NF-κB/IκB

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  1. Sphingomyelinase Inhibitor, K-Ras Inhibitor, H-Ras Inhibitor, NF-κB Inhibitor

    Avicin G is a potent inhibitor of sphingomyelinases, specifically targeting neutral sphingomyelinases (SMPD2/3) and acid sphingomyelinase (SMPD1). This compound elevates intracellular sphingomyelin levels and modulates the distribution of sphingomyelin, disrupting signal transduction pathways in oncogenic K-Ras and H-Ras. Avicin G exhibits significant biological activity, including the reduction of ERK and Akt phosphorylation and alterations in lysosomal pH. Its applications extend to research on pancreatic ductal adenocarcinoma and non-small cell lung cancer.
  2. AP-1/NF-κB Activation Inhibitor

    SPC 839 is an orally active inhibitor that targets AP-1 and NF-κB mediated transcriptional activation, demonstrating an IC50 of 0.008 μM. This compound is essential for studying pathways associated with inflammation, cancer progression, and cellular stress responses. Its potent inhibition of key transcription factors makes it a valuable tool for researchers investigating the role of AP-1 and NF-κB in various biological processes.
  3. NF-κB Inhibitor

    Ganoderic acid H is a lanostane-type triterpene that functions as an NF-κB inhibitor. It effectively suppresses the growth and invasive behavior of breast cancer cells by inhibiting the activity of transcription factors AP-1 and NF-κB. This compound holds potential for research applications in cancer biology, particularly for studies focusing on the modulation of signaling pathways involved in tumor progression and metastasis.
  4. NF-κB/AP-1 Inhibitor

    Glucocorticoid receptor modulator 1 is a selective non-steroidal modulator that targets the glucocorticoid receptor, exhibiting potent inhibition of NF-κB and AP-1 with IC50 values of 9 nM and 130 nM, respectively. This compound effectively reduces the expression of key inflammatory cytokines, including IL-6, IL-1β, and TNF-α. Additionally, it demonstrates potential in alleviating dermatitis in preclinical models, making it a valuable tool for research in inflammation and immune response.
  5. COX Inhibitor

    Inulicin (1-O-Acetylbritannilactone) is a potent inhibitor of cyclooxygenase (COX) enzymes, specifically targeting COX-2 activity. This compound demonstrates significant biological activity by inhibiting lipopolysaccharide (LPS)-induced production of prostaglandin E2 (PGE2) as well as the expression of COX-2. Additionally, Inulicin suppresses NF-κB activation and its translocation, making it valuable for research applications related to inflammation and cancer.
  6. 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.
  7. 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.
  8. 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.
  9. 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.
  10. 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.
  11. 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.
  12. 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.
  13. 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.
  14. 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.
  15. 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.
  16. 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.
  17. 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.
  18. 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.
  19. NF-κB Inhibitor, GPx Inhibitor, HIV Replication Inhibitor

    α-MSH (11-13) acetate is a selective melanocortin-1 receptor ligand that functions as an inhibitor of NF-κB, GPx activity, and HIV replication. It induces an acute elevation of intracellular calcium levels under certain costimulation or pathway inhibition conditions. This compound effectively suppresses TNF-α-induced NF-κB activation, inhibits colony formation of Staphylococcus aureus and Candida albicans, and demonstrates potential in the study of infections related to these pathogens, as well as in traumatic brain injury, corneal epithelial wounds, and inflammatory bowel disease research.
  20. 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.
  21. 20S Proteasome Inhibitor

    5-Amino-8-hydroxyquinoline is a non-competitive inhibitor of the 20S proteasome, demonstrating potent inhibitory effects on NF-κB activity. This compound induces apoptosis in cancer cells while exhibiting minimal cytotoxicity towards normal hematopoietic cells. It is valuable for research applications in cancer biology, particularly in the study of leukemia and related malignancies.
  22. Immunoproteasome β5i Subunit Inhibitor

    DPLG3 is a selective inhibitor of the immunoproteasome β5i subunit, demonstrating an IC50 of 4.5 nM. It effectively inhibits the mouse i-20S proteasome with an IC50 value of 9.4 nM. DPLG3 is capable of downregulating the protein levels of NF-κB p50 and p65, highlighting its potential in the study of immune-related diseases and therapeutic applications.
  23. Proteasome Inhibitor

