NF-κB/IκB

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  1. 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.
  2. Active Compound

    (-)-Camphoric acid is an active compound known to modulate glutamate receptor expression. It significantly stimulates the activation of key transcription factors NF-κB and AP-1. This compound has been shown to promote the differentiation of mouse osteoblastic MC3T3-E1 cells, highlighting its potential in osteogenesis research. Additionally, (-)-Camphoric acid can induce the mRNA expression of glutamate signaling molecules, further supporting its role in osteoblast differentiation and related biological pathways.
  3. 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.
  4. 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.
  5. 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.
  6. 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.
  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. 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.
  11. 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.
  12. 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.
  13. 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.
  14. 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.
  15. 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.
  16. 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.
  17. 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).
  18. 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.
  19. 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.
  20. 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.
  21. 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.
  22. Anti-inflammatory Agent

    11-Keto-beta-boswellic acid is a pentacyclic triterpenic acid derived from the oleogum resin of the Boswellia serrata tree, commonly known as Indian Frankincense. This compound exhibits significant anti-inflammatory activity through the inhibition of 5-lipoxygenase (5-LOX), which subsequently reduces leukotriene synthesis and attenuates nuclear factor-kappa B (NF-κB) activation, along with the production of tumor necrosis factor alpha. Due to its mechanism of action, 11-Keto-beta-boswellic acid is of interest in studies focused on inflammation-related conditions.
  23. Q8

    CysLt1 Antagonist

    Q8 is a potent CysLt1 antagonist with an IC50 of 4.9 μM. This compound effectively inhibits angiogenesis by reducing cellular levels of NF-κB and calpain-2. Additionally, Q8 decreases the secretion of proangiogenic proteins such as intercellular adhesion molecule-1, vascular cell adhesion protein-1, and VEGF, making it valuable for research in cancer and vascular biology.
  24. Stable Isotope

    Tolterodine-d14 hydrochloride is a deuterium-labeled version of Tolterodine hydrochloride, a potent muscarinic acetylcholine receptor (mAChR) inhibitor. This compound competitively binds to acetylcholine, thereby reducing involuntary bladder muscle contractions and modulating sympathetic nervous activity. In addition to its role in managing overactive bladder and urinary tract infections, Tolterodine has been shown to restore the Nrf2/NF-κB signaling pathway, offering protective effects against inflammation and ferroptosis. Its applications extend to studies involving reactive oxygen species and lipid oxidation.
  25. 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.
  26. 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.
  27. 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.
  28. 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.
  29. 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.
  30. 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.
  31. 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.
  32. 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.
  33. 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.
  34. 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.
  35. 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.
  36. 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.
  37. 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.
  38. Chalcone

    4'-Hydroxychalcone is a chalcone derivative known for its hepatoprotective properties. It exerts its biological activity by inhibiting TNFα-induced NF-κB activation through the modulation of the proteasome. Additionally, 4'-Hydroxychalcone has been shown to induce rapid potassium release from mitochondrial vesicles, adversely affecting respiratory control and oxidative phosphorylation in isolated rat liver mitochondria. This compound is valuable for research focused on liver protection and mitochondrial function.
  39. Stable Isotope

    Metaxalone-d3 is a deuterium-labeled form of Metaxalone, an FDA-approved muscle relaxant primarily acting on the central nervous system. Its primary mechanism involves inhibition of polysynaptic reflex arcs, promoting muscle relaxation. Additionally, Metaxalone demonstrates inhibitory effects on MAO-A, contributing to its anti-inflammatory and antioxidant properties. This reagent is useful for research applications investigating inflammatory responses, as it modulation of IL-1β-induced phenotypes impacts NF-κB and related signaling pathways in microglia.
  40. Stable Isotope

    Metaxalone-d6 is a deuterium-labeled analog of Metaxalone, an FDA-approved muscle relaxant primarily targeting the central nervous system. It promotes muscle relaxation by inhibiting polysynaptic reflex arcs and also exhibits activity as an inhibitor of MAO-A, contributing to anti-inflammatory and antioxidant effects. Metaxalone effectively reduces the IL-1β-induced inflammatory phenotype, modulates NF-κB signaling pathways, and lowers both expression and activity of MAO-A in IL-1β-treated microglia, making it a valuable tool for research in neurobiology and inflammation.
  41. 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.
  42. 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.
  43. 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.
  44. 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.
  45. 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.
  46. 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.
  47. 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.
  48. 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.
  49. Vitamin K2

    Geranylgeraniol is an orally active vitamin K2 precursor that functions as an intermediate in the mevalonate pathway. It primarily targets the NF-kB signaling pathway, demonstrating the potential to reduce LPS-induced microglial inflammation in animal models. This compound is valuable for research investigating neuroinflammation and the broader implications of vitamin K2 in cellular signaling and immune responses.
  50. 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.

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