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

NF-κB

Nuclear factor-κB; Nuclear factor-kappaB

NF-κB

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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.

NF-κB Isoform Specific Products:

NF-κB Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-P0151
    SN50
    		Inhibitor 99.62%
    SN50 is a cell permeable inhibitor of NF-κB translocation.
    SN50
  • HY-N0015
    Astragalin
    		Inhibitor 99.94%
    Astragalin (Astragaline) a flavonoid with anti-inflammatory, antioxidant, anticancer, bacteriostatic activity. Astragalin inhibits cancer cells proliferation and migration, induces apoptosis. Astragalin is orally active and provides nerve and heart protection, and resistance against and osteoporosis.
    Astragalin
  • HY-N0787
    Cryptochlorogenic acid
    		Inhibitor 99.87%
    Cryptochlorogenic acid (4-Caffeoylquinic acid) is a naturally occurring phenolic acid compound with oral effectiveness, anti-inflammatory, antioxidant and anti-cardiac hypertrophy effects. Alleviating LPS (HY-D1056) and ISO (HY-B0468) by regulating proinflammatory factor expression, inhibiting NF-κB activity, promoting Nrf2 nuclear transfer, and regulating PI3Kα/Akt/ mTOR / HIF-1α signaling pathway Induced physiological stress response.
    Cryptochlorogenic acid
  • HY-P9928
    Alirocumab
    Alirocumab is an anti-PCSK9 human monoclonal antibody. Alirocumab inhibits PCSK9. Alirocumab reduces NLRP3 inflammasome, regulates Nrf2/HO-1, HMGB1/NF-κB and Fractalkine/CX3CR1. Alirocumab increases the ability of the liver to bind LDL-cholesterol (LDL-C) and reduces levels of LDL-C in blood. Alirocumab improves atherosclerosis and inflammation.
    Alirocumab
  • HY-N0773
    Isovitexin
    		Inhibitor 99.90%
    Isovitexin is a flavonoid isolated from passion flower, Cannabis and, and the palm, possesses anti-inflammatory and anti-oxidant activities; Isovitexin acts like a JNK1/2 inhibitor and inhibits the activation of NF-κB.
    Isovitexin
  • HY-14654R
    Aspirin (Standard)
    		Inhibitor
    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-P3229
    SN52
    		Inhibitor 99.31%
    SN52 is a potent, competitive, and cell-permeable inhibitor of NF-κB2. SN52 is a variant of the SN50 peptide and inhibits the nuclear translocation of p52-RelB heterodimers. SN52 has a strong radiosensitization effect on prostate cancer cells. SN52 can be used for cancer research.
    SN52
  • HY-152860
    Darizmetinib
    		Activator 99.94%
    Darizmetinib (HRX-0215) is an orally active, potent and selective inhibitor of mitogen-activated protein kinase kinase 4 (MKK4). Darizmetinib leads to enhancement of the MKK7 and JNK1 signaling pathways, thereby activating the transcription factors ATF2 and ELK1, promoting cell proliferation and liver regeneration. Darizmetinib is promising for research of preventing liver failure after extensive oncological liver resections or transplantation of small liver grafts.
    Darizmetinib
  • HY-109017
    Vamorolone
    		Inhibitor 99.96%
    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-N0722
    Neochlorogenic acid
    		Inhibitor 99.80%
    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-P99673
    Itepekimab
    		Inhibitor 99.496%
    Itepekimab (REGN-3500) is an IgG4 monoclonal antibody against IL-33. Itepekimab reduced airway inflammation and related tissue damage in preliminary clinical studies. Itepekimab has potential effects in asthma, chronic obstructive pulmonary disease (COPD), and atopic dermatitis (AD).
    Itepekimab
  • HY-17473
    Embelin
    		Inhibitor 99.01%
