1. Signaling Pathways
  2. NF-κB
  3. NF-κB

NF-κB

Nuclear factor-κB; Nuclear factor-kappaB

NF-κB (Nuclear factor kappa-light-chain-enhancer of activated B cells) is a protein complex that controls transcription of DNA. NF-κB is found in almost all animal cell types and is involved in cellular responses to stimuli such as stress, cytokines, free radicals, ultraviolet irradiation, oxidized LDL, and bacterial or viral antigens. NF-κB plays a key role in regulating the immune response to infection. Incorrect regulation of NF-κB has been linked to cancer, inflammatory, and autoimmune diseases, septic shock, viral infection, and improper immune development. NF-κB has also been implicated in processes of synaptic plasticity and memory. There are five proteins in the mammalian NF-κB family: NF-κB1, NF-κB2, RelA, RelB, c-Rel.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-N0081
    (±)-Praeruptorin A
    Inhibitor 99.94%
    (±)-Praeruptorin A, a coumarin compound, is the main bioactive component in Peucedani Radix. As a calcium channel blocker, (±)-Praeruptorin A exhibits great antihypertensive effects. In addition, (±)-Praeruptorin A also has the effects of relaxing vascular smooth muscle, inhibiting airway inflammation and airway hyperresponsiveness. (±)-Praeruptorin A can be used for the research of allergic asthma, hypertension and other diseases.
    (±)-Praeruptorin A
  • HY-Y0586
    2,4,5-Trimethoxybenzoic acid
    Inhibitor 99.98%
    2,4,5-Trimethoxybenzoic acid (Asaronic acid) is a compound identified in purple perilla extracts. 2,4,5-Trimethoxybenzoic acid inhibits LPS (HY-D1056)-induced inflammatory responses, inhibits the activation of NF-κB and STAT signaling pathways. 2,4,5-Trimethoxybenzoic acid inhibits M1 macrophage phenotype-mediated inflammation in diabetes.
    2,4,5-Trimethoxybenzoic acid
  • HY-N0176R
    Dihydroartemisinin (Standard)
    Inhibitor
    Dihydroartemisinin (Standard) is the analytical standard of Dihydroartemisinin. This product is intended for research and analytical applications. Dihydroartemisinin is a potent anti-malaria agent.
    Dihydroartemisinin (Standard)
  • HY-N3225
    Myricanol
    Inhibitor ≥98.0%
    Myricanol is a diarylheptanoid and a Nampt activator. Myricanol exerts anti-inflammatory effects and alleviates glucocorticoid-induced muscle atrophy by increasing Sirtuin 1 (SIRT1) and PRDX5 activities while regulating inflammatory factors. Myricanol exhibits growth inhibition and induces apoptosis in human lung adenocarcinoma A549 cells. Myricanol promotes autophagy-mediated clearance of microtubule-associated protein tau to exert neuroprotective effects. Myricanol protects cardiovascular function by inhibiting PDGFRβ and NF-κB signaling pathways. Myricanol activates mitochondrial transcription factor A (TFAM) expression to exert anti-renal fibrosis effects. Myricanol improves insulin resistance through AMPK activation.
    Myricanol
  • HY-N9451
    Ginger extract
    Inhibitor
    Ginger extract exhibits anti-cancer, anti-inflammatory and chemotherapeutic effects in vivo.
    Ginger extract
  • HY-148552
    Anti-inflammatory agent 35
    Inhibitor 99.77%
    Anti-inflammatory agent 35 (compound 5a27) is an orally active curcumin analogue with anti-inflammatory activity. Anti-inflammatory agent 35 blocks mitogen-activated protein kinase (MAPK) signaling and p65 nuclear translocation of NF-kB. Anti-inflammatory agent 35 also inhibits yellow neutrophil infiltration and pro-inflammatory cytokine production. Anti-inflammatory agent 35 significantly attenuates lipopolysaccharide (LPS)-induced acute lung injury (ALI) in vivo.
    Anti-inflammatory agent 35
  • HY-N1956
    Rubiadin-1-methyl ether
    Inhibitor 98.57%
    Rubiadin-1-methyl ether is a natural anthraquinone isolated from Morinda officinalis How, and inhibits osteoclastic bone resorption via inhibition on the phosphorylation of NF-κB p65 and the degradation of IκBα as well as decrease in the nuclear translocation of p65.
    Rubiadin-1-methyl ether
  • HY-N1513
    Ganoderic acid H
    Inhibitor 99.68%
    Ganoderic acid H is a lanostane-type triterpene isolated from Ganoderma lucidum. Ganoderic acid H suppresses growth and invasive behavior of breast cancer cells through the inhibition of transcription factors AP-1 and NF-kappaB signaling.
    Ganoderic acid H
  • HY-N6599
    3-Feruloylquinic acid
    Inhibitor 98.98%
    3-Feruloylquinic acid (3-O-Feruloylquinic acid), a derivative of quinic acid-bound phenolic acid, shows antioxidant and anti-inflammatory activities.
    3-Feruloylquinic acid
  • HY-N1196
    Suberosin
    Inhibitor 99.84%
    Suberosin, isolated from Plumbago zeylanica, exhibits anti-inflammatory and anticoagulant activity. Suberosin suppresses PHA-induced PBMC proliferation and arrested cell cycle progression from the G1 transition to the S phase through the modulation of the transcription factors NF-AT and NF-κB.
    Suberosin
  • HY-101481
    Flurbiprofen axetil
    Inhibitor 99.34%
