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-W011474
    Geranylgeraniol
    Inhibitor 99.18%
    Geranylgeraniol is an orally acitve vitamin K2 sub-type, an intermediate of the mevalonate pathway. Geranylgeraniol targets NF-kB signaling pathway and could alleviate LPS-induced microglial inflammation in animal model.
    Geranylgeraniol
  • HY-B0185A
    Lidocaine hydrochloride
    Inhibitor 99.96%
    Lidocaine hydrochloride (Lignocaine hydrochloride) inhibits sodium channels involving complex voltage and using dependence. Lidocaine hydrochloride decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride is an amide derivative and a agent to treat ventricular arrhythmia and an effective tumor-inhibitor.
    Lidocaine hydrochloride
  • HY-N0652
    2,3,5,4'-Tetrahydroxystilbene 2-O-β-D-glucoside
    Inhibitor 99.91%
    2,3,5,4'-Tetrahydroxystilbene 2-O-β-D-glucoside isolats from the roots of Polygonaceae species, inhibits the formation of 5-HETE, HHT and thromboxane B2. 2,3,5,4'-Tetrahydroxystilbene 2-O-β-D-glucoside has hypotensive, anti-ageing, anti-inflammatory, hypolipidemic, cardioprotective, and neuroprotective actions.
    2,3,5,4'-Tetrahydroxystilbene 2-O-β-D-glucoside
  • HY-109017
    Vamorolone
    Inhibitor 99.10%
    Vamorolone (VBP15) is a first-in-class, orally active dissociative steroidal anti-inflammatory agent and membrane-stabilizer. Vamorolone improves muscular dystrophy without side effects. Vamorolone shows potent NF-κB inhibition and substantially reduces hormonal effects.
    Vamorolone
  • HY-N0044
    Ginsenoside Re
    Inhibitor 99.22%
    Ginsenoside Re (Ginsenoside B2) is an extract from Panax notoginseng. Ginsenoside Re decreases the β-amyloid protein (). Ginsenoside Re plays a role in antiinflammation through inhibition of JNK and NF-κB.
    Ginsenoside Re
  • HY-N0220
    Dauricine
    Inhibitor 99.91%
    Dauricine, a bisbenzylisoquinoline alkaloid in Menispermum dauricum, possesses anti-inflammatory activity. Dauricine inhibits cell proliferation and invasion, and induces apoptosis by suppressing NF-κB activation in a dose- and time-dependent manner in colon cancer.
    Dauricine
  • HY-14654R
    Aspirin (Standard)
    Inhibitor 99.85%
    Aspirin (Standard) is the analytical standard of Aspirin. This product is intended for research and analytical applications. Aspirin (Acetylsalicylic Acid) is an orally active, potent and irreversible inhibitor of cyclooxygenase COX-1 and COX-2, with IC50 values of 5 and 210 μg/mL, respectively. Aspirin induces apoptosis. Aspirin inhibits the activation of NF-κB. Aspirin also inhibits platelet prostaglandin synthetase, and can prevent coronary artery and cerebrovascular thrombosis.
    Aspirin (Standard)
  • HY-10454
    Delanzomib
    Inhibitor ≥98.0%
    Delanzomib (CEP-18770) is a potent and orally active chymotrypsin-like activity of the proteasome inhibitor with an IC50 of 3.8 nM. Delanzomib inhibits NF-κB activity, induces cancer cell apoptotic, and has strong antiangiogenic and anti-cancer activities.
    Delanzomib
  • HY-N0298
    Stachydrine
    Inhibitor ≥98.0%
    Stachydrine is a major constituent of Chinese herb leonurus heterophyllus sweet used to promote blood circulation and dispel blood stasis. Stachydrine can inhibit the NF-κB signal pathway.
    Stachydrine
  • HY-B2123
    Lactose
    Inhibitor ≥98.0%
    Lactose is a β-galactoside consisting of galactose and glucose residues, the main carbohydrate in mammalian breast milk. Lactose, a macronutrient and an inducer of host innate immune responses, possesses immune modulatory functions.
    Lactose
  • HY-116035
    Nimbolide
    Inhibitor 99.79%
    Nimbolide is a triterpene compound that can be isolated from neem (Azadirachta indica), possesses anticancer and antiproliferative activity. Nimbolide induces tumor cell apoptosis by inhibiting NF-κB and CDK4/CDK6 kinase. Nimbolide suppresses the Wnt, PI3K-Akt, MAPK and JAK-STAT signaling pathways.
