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-163478
    TNIK-IN-9
    Inhibitor
    TNIK-IN-9 (Compound 54) is a selective and potent NIK inhibitor, with an IC50 of 1.27 nM. TNIK-IN-9 can inhibit pro-inflammatory cytokines and nitric oxide production. TNIK-IN-9 exhibits significant anti-inflammatory effects, improved mortality, and hepatoprotective effects in sepsis models.
    TNIK-IN-9
  • HY-N0015R
    Astragalin (Standard)
    Inhibitor
    Astragalin (Standard) is the analytical standard of Astragalin. This product is intended for research and analytical applications. 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 (Standard)
  • HY-B0289S
    Erdosteine-13C4
    Inhibitor
    Erdosteine-13C4 is a 13C-labeled Erdosteine. Erdosteine inhibits lipopolysaccharide (LPS)-induced NF-κB activation. Erdosteine has muco-modulatory, anti-bacterial, anti-inflammatory and anti-oxidant effects.
    Erdosteine-<sup>13</sup>C<sub>4</sub>
  • HY-N0017R
    Bergenin (Standard)
    Bergenin (Standard) is the analytical standard of Bergenin. This product is intended for research and analytical applications. 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 (Standard)
  • HY-149351
    NF-κB-IN-10
    Inhibitor
    NF-κB-IN-10 (compound E1) is an NF-κB inhibitor that can improve heart failure by reducing oxidative stress and inflammation by regulating Nrf2/NF-κB signaling pathway. NF-κB-IN-10 inhibits LPS-induced NO production and expression of iNOS and COX-2 in RAW264.7 cells. NF-κB-IN-10 can be used in the research of cardiovascular diseases.
    NF-κB-IN-10
  • HY-15027S2
    5-Aminosalicylic acid-13C6
    5-Aminosalicylic acid-13C6 is the 13C labeled 5-Aminosalicylic Acid. 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.
    5-Aminosalicylic acid-<sup>13</sup>C<sub>6</sub>
  • HY-N1380S
    Guaiacol-d7
    Guaiacol-d7 is the deuterium labeled Guaiacol. Guaiacol, a phenolic compound, inhibits LPS-stimulated COX-2 expression and NF-κB activation. Anti-inflammatory activity.
    Guaiacol-d<sub>7</sub>
  • HY-168207
    TH023
    Inhibitor
    TH023 is an inhibitor for the TLR4 signaling pathway, that targets especially the formation of TLR4 homodimer. TH023 inhibits secreted embryonic alkaline phosphatase in cell HEK-Blue hTLR4 with an IC50 of 0.354 μM, and inhibits the NO expression in RAW264.7 with an IC50 of 1.61μM. TH023 also inhibits the activation of NF-κB, reduces the nuclear translocation of NF-κB p65. TH023 exhibits anti-inflammatory efficacy in LPS (HY-D1056)-induced mouse acute sepsis model, and ameliorates the mouse lung injury.
    TH023
  • HY-P10972
    GIP (22-51) human
    Activator
    GIP (22-51) human (Glucose-dependent Insulinotropic Peptide (22-51) human) is a potent proatherosclerotic peptide hormone consisting of 30 amino acids. GIP (22-51) human can activate the NF-κB signaling pathway, promote the expression of MMP-8, and induce the expression of proinflammatory and proatherosclerotic proteins. GIP (22-51) human can also increase the level of intracellular free Ca2+ in THP-1-induced macrophages. GIP (22-51) human can be used in the research of atherosclerosis.
    GIP (22-51) human
  • HY-146421
    Anti-inflammatory agent 21
    Inhibitor
    Anti-inflammatory agent 21 (compound 9o) is an orally active and low cytotoxic anti-inflammatory agent, with an IC50 value of 0.76 μM for NO. Anti-inflammatory agent 21 acts via accumulation ROS and blocks the NF-κB/MAPK signaling pathway. Anti-inflammatory agent 21 can ameliorate cartilage destruction and inflammatory cell infiltration in arthritis rats model.
