significant biological activity by modulating signaling pathways involved in cell growth, metabolism, and survival. PI3K/PIKK-IN-2 is suitable for use in research applications focused on targeted therapies, including the development of antibody-drug conjugates (ADCs).
  38. Sigma-2 ligand/Agonist

    SW43 is a selective Sigma-2 ligand and agonist that plays a pivotal role in cancer research. This compound enhances the development of targeted therapeutic agents, showing significant antitumor activity when conjugated with DOX-L-NETA (89Y) in a VX2 liver tumor allograft rabbit model. Additionally, when combined with SW IV-52s to create SW III-123, SW43 activates the NF-κB pathway, demonstrating potent cytotoxic effects against ovarian cancer cell lines and promoting apoptosis. This dual functionality underscores its utility in cancer therapeutic development.
  39. TBK1/IKKε Inhibitor

    BAY-985 is a selective ATP-competitive dual inhibitor targeting TBK1 and IKKε, demonstrating high potency with IC50 values of 2 nM for TBK1 under low ATP conditions and 30 nM under high ATP conditions, and 2 nM for IKKε. This inhibitor exhibits significant antitumor activity, making it a valuable tool for research applications focused on cancer therapy and the modulation of inflammatory pathways. Its oral bioavailability further enhances its utility in preclinical studies.
  40. IKKα Inhibitor

    BAY32-5915 is a selective inhibitor of IKKα, exhibiting an IC50 value of 60 nM. This compound effectively prevents the activation of NF-κB without interfering with Doxorubicin-induced pathways. It is valuable for research in inflammation and cancer, providing insights into NF-κB signaling modulation.
  41. IKK/NF-κB Inhibitor

    NF-κB-IN-1 is a selective inhibitor of the IκB kinase (IKK) and functions primarily through the inhibition of NF-κB signaling. This compound effectively blocks the activation of NF-κB, demonstrating potent anti-cancer activity by reducing cell viability in lung cancer cells. Additionally, NF-κB-IN-1 significantly diminishes the clonogenic potential of A549 cells, making it a valuable tool for research on cancer therapeutics targeting NF-κB pathways.
  42. Negative control of IKK

    6-Chloro-7-deazaguanine serves as a negative control for IκB kinase (IKK), specifically lacking the essential 5-cyano group that defines its activity. As an inactive analog, it provides a useful reference for studying the IKKβ and IKKα pathways, which are crucial components of the canonical and non-canonical NF-κB signaling pathways. Researchers can utilize this compound to delineate the role of IKK in various cellular processes and disease models, particularly in inflammation and immune responses.
  43. IKK Inhibitor

    SU1261 is a potent inhibitor of IKK, displaying Ki values of 10 nM for IKKα and 680 nM for IKKβ. This compound effectively inhibits non-canonical NF-κB signaling pathways, making it a valuable tool for studying the role of IKK in various cellular processes. Its application in research, particularly in osteosarcoma cell models such as U2OS, can provide insights into inflammatory responses and oncogenic signaling mechanisms.
  44. IKK/NF-κB Inhibitor

    SR12343 is an IKK/NF-κB inhibitor that acts as a mimetic of the NF-κB essential modulator (NEMO)-binding domain. It effectively disrupts the interaction between IKKβ and NEMO, leading to inhibition of TNF-α- and LPS-induced NF-κB activation, with an IC50 of 37.02 μM for TNF-α-mediated pathways. SR12343 has been shown to reduce LPS-induced acute pulmonary inflammation in murine models, making it valuable for research into inflammatory and degenerative diseases.
  45. TBK1/IKKε Inhibitor

    TBK1/IKKε-IN-4 is a selective inhibitor of TBK1 and IKKε, characterized by its 6-aminopyrazolopyrimidine structure. With IC50 values of 13 nM and 59 nM for TBK1 and IKKε, respectively, this compound demonstrates significant potency. It exhibits minimal activity against other protein kinases, including PDK1, PI3K family members, and mTOR, making it an efficient tool for investigating TBK1/IKKε-related pathways in various biological contexts. This inhibitor is useful for studies in inflammation, immune response, and neurodegenerative diseases.
  46. IKKβ Inhibitor

    BOT-64 is a selective IκB kinase β (IKKβ) inhibitor with an IC50 value of 1 µM. This compound effectively inhibits lipopolysaccharide-induced activation of nuclear factor-κB (NF-κB) and the subsequent transcription of NF-κB-regulated inflammatory genes. BOT-64 is valuable for research into inflammatory pathways and NF-κB signaling, providing insights into potential therapeutic strategies for inflammatory diseases.
  47. IKK-2 Inhibitor

    IKK2-IN-4 is a selective inhibitor of IKK-2, exhibiting a potent IC50 value of 25 nM. This compound effectively inhibits LPS-induced TNFα production in peripheral blood mononuclear cells (PBMCs), making it a valuable tool for studying inflammatory responses. Research applications include investigations into signaling pathways involved in inflammation and potential therapeutic strategies for immune-related disorders.
  48. IKK Inhibitor

    HPN-01 is a potent and selective inhibitor of IκB kinase (IKK), demonstrating pIC50 values of 6.4, 7.0, and <4.8 for IKK-α, IKK-β, and IKK-ε, respectively. This compound exhibits significant selectivity, showing more than 50-fold preference over a diverse panel of over 50 kinases, including ALK5, CDK-2, EGFR, ErbB2, GSK3β, PLK1, Src, and VEGFR-2. HPN-01 is a valuable tool for research applications focused on inflammatory pathways, cancer cell signaling, and the study of immune responses.
  49. ikkβ Inhibitor

    IKKβ-IN-4 is a selective inhibitor of IkappaB kinase-β (IKKβ), with an IC50 value of 1.9 μM. IKKβ plays a crucial role in the NF-κB signaling pathway, which is implicated in various diseases, including inflammation and cancer. This compound is utilized in research to study the modulation of NF-κB activity and its potential therapeutic applications in related disease models.
  50. IKKβ Inhibitor

    MLN120B dihydrochloride is a potent inhibitor of IKKβ, exhibiting competitive ATP binding with an IC50 of 60 nM. This compound effectively inhibits the growth of multiple myeloma cells both in vitro and in vivo, making it a valuable tool for cancer research. Additionally, MLN120B can be utilized in studies focused on rheumatoid arthritis, contributing to the understanding of inflammatory pathways and potential therapeutic interventions.

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