    Biotin-(Oaa)3-epoxomicin is a biotinylated proteasome inhibitor derived from Epoxomicin, connected through three hydrophilic oxaacetyl amino acid linkers. This compound is utilized primarily in proteomic research for the capture and identification of proteasome complexes, facilitating target validation and elucidation of intracellular targets. Epoxomicin effectively inhibits proteasome activity through covalent binding to catalytic subunits such as LMP7, X, MECL1, and Z, with a pronounced effect on chymotrypsin-like activity, while sparing non-proteasomal proteases like trypsin and papain. Additionally, it serves as an NF-κB inhibitor, demonstrating potential in studies of inflammatory responses.
  24. 20S Proteasome Inhibitor

    5-Amino-8-hydroxyquinoline dihydrochloride is a potent non-competitive inhibitor of the 20S proteasome. This compound effectively inhibits NF-κB activity, leading to apoptosis in cancer cells while exhibiting minimal cytotoxicity towards normal hematopoietic cells. Its unique properties make it a valuable tool for cancer research, particularly in studies related to leukemia and other malignancies.
  25. Proteasome Inhibitor

    Z-LLF-CHO (Z-Leu-Leu-Phe-CHO) is a potent inhibitor of the chymotrypsin-like activity of the proteasome, exhibiting an inhibition constant (Ki) of 460 nM. This compound also functions as an inhibitor of NF-κB nuclear translocation, making it valuable for studies involving immune response and inflammation. Research applications include investigations into proteolytic processes and the role of cytokines in various disease models.
  26. Proteasome Inhibitor

    4-Nitrochalcone serves as a proteasome inhibitor, specifically targeting the proteasomal degradation pathway. It effectively inhibits the activity of NF-κB induced by TNFα, making it a valuable tool for studying inflammatory processes and signaling pathways. This compound is utilized in research focused on cancer, neurodegenerative diseases, and other conditions where proteasome activity plays a critical role.
  27. Trx/TrxR System Inhibitor

    PMX464 is a thiol-reactive quinol that acts as an inhibitor of the thioredoxin-thioredoxin reductase (Trx/TrxR) system. This compound has been shown to inhibit NF-κB-mediated pro-inflammatory activation in human type II alveolar epithelial cells, making it a valuable tool for research focused on inflammation and oxidative stress. PMX464 is particularly useful in studies examining the role of redox signaling in various pathophysiological conditions.
  28. Tyrosinase Inhibitor

    MHY884 is a potent tyrosinase inhibitor that effectively mitigates UVB-induced activation of the NF-κB signaling pathway by downregulating oxidative stress. This compound demonstrates a reduction in oxidative stress within melanoma cells, leading to diminished NF-κB activity in irradiated models. MHY884 holds significant promise for investigations into the mechanisms of UVB-induced skin damage and its potential therapeutic applications.
  29. Aβ Inhibitor

    TML-6 is an orally active curcumin derivative that functions as a β-amyloid (Aβ) inhibitor by impeding the synthesis of β-amyloid precursor protein. It demonstrates key biological activities including the upregulation of Apo E, suppression of NF-κB and mTOR pathways, and enhancement of the anti-oxidative Nrf2 response. TML-6 is positioned as a promising candidate for research in Alzheimer's disease (AD) mechanisms and therapeutic developments.
  30. NIK Inhibitor

    B022 is a selective inhibitor of NF-κB-inducing kinase (NIK) with a Ki of 4.2 nM and an IC50 of 15.1 nM. This compound exhibits protective effects against liver inflammation, oxidative stress, and injury caused by toxins. Additionally, B022 features an alkyne group, enabling its use in click chemistry applications, specifically for copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules.
  31. NF-κB Inhibitor

    Helenalin is a sesquiterpene lactone that acts as an inhibitor of the transcription factor NF-κB. By directly targeting the p65 subunit, Helenalin exhibits alkylating activity through its interaction with cysteine sulfhydryl groups, effectively hindering NF-κB's ability to bind DNA. This compound is primarily utilized in research focused on anti-inflammatory pathways and mechanisms involving NF-κB signaling.
  32. NF-κB Inhibitor