    Embelin (Embelic acid), a potent, nonpeptidic XIAP inhibitor (IC50=4.1 μM), inhibits cell growth, induces apoptosis, and activates caspase-9 in prostate cancer cells with high levels of XIAP. Embelin blocks NF-kappaB signaling pathway leading to suppression of NF-kappaB-regulated antiapoptotic and metastatic gene products. Embelin also induces autophagic and apoptotic cell death in human oral squamous cell carcinoma cells.
    Embelin
  • HY-126307
    Urolithin B
    		Inhibitor 99.85%
    Urolithin B is one of Ellagitannins' slow microbial products, and has anti-inflammatory and anti-inflammatory effects. Urolithin B suppresses NF-κB activity. Urolithin B suppresses JNK, ERK and Akt's oxidation, and increases AMPK's oxidation. Urolithin B is also a quantitative change factor for bone and skin quality.
    Urolithin B
  • HY-P1439
    RS 09
    		Activator 99.88%
    RS 09 is an LPS (HY-D1056) peptide mimic and TLR4 agonist. RS 09 can bind to TLR-4 and activate NF-κB. RS 09 can function as an adjuvant in vivo, enhancing the antigen-specific immune response.
    RS 09
  • HY-B0185A
    Lidocaine hydrochloride
    		Inhibitor 99.84%
    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-100507
    Avadomide
    		Inhibitor 99.56%
    Avadomide is an orally active cereblon modulator. Avadomide modulates cereblon E3 ligase activity, inhibits NF-κB pathway, arrests the cell cycle at G1 phase, and thus induces apoptosis in cancer cell PDAC. Avadomide exhibits potent antitumor and immunomodulatory activities.
    Avadomide
  • HY-P1956A
    Human serum albumin (Cell culture grade, Endotoxin<0.125 EU/mg)
    		Inhibitor 99.60%
    Human serum albumin (Cell culture grade, Endotoxin<0.125 EU/mg) (HSA) is the most abundant protein in plasma and is a major determinant of plasma oncotic pressure. Human serum albumin (Cell culture grade, Endotoxin<0.125 EU/mg) exhibits antioxidant, anticoagulant, anti-inflammatory, anti-platelet aggregation activities as well as colloid osmotic action. Human serum albumin (Cell culture grade, Endotoxin<0.125 EU/mg) can block the inhibitory effect of GML on human T cells, providing protective function for T cells. Human serum albumin (Cell culture grade, Endotoxin<0.125 EU/mg) is also associated with cardiovascular diseases and can partially prevent the LPS (HY-D1056) induced oxidative stress, as well as the upregulation of NF-κB, iNOS, and peroxynitrite (ONOO−) in the vascular wall, contributing to the reduction of blood pressure. Human serum albumin (Cell culture grade, Endotoxin<0.125 EU/mg) can be used for in vitro cell culture.
    This product is human serum albumin recombinantly expressed in an Escherichia coli expression system.
    Human serum albumin (Cell culture grade, Endotoxin<0.125 EU/mg)
  • HY-B0008
    Sulindac
    		Inhibitor 99.68%
    Sulindac (MK-231) is an orally active nonsteroidal anti-inflammatory agent. Sulindac also is an immunomodulatory agent. Sulindac can be used for the research of arthritis of the spine, gouty arthritis and kinds of cancer including colorectal cancer (CRC) and lung cancer.
    Sulindac
  • HY-N0509
    Astilbin
    		Inhibitor 99.80%
    Astilbin is a flavonoid compound and enhances NRF2 activation. Astilbin also suppresses TNF-α expression and NF-κB activation.
    Astilbin
  • HY-N0044
    Ginsenoside Re
    		Inhibitor 99.92%
    Ginsenoside Re (Ginsenoside B2) is an extract from Panax notoginseng. Ginsenoside Re decreases the β-amyloid protein (Aβ). Ginsenoside Re plays a role in antiinflammation through inhibition of JNK and NF-κB.
    Ginsenoside Re
Cat. No. Product Name / Synonyms Application Reactivity
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Download NF-κB Signaling Pathway Map.

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.

NF-κB Isoform Comparison

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