    Flurbiprofen axetil is a non-selective COX inhibitor and a nonsteroidal anti-inflammatory agent with anti-inflammatory and analgesic effects. Flurbiprofen axetil inhibits basal-like breast cancer metastasis by inhibiting the MEK/ERK signaling pathway. Flurbiprofen axetil can promote neuroprotection after focal cerebral ischemia in rats by partially activating PPAR-γ. Flurbiprofen axetil alleviates cerebral ischemia/reperfusion injury by reducing inflammation in a transient global cerebral ischemia/reperfusion rat model. Flurbiprofen axetil can alleviate inflammatory responses and cognitive function in a mild cognitive impairment (MCI) SD rat model through the AMPKα/NF-κB signaling pathway.
    Flurbiprofen axetil
  • HY-N2041R
    Myristic acid (Standard)
    Activator
    Myristic acid (Standard) is the analytical standard of Myristic acid. This product is intended for research and analytical applications. Myristic acid is an orally active saturated 14-carbon fatty acid found in most animal and plant fats, especially milk fat coconut oil, palm oil and nutmeg oil. Myristic acid exerts anti-inflammatory activity through the NF-κB pathway. Myristic acid has antibacterial, anti-inflammatory and analgesic properties.
    Myristic acid (Standard)
  • HY-N0510A
    Aristolochic acid A sodium
    Inhibitor 99.37%
    Aristolochic acid A (Aristolochic acid I) sodium is the main component of plant extract Aristolochic acids, which are found in various herbal plants of genus Aristolochia and Asarum. Aristolochic acid A sodium significantly reduces both activator protein 1 (AP-1) and NF-κB activities. Aristolochic acid A sodium reduces BLCAP gene expression in human cell lines.
    Aristolochic acid A sodium
  • HY-P990208
    Anti-Mouse IL-9 Antibody (9C1)
    Inhibitor
    Anti-Mouse IL-9 Antibody (9C1) is an anti-mouse IL-9 IgG2a monoclonal antibody. Anti-Mouse IL-9 Antibody (9C1) can reduce the activation of NF-κB signaling pathway and decrease the infiltration of inflammatory cells. Anti-Mouse IL-9 Antibody (9C1) effectively reduces Th9 cell-mediated allergic reactions and anti-tumor effects. Anti-Mouse IL-9 Antibody (9C1) can be used for researches on inflammation, infection conditions and cancer such as parasitic infections, allergic reactions, breast cancer and osteosarcoma.
    Anti-Mouse IL-9 Antibody (9C1)
  • HY-113416R
    Dehydroepiandrosterone sulfate (Standard)
    Inhibitor
    Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) (Standard) is the analytical standard of Dehydroepiandrosterone sulfate (HY-113416). This product is intended for research and analytical applications. Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate has both non-competitive antagonist activity of GABAA receptor and agonist activity of σ1 receptor. Dehydroepiandrosterone sulfate can partially penetrate the blood-brain barrier, inhibit GABAA receptor-mediated chloride influx, enhance NMDA receptor activity through σ1 receptors, exert anti-inflammatory, anti-glucocorticoid and antidepressant effects, and increase convulsive sensitivity. Dehydroepiandrosterone sulfate participates in neuroprotection, neurite growth regulation and catecholamine secretion regulation, and can be used in the study of depression, post-traumatic stress disorder (PTSD), Alzheimer's disease, etc. Dehydroepiandrosterone sulfate may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality.
    Dehydroepiandrosterone sulfate (Standard)
  • HY-W011398
    Linoleate sodium
    99.88%
    Linoleate sodium is an orally active IL8 regulator via the JNK and NF-κB pathway. Linoleate sodium can change the composition of fatty acids and the production of metabolites in cells. Linoleate sodium has anti-inflammatory, immune-regulating, and tumor cell growth-affecting activities.
    Linoleate sodium
  • HY-126818
    Desfuroylceftiofur
    Inhibitor
    Desfuroylceftiofur is an active metabolite of Ceftiofur which is a broad-spectrum cephalosporin antibiotic. Desfuroylceftiofur is active against gram-positive and gram-negative bacteria.
    Desfuroylceftiofur
  • HY-P99635
    Gatralimab
    Inhibitor 99.90%
    Gatralimab (GZ-402668) is an IgG1 anti-CD52 monoclonal antibody.
    Gatralimab
  • HY-N1913A
    Danshensu sodium
    Inhibitor 99.9%
    Danshensu (Dan shen suan A) sodium, an orally active phenolic compound, can induce Nrf2/HO-1 activation and inhibition of NF-κB pathway. Danshensu sodium reduces reactive oxygen species (ROS) production, upregulates antioxidant defense mechanism and inhibits intrinsic apoptotic pathway. Danshensu sodium displays a potent antiviral activity against SARS-CoV-2 with EC50 of 0.97 μM. Danshensu sodium has anti-oxidation, anti-apoptosis, anti-lung inflammatory and has the potential for COVID-19, cardiovascular and cerebrovascular diseases research.
    Danshensu sodium
  • HY-137941
    Roxatidine
    Inhibitor 98.25%
    Roxatidine is an active metabolite of Roxatidine acetate hydrochloride, is an orally active histamine H2-receptor antagonist. Roxatidine, an anti-ulcer agent, suppresses histamine release (thus inhibiting proton secretion) and inhibits the production of VEGF-1, an important marker of inflammation and angiogenesis. Anti-allergic inflammatory effect. Roxatidine is promising for research of gastric and duodenal ulcers.
    Roxatidine
Cat. No. Product Name / Synonyms Application Reactivity