    Anti-inflammatory agent 21
  • HY-P10081
    CTP-NBD
    Inhibitor
    CTP-NBD is a cell permeable specific NFκB peptide inhibitor. CTP-NBD could be used in colitis study
    CTP-NBD
  • HY-P1847
    IKKγ NBD Inhibitory Peptide
    IKKγ NBD Inhibitory Peptide is a highly specific inhibitor NF-κB inhibitor. IKKγ NBD Inhibitory Peptide acts by disrupting the interaction between IKKγ/NEMO-binding domain (NBD) with IKKα and IKKβ, thus blocking TNF-α-induced NF-kB activation. IKKγ NBD Inhibitory Peptide could significantly suppresses inflammation and ameliorate the cerebral ischemia-induced neurological deficits.
    IKKγ NBD Inhibitory Peptide
  • HY-NP018
    Bovine fibrinogen (from plasma)
    Activator
    Bovine fibrinogen (from fibrinogen) is a native fibrinogen from bovine plasma. Bovine fibrinogen (from fibrinogen) can regulate the activation of NF-KB in endothelial cells and upregulate the expression of inflammatory chemokines MCP-1.
    Bovine fibrinogen (from plasma)
  • HY-78131BS
    (R)-(-)-Ibuprofen-d3
    Inhibitor 99.97%
    (R)-(-)-Ibuprofen-d3 is the deuterium labeled (R)-(-)-Ibuprofen. (R)-(-)-Ibuprofen is the R enantiomer of Ibuprofen, inactive on COX, inhibits NF-κB activation; (R)-(-)-Ibuprofen exhibits anti-inflammatory and antinociceptive effects.
    (R)-(-)-Ibuprofen-d<sub>3</sub>
  • HY-N0908R
    Ginsenoside Rg5 (Standard)
    Inhibitor
    Ginsenoside Rg5 (Standard) is the analytical standard of Ginsenoside Rg5. This product is intended for research and analytical applications. Ginsenoside Rg5 is the main component of Red ginseng and IGF-1R agonist. Ginsenoside Rg5 compets for the binding site of IGF-1R and blocks the binding of IGF-1 to IGF-1R (IC50 about 90 nM). Ginsenoside Rg5 also inhibits the mRNA expression of COX-2 via suppression of the DNA binding activities of NF-κB p65.
    Ginsenoside Rg5 (Standard)
  • HY-N0608A
    (Rac)-Myrislignan
    Inhibitor ≥99.0%
    (Rac)-Myrislignan is the racemate of Myrislignan. Myrislignan, a lignan isolated from Myristica fragrans Houtt, possesses anti-inflammatory activities. Myrislignan attenuates LPS-induced inflammation reaction in murine macrophage cells through inhibition of NF-kB signalling pathway activation.
    (Rac)-Myrislignan
  • HY-155646
    Anti-inflammatory agent 48
    Inhibitor
    Anti-inflammatory agent 48 is an anti-inflammatory agent based on its role in inhibiting the NF-κB signaling pathway and activating HO-1 expression.
    Anti-inflammatory agent 48
  • HY-121239
    Lemnalol
    Modulator
    Lemnalol is a potent agent for neuropathic pain. Lemnalol possesses potent anti-inflammatory, analgesic and anti-tumor activities. Lemnalol has the capacity to attenuate hyperalgesia and allodynia by modulation of neuroinflammatory processes in neuropathy. Lemnalol modulates LPS-induced alterations of left atrial (LA) calcium homeostasis and blocks the NF-κB pathways, which may contribute to the attenuation of lipopolysaccharide (LPS)-induced arrhythmogenesis and neuropathic pain. Lemnalolis a ylangene-type sesquiterpenoid compound, isolated from Lemnalia cervicorni.
    Lemnalol
  • HY-111024R
    2,2,5,7,8-Pentamethyl-6-Chromanol (Standard)
    Inhibitor
    2,2,5,7,8-Pentamethyl-6-Chromanol (Standard) is the analytical standard of 2,2,5,7,8-Pentamethyl-6-Chromanol. This product is intended for research and analytical applications. 2,2,5,7,8-Pentamethyl-6-Chromanol (PMC) is the anti-oxidant moiety of vitamin E (α-tocopherol). 2,2,5,7,8-Pentamethyl-6-Chromanol has potent androgen receptor (AR) signaling modulation and anti-cancer activity against prostate cancer cell lines[1].
    2,2,5,7,8-Pentamethyl-6-Chromanol (Standard)
  • HY-B1640S
    Ethacrynic acid-13C2,d5
    Ethacrynic acid-13C2,d5 is the deuterium and 13C labeled Ethacrynic acid.
    Ethacrynic acid-<sup>13</sup>C<sub>2</sub>,d<sub>5</sub>
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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