    NF-κB-IN-11 is a selective NF-κB inhibitor that targets the NF-κB signaling pathway. It effectively inhibits TNF-α induced activation of NF-κB and prevents its nuclear translocation, leading to down-regulation of phospho-IKK, IκBα, and NF-κB p65 expression levels. This compound demonstrates significant anti-inflammatory properties, as evidenced by its ability to alleviate dextran sulfate sodium-induced colitis in murine models. NF-κB-IN-11 also exhibits a maximum tolerated dose (MTD) exceeding 1852 mg/kg in acute toxicity assessments in mice, highlighting its safety profile for research applications.
  33. NF-κB Inhibitor

    Bezisterim is a synthetic derivative of the natural anti-inflammatory steroid β-AET, functioning as a partial inhibitor of NF-κB. This compound effectively reduces pro-inflammatory signals, such as IL-6 and matrix metallopeptidase 3, and demonstrates the ability to penetrate the blood-brain barrier in murine models. Bezisterim is valuable in research applications related to ulcerative colitis, arthritis, and experimental autoimmune encephalomyelitis. Additionally, its alkyne group allows it to participate in copper-catalyzed azide-alkyne cycloaddition, making it a versatile tool in click chemistry.
  34. NF-κB Inhibitor

    AP-1/NF-κB activation inhibitor 1 is a potent inhibitor of AP-1 and NF-κB-mediated transcriptional activation, with an IC50 of 1 μM. This compound does not interfere with basal transcription driven by the β-actin promoter, making it suitable for study in various cellular contexts. Additionally, AP-1/NF-κB activation inhibitor 1 effectively reduces IL-2 and IL-8 production in stimulated cells, supporting its utility in inflammatory and immunological research applications.
  35. NF-κB/AP-1 Inhibitor

    SP-100030 is a potent inhibitor of NF-κB and activator protein-1 (AP-1), exhibiting IC50 values of 50 nM for both targets. This compound effectively suppresses the production of pro-inflammatory cytokines, including IL-2, IL-8, and TNF-alpha, in Jurkat and other T cell lines. Additionally, SP-100030 has demonstrated efficacy in reducing symptoms in murine models of collagen-induced arthritis (CIA).
  36. c-Rel Inhibitor

    IT-901 is a potent and orally active inhibitor of the NF-κB subunit c-Rel, exhibiting an IC50 of 0.1 μM for NF-κB DNA binding and 3 μM for c-Rel DNA binding. As a bioactive derivative of naphthalenethiobarbiturate, IT-901 holds promise for therapeutic applications in human lymphoid tumors and may provide benefits in mitigating graft-versus-host disease (GVHD). This compound is valuable for research in cancer and immunological responses, facilitating the exploration of NF-κB-related pathways.
  37. NF-κB Inhibitor

    DMAPT (Dimethylamino Parthenolide) is a potent inhibitor of NF-κB signaling, characterized by an LD50 of 1.7 μM in acute myeloid leukemia (AML) cells. This compound exhibits significant anti-cancer and anti-metastatic properties, making it a valuable tool for research in cancer therapeutics. DMAPT can be used to investigate the role of NF-κB in cancer progression and to explore new treatment strategies.
  38. NF-κB Inhibitor

    Hesperidin methylchalcone is a potent NF-κB inhibitor, functioning as an orally bioavailable flavonoid with notable analgesic, anti-inflammatory, and antioxidant properties. Its ability to inhibit oxidative stress, cytokine production, and NF-κB activation highlights its potential in managing inflammatory conditions. This compound is particularly relevant for research into gout disease and related inflammatory disorders.
  39. NF-κB Inhibitor

    Myrcene, a natural aromatic compound, functions as an NF-κB inhibitor by suppressing TNFα and NF-κB activity. It exhibits notable anti-invasive properties, induces cell cycle arrest, and promotes apoptosis in cancer cells. Additionally, myrcene demonstrates significant blood protective effects and possesses anti-inflammatory activity, making it valuable for various research applications in cancer and inflammation studies.
  40. JS6

    Bcl3 Inhibitor

    JS6 is a potent Bcl3 inhibitor that disrupts the interaction between Bcl3 and NF-κB1. This compound demonstrates significant anti-tumor activity by inhibiting tumor cell growth in both in vitro and in vivo models. JS6 is valuable for research focused on cancer biology, specifically regarding NF-κB signaling pathways and their implications in tumorigenesis.
  41. NF-κB Inhibitor

