NF-κB

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  1. 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).
  2. 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.
  3. 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.
  4. 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.
  5. 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.
  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. 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.
  8. 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.
  9. 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.
  10. 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.
  11. 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.
  12. 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.
  13. 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.
  14. 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.
  15. 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.
  16. 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.
  17. 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.
  18. 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.
  19. 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.
  20. IKK2 Inhibitor

    IKK2-IN-3 is a selective inhibitor of IKK2, demonstrating a potent inhibitory effect with an IC50 value of 0.075 μM. This compound effectively disrupts the NF-κB signaling pathway, impacting various cellular processes such as inflammation and immune response. IKK2-IN-3 is suitable for research applications involving the modulation of IKK2 activity in disease models and studying the role of NF-κB in cellular signaling.
  21. IKK2 Inhibitor

    LY2409881 is a selective inhibitor of IκB kinase β (IKK2), demonstrating potent inhibition with an IC50 of 30 nM. This compound is primarily used in research for its ability to modulate the NF-κB signaling pathway, making it relevant for studying inflammation, cancer, and autoimmune diseases. Researchers utilize LY2409881 to explore its therapeutic potential in various disease models and to investigate the role of IKK2 in cellular processes.
  22. IκB Kinase-2 Inhibitor

    PS-1145 dihydrochloride is a selective inhibitor of IκB kinase-2, exhibiting an IC50 value of 88 nM. This compound effectively inhibits the phosphorylation of IκB kinase, thereby suppressing NF-κB activity. PS-1145 dihydrochloride is utilized in research applications targeting inflammatory responses and cancer biology.
  23. IKK2 Inhibitor

    IKK-IN-4 is a selective inhibitor of IkappaB kinase 2 (IKKβ), exhibiting an IC50 of 45 nM for IKKβ and 650 nM for IKKα. This compound is instrumental in research focusing on the NF-κB signaling pathway and its regulation, providing insights into inflammation, cancer, and other diseases linked to IKK activity. IKK-IN-4 serves as a valuable tool for studying IKKβ-mediated signaling mechanisms and potential therapeutic interventions.
  24. IKK Inhibitor

    (E/Z)-HOIPIN-1 is a selective inhibitor of the linear ubiquitin chain assembly complex (LUBAC), targeting the IκB kinase (IKK) pathway. With an IC50 value greater than 2.8 μM, this compound effectively inhibits LUBAC-mediated NF-κB activation. Its potential applications include studies of inflammatory responses, cancer biology, and the modulation of immune signaling pathways.
  25. IKKβ Inhibitor

    MLN-0415 is an inhibitor of IKKβ, a key regulator in the NF-κB signaling pathway. This compound exhibits significant anti-inflammatory activity and is instrumental in researching conditions such as arthritis and other inflammatory diseases. MLN-0415 facilitates the exploration of therapeutic strategies targeting the modulation of inflammatory responses.
  26. IKKβ Inhibitor

    1-Dehydro-[10]-gingerdione functions as a selective inhibitor of IKKβ by targeting its activation loop, leading to the disruption of IKKβ-mediated phosphorylation of IκBα in macrophages stimulated with various agonists. This compound effectively inhibits LPS-induced NF-κB transcriptional activity. 1-Dehydro-[10]-gingerdione holds promise for research into NF-κB-related inflammation and autoimmune disorders.
  27. Vasodilator

    (Z)-11,12-Epoxyeicosatrienoic acid acts as a potent vasodilator, primarily targeting small renal arteries. This compound exhibits anti-inflammatory properties by inhibiting leukocyte adhesion to the vascular wall through modulation of the NF-κB signaling pathway and IκB kinase (IKK) activity. It is suitable for research applications focused on vascular inflammation and related cardiovascular studies.
  28. IkappaB kinase inhibitor

    CGA-JK3 is an ATP-competitive inhibitor of IκB kinase (IKKβ), effectively hindering its kinase activity. This compound inhibits the phosphorylation of IκBα in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells, demonstrating its potential in studying inflammatory signaling pathways. CGA-JK3 is useful for researchers investigating the modulation of NF-κB signaling and related biological processes.
  29. IKKα/β Inhibitor

    GTCpFE is a selective inhibitor of IKKα/β, functioning within the NF-κB signaling pathway. This compound exhibits significant anti-inflammatory properties by preventing the nuclear translocation of the p65 subunit of NF-κB. Additionally, GTCpFE demonstrates targeted anti-cancer stem-like cell activity by impairing mammosphere formation and reducing the CD44+ CD24- immunophenotype associated with aggressive breast cancer. Its dual mechanism positions GTCpFE as a promising agent for both inflammation and cancer research.
  30. Anti-inflammatory Drug

    Sanggenon A is an anti-inflammatory compound that modulates the NF-κB and HO-1/Nrf2 signaling pathways, demonstrating significant effects in BV2 and RAW264.7 cells. This reagent effectively inhibits the lipopolysaccharide (LPS)-induced production of nitric oxide, making it a valuable tool for research into inflammatory processes and potential therapeutic applications in inflammation-related diseases.
  31. Phenylpropanoid Glycoside