NF-κB transcription factors are critical regulators of immunity, stress responses, apoptosis and differentiation. In mammals, there are five members of the transcription factor NF-κB family: RELA (p65), RELB and c-REL, and the precursor proteins NF-κB1 (p105) and NF-κB2 (p100), which are processed into p50 and p52, respectively. NF-κB transcription factors bind as dimers to κB sites in promoters and enhancers of a variety of genes and induce or repress transcription. NF-κB activation occurs via two major signaling pathways: the canonical and the non-canonical NF-κB signaling pathways[1]

 

The canonical NF-κB pathway is triggered by signals from a large variety of immune receptors, such as TNFR, TLR, and IL-1R, which activate TAK1. TAK1 then activates IκB kinase (IKK) complex, composed of catalytic (IKKα and IKKβ) and regulatory (NEMO) subunits, via phosphorylation of IKKβ. Upon stimulation, the IKK complex, largely through IKKβ, phosphorylates members of the inhibitor of κB (IκB) family, such as IκBα and the IκB-like molecule p105, which sequester NF-κB members in the cytoplasm. IκBα associates with dimers of p50 and members of the REL family (RELA or c-REL), whereas p105 associates with p50 or REL (RELA or c-REL). Upon phosphorylation by IKK, IκBα and p105 are degradated in the proteasome, resulting in the nuclear translocation of canonical NF-κB family members, which bind to specific DNA elements, in the form of various dimeric complexes, including RELA-p50, c-REL-p50, and p50-p50. Atypical, IKK-independent pathways of NF-κB induction also provide mechanisms to integrate parallel signaling pathways to increase NF-κB activity, such as hypoxia, UV and genotoxic stress.

 

The non-canonical NF-κB pathway is induced by certain TNF superfamily members, such as CD40L, BAFF and lymphotoxin-β (LT-β), which stimulates the recruitment of TRAF2, TRAF3, cIAP1/2 to the receptor complex. Activated cIAP mediates K48 ubiquitylation and proteasomal degradation of TRAF3, resulting in stabilization and accumulation of the NFκB-inducing kinase (NIK). NIK phosphorylates and activates IKKα, which in turn phosphorylates p100, triggering p100 processing, and leading to the generation of p52 and the nuclear translocation of p52 and RELB[2][3].

 

Reference:

[1]. Oeckinghaus A, et al. The NF-kappaB family of transcription factors and its regulation.Cold Spring Harb Perspect Biol. 2009 Oct;1(4):a000034. 
[2]. Taniguchi K, et al. NF-κB, inflammation, immunity and cancer: coming of age. Nat Rev Immunol. 2018 May;18(5):309-324.
[3]. Perkins ND,et al. Integrating cell-signalling pathways with NF-kappaB and IKK function. Nat Rev Mol Cell Biol. 2007 Jan;8(1):49-62.

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