    Deoxyelephantopin is a natural bioactive sesquiterpene lactone that primarily targets NF-κB signaling pathways. It exhibits potent anticancer activity across various cancer types by inhibiting key cellular signaling mechanisms, including MAPK, PI3K/Akt, and β-catenin. This compound serves as a valuable tool for researchers investigating cancer biology and therapeutic interventions.
  42. NF-κB Inhibitor

    Handelin is a guaianolide dimer derived from Chrysanthemum boreale that acts as a potent inhibitor of NF-κB signaling. This compound effectively down-regulates the production of pro-inflammatory cytokines, demonstrating significant anti-inflammatory activity. Handelin is valuable for research applications focused on inflammation, immune response modulation, and related signaling pathways.
  43. NF-κB Inhibitor

    Galloylpaeoniflorin is a potent NF-κB inhibitor that plays a significant role in modulating inflammatory responses. Its mechanism involves the inhibition of NF-κB signaling, which is critical in various pathological conditions. This compound is valuable for research applications focused on inflammation, cancer, and other diseases linked to dysregulated NF-κB activity. Additionally, Galloylpaeoniflorin has been shown to inhibit DNA cleavage, contributing to its potential therapeutic effects in molecular biology studies.
  44. NF-κB Inhibitor

    14-Deoxy-11,12-didehydroandrographolide is a potent inhibitor of NF-κB activation. This natural compound, an analogue of Andrographolide, demonstrates significant anti-inflammatory properties by modulating the NF-κB signaling pathway. It is suitable for research applications investigating inflammation, cancer, and autoimmune disorders.
  45. NF-κB Inhibitor

    Quinoclamine, a naphthoquinone derivative, functions as an NF-κB inhibitor. It has demonstrated anti-cancer properties, making it a valuable tool for cancer research and the investigation of NF-κB signaling pathways. Its ability to modulate NF-κB activity opens avenues for studying inflammatory responses and potential therapeutic approaches in oncology.
  46. XT2

    NIK Inhibitor

    XT2 is a selective inhibitor of NF-κB-inducing kinase (NIK), demonstrating potent oral activity with an IC50 of 9.1 nM. It effectively suppresses the CCl4-induced upregulation of alanine aminotransferase (ALT), a significant biomarker for acute liver injury, and reduces immune cell infiltration in damaged liver tissue. XT2 is valuable for investigating inflammatory liver diseases and features an alkyne group for click chemistry applications, allowing for copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules.
  47. NF-κB Inhibitor

    Armepavine is a potent NF-κB inhibitor derived from Nelumbo nucifera. It demonstrates significant anti-inflammatory effects on human peripheral blood mononuclear cells and exhibits immunosuppressive activity towards T lymphocytes and in lupus nephritic mice models. Armepavine effectively inhibits TNF-α-induced MAPK and NF-κB signaling pathways, making it a valuable reagent for research into inflammatory and autoimmune disorders.
  48. NF-κB Inhibitor

    NF-κB-IN-4 is a potent inhibitor of the NF-κB signaling pathway, demonstrating significant blood-brain barrier permeability. This compound exhibits anti-neuroinflammatory activity through its ability to block the phosphorylation and activation of IκBα, thereby reducing NLRP3 expression and inhibiting NF-κB activation. NF-κB-IN-4 is suitable for research applications related to neuroinflammatory diseases, providing a valuable tool for therapeutic investigations.
  49. NF-κB Inhibitor

    (R)-(-)-Ibuprofen is a selective inhibitor of NF-κB activation. It demonstrates significant anti-inflammatory and antinociceptive properties, making it a valuable tool in research related to inflammation and pain modulation. This compound is particularly useful for studying pathways associated with NF-κB and its role in inflammatory responses.
  50. NF-κB Inhibitor

    Ginsenoside Rk3 functions as an NF-κB inhibitor, extracted from the roots of Panax ginseng. It exhibits significant inhibition of TNF-α-induced NF-κB transcriptional activity, with an IC50 value of 14.24±1.30 μM in HepG2 cells. This compound is useful in research focusing on inflammation, cancer, and signaling pathways mediated by NF-κB.

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