    Tadehaginoside is a phenylpropanoid glycoside that plays a crucial role in regulating lipogenesis and glucose metabolism. This compound exhibits antioxidant properties and offers hepatoprotective effects by modulating Nrf2 and NF-κB signaling pathways, thereby mitigating oxidative stress and inflammation in liver cells. Tadehaginoside is applicable in research focusing on obesity and diabetes, providing insights into metabolic regulation and associated pathologies.
  32. E-isomer of Tadehaginoside

    (E)-Tadehaginoside is the E-isomer of Tadehaginoside, a phenylpropanoid glycoside known for its role in modulating lipogenesis and glucose metabolism. This compound exhibits antioxidant properties and provides liver protection against oxidative stress and inflammation by influencing the Nrf2 and NF-κB signaling pathways in hepatocytes. (E)-Tadehaginoside is suitable for research applications focused on obesity and diabetes.
  33. Antioxidant Agent

    Santamarine is a sesquiterpene lactone that serves as an effective antioxidant agent. It enhances the expression of heme oxygenase-1 (HO-1) through the translocation of nuclear factor erythroid 2–related factor 2 (Nrf2) while inhibiting the production of nitric oxide (NO), prostaglandin E2 (PGE2), tumor necrosis factor-alpha (TNF-α), and interleukin-1 beta (IL-1β) by blocking NF-κB translocation in LPS-stimulated macrophages. Additionally, Santamarine displays anti-photoaging effects by inhibiting the MAPK/AP-1 pathway and promoting TGF-β/Smad signaling in UVA-irradiated human dermal fibroblasts, highlighting its potential for various biological applications.
  34. ITK PROTACs Degrader

    BSJ-05-037 is an ITK PROTACs degrader that efficiently induces the degradation of ITK in T-cell lymphoma cell lines. This compound inhibits the NF-κB/GATA-3 signaling pathway and decreases PLCγ1 phosphorylation, thereby reducing the proliferation of T-cell lymphoma cells. Additionally, BSJ-05-037 enhances the sensitivity of these cancer cells to chemotherapy. In mouse models, it has shown the ability to diminish GATA-3 expression, lower tumor volume, and counteract chemotherapy resistance, making it a valuable tool for research on T-cell lymphoma.
  35. Neuroprotective Agent

    Hericenone C is a neuroprotective agent derived from the mushroom Hericium erinaceus. It has been shown to inhibit lipopolysaccharide (LPS)-induced NRE::Luc luciferase activity, reduce the phosphorylation of p65, and suppress NF-κB signaling pathways. Due to these effects, Hericenone C is useful for research focused on neuroprotection and the modulation of inflammatory responses in neurological disorders.
  36. NF-κB Activator

    NF-κB activator 1 is a potent activator of the NF-κB signaling pathway, exhibiting an EC50 of 0.9 μM. This compound effectively induces the expression of superoxide dismutase (SOD)2 mRNA, contributing to enhanced cellular antioxidant responses. NF-κB activator 1 is valuable for research applications focusing on inflammation, oxidative stress, and related signaling pathways.
  37. Anti-inflammatory agent

    N,N-Dimethylacetamide (DMAc) is an anti-inflammatory agent that primarily inhibits the NF-κB signaling pathway. Its ability to traverse the blood-brain barrier and function as an FDA-approved drug excipient enhances its utility in various research contexts. DMAc is particularly relevant for investigating the mechanisms of weight gain related to high-fat diets and exploring neuroinflammation associated with Alzheimer's disease.
  38. 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.
  39. 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.
  40. Gibberellin

    Gibberellin A4 is a bioactive gibberellin that primarily targets gibberellin receptors, promoting flowering in apple trees. Additionally, it demonstrates anti-NF-κB and antioxidant activities, making it valuable in studies investigating inflammatory pathways. Gibberellin A4 is also applicable in research focused on periodontal diseases, contributing to the understanding of plant and human health interactions.
  41. NF- B Activator

    NF-κΒ Activator 2 is a potent and orally active NF-κB activator, exhibiting an EC50 of 1.58 μM. This compound enhances the expression and activation of NF-κB, leading to the induction of SOD2. NF-κΒ Activator 2 is useful in researching mechanisms related to amyotrophic lateral sclerosis (ALS) and other conditions associated with NF-κB signaling.
  42. 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.
  43. 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.
  44. 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.
  45. 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).
  46. 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.
  47. 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.
  48. Anti-Oxidative/Inflammatory Agent

    Sulfuretin is a potent anti-oxidative and anti-inflammatory agent that inhibits the NF-κB signaling pathway. It demonstrates efficacy in reducing oxidative stress, platelet aggregation, and mutagenesis, making it relevant for research in allergic airway inflammation. Sulfuretin acts as a competitive inhibitor of monophenolase and diphenolase activities, with an IC50 of 13.64 μM, underscoring its significance in exploring inflammatory responses and oxidative damage in biochemical studies.
  49. 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.
  50. 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.

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