    Nimbolide
  • HY-B0167A
    Sodium Salicylate
    Inhibitor 99.93%
    Sodium Salicylate (Salicylic acid sodium salt) inhibits cyclo-oxygenase-2 (COX-2) activity independently of transcription factor (NF-κB) activation. Sodium Salicylate is also a S6K inhibitor.Sodium Salicylate is a NF-κB inhibitor that decreases inflammatory gene expression and improves repair in aged muscle.
    Sodium Salicylate
  • HY-110247
    TRAF-STOP inhibitor 6877002
    Inhibitor 99.67%
    TRAF-STOP inhibitor 6877002, is a selective inhibitor of CD40-TRAF6 interaction, compound VII, shows inhibition of NF-κB activation in RAW cells, extracted from patent WO2014033122A1. TRAF-STOP 6877002 prevents the progression of established atherosclerosis in mice, reduces leukocyte recruitment and reduces macrophage activation; reduces macrophage proliferation in atherosclerotic plaques.
    TRAF-STOP inhibitor 6877002
  • HY-17403
    Manidipine dihydrochloride
    Inhibitor 99.91%
    Manidipine dihydrochloride is a third-generation, lipophilic, orally active and highly vasoselective calcium channel antagonist (IC50 = 2.6 nM in guinea-pig ventricular cells) and acts as an antihypertensive agent. Manidipine effectively reduces blood pressure as well as improving insulin sensitivity, renal protection, and antiatherosclerotic activity. Manidipine also exerts anti-inflammatory activity mediated by NF-κB and antiviral activity against many flavivirus and negative-strand RNA viruses through the inhibition of calcium channel. Manidipine is widely applied to research of cardiovascular, metabolic disease and infection.
    Manidipine dihydrochloride
  • HY-113556
    Sappanone A
    99.58%
    Sappanone A is a homoisoflavanone which exhibits anti-inflammatory effects via modulation of Nrf2 and NF-κB. Sappanone can attenuate allergic airway inflammation in Ovalbumin-induced asthma.
    Sappanone A
  • HY-N0722
    Neochlorogenic acid
    Inhibitor 99.77%
    Neochlorogenic acid is a natural polyphenolic compound found in dried fruits and other plants. Neochlorogenic acid inhibits the production of TNF-α and IL-1β. Neochlorogenic acid suppresses iNOS and COX-2 protein expression. Neochlorogenic acid also inhibits phosphorylated NF-κB p65 and p38 MAPK activation.
    Neochlorogenic acid
  • HY-B0435
    Roxithromycin
    Inhibitor 99.93%
    Roxithromycin (RU-28965) is an orally active semi-synthethic macrolide antibiotic. Roxithromycin inhibits protein biosynthesis in the elongation step by binding to 50S bacterial ribosome. Roxithromycin has antimicrobial, antiproliferative, anti-inflammatory, tumour vasculature inhibiting and lung injury ameliorating effects.
    Roxithromycin
  • HY-N0498
    Nitidine chloride
    Inhibitor 99.75%
    Nitidine chloride, a potential anti-malarial lead compound derived from Zanthoxylum nitidum (Roxb) DC, exerts potent anticancer activity through diverse pathways, including inducing apoptosis, inhibiting STAT3 signaling cascade, DNA topoisomerase 1 and 2A, ERK and c-Src/FAK associated signaling pathway, also has anti-inflammatory activity. Nitidine chloride inhibits LPS-induced inflammatory cytokines production via MAPK and NF-kB pathway.
    Nitidine chloride
  • HY-N6949
    Juglone
    Inhibitor 99.68%
    Juglone (5-hydroxy-1,4-naphthalenedione) is a yellow dye that can be extracted from Juglans regia. Juglone induces apoptosis through the mitochondrial pathway. Juglone has antibacterial and antitumor activity .
    Juglone
  • HY-N0017
    Bergenin
    99.21%
    Bergenin is a cytoprotective and antioxidative polyphenol found in many medicinal plants. Bergenin has a wide spectrum activities such as hepatoprotective, antiinflammatory, immunomodulatory, antitumor, antiviral, and antifungal properties.
    Bergenin
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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