1. NF-κB
  2. NF-κB

NF-κB

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.

View NF-κB Pathway Map

NF-κB Isoform Specific Products:

  • NF-κB

  • NF-κB1/p50

  • RelA/p65

NF-κB Related Products (71):

Cat. No. Product Name Effect Purity
  • HY-13453
    BAY 11-7082 Inhibitor 99.42%
    BAY 11-7082 is a NF-κB inhibitor. BAY 11-7082 results in decreased NF-κB by inhibiting TNF-α-induced phosphorylation of IκB-α. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 with an IC50 of 0.19 μM and 0.96 μM, respectively.
  • HY-18738
    Pyrrolidinedithiocarbamate ammonium Inhibitor 99.61%
    Pyrrolidinedithiocarbamate ammonium is a selective NF-κB inhibitor.
  • HY-P0151
    SN50 Inhibitor
    SN50 is a cell permeable inhibitor of NF-κB translocation. Sequence: Ala-Ala-Val-Ala-Leu-Leu-Pro-Ala-Val-Leu-Leu-Ala-Leu-Leu-Ala-Pro-Val-Gln-Arg-Lys-Arg-Gln-Lys-Leu-Met-Pro.
  • HY-32735
    Triptolide Inhibitor 99.83%
    Triptolide is a diterpenoid triepoxide extracted from the root of Tripterygium wilfordii with immunosuppressive, anti-inflammatory and antiproliferative effects. Triptolide is a NF-κB activation inhibitor.
  • HY-13982
    JSH-23 Inhibitor 99.10%
    JSH-23 is an NF-κB inhibitor which inhibits NF-κB transcriptional activity with an IC50 of 7.1 μM.
  • HY-N2065
    Withaferin A Inhibitor 99.68%
    Withaferin A is a steroidal lactone isolated from Withania somnifera, inhibits NF-kB activation and targets vimentin, with potent antiinflammatory and anticancer activities.
  • HY-N0773
    Isovitexin Inhibitor 98.94%
    Isovitexin is a flavonoid isolated from rice hulls of Oryza sativa, possesses anti-inflammatory and anti-oxidant activities; Isovitexin acts like a JNK1/2 inhibitor and inhibits the activation of NF-κB.
  • HY-N0436
    Engeletin Inhibitor 98.88%
    Engeletin is a flavanonol glycoside isolated from hymenaea martiana, inhibits NF-κB signaling-pathway activation, and possesses anti-inflammatory, analgesic, diuresis, detumescence, and antibiosis effects.
  • HY-N0822
    Shikonin Inhibitor 99.64%
    Shikonin is an inhibitor of TMEM16A chloride channel with an IC50 of 6.5 μM. Shikonin is also a specific inhibitor of PKM2 and can also inhibit tumor necrosis factor-α (TNF-α) and prevent activation of nuclear factor-κB (NF-κB) pathway.
  • HY-10257
    BAY 11-7085 Inhibitor 98.84%
    BAY 11-7085 is an inhibitor of NF-κB activation and phosphorylation of IκBα; it stabilizes IκBα with an IC50 of 10 μM.
  • HY-19356
    Rocaglamide Inhibitor
    Rocaglamide is a potent NF-κB activation inhibitor.
  • HY-N0176
    Dihydroartemisinin Inhibitor >99.0%
    Dihydroartemisinin is a potent anti-malaria agent.
  • HY-14645
    (-)-DHMEQ Inhibitor 98.05%
    (–)-DHMEQ is a potent NF-κB inhibitor.
  • HY-N2149
    Tomatidine Inhibitor >98.0%
    Tomatidine acts as an anti-inflammatory agent by blocking NF-κB and JNK signaling.
  • HY-13812
    QNZ Inhibitor 98.46%
    QNZ shows strong inhibitory effects on NF-κB transcriptional activation and TNF-α production with IC50s of 11 and 7 nM, respectively. EVP4593 is a neuroprotective inhibitor of SOC channel.
  • HY-N0197
    Baicalin Inhibitor 98.01%
    Baicalin is a flavonoid glycoside isolated from Scutellaria baicalensis. Baicalin reduces the expression of NF-κB.
  • HY-14655
    Sulfasalazine Inhibitor 99.42%
    Sulfasalazine is a drug for the treatment of rheumatoid arthritis and ulcerative colitis. Sulfasalazine is reported to suppress NF-κB activity.
  • HY-N0141
    Parthenolide Inhibitor 99.13%
    Parthenolide is an NF-κB inhibitor, reduces histone deacetylase 1 (HDAC-1) and DNA methyltransferase 1 independent of NF-κB inhibition.
  • HY-13010
    Laquinimod Inhibitor 99.84%
    Laquinimod is a potent immunomodulator which prevents neurodegeneration and inflammation in the central nervous system.
  • HY-N0603
    Ginsenoside Rg3 Inhibitor >98.0%
    Ginsenoside Rg3 is the main component of Red ginseng. Ginsenoside Rg3 inhibits Na+ and hKv1.4 channel with IC50s of 32.2±4.5 and 32.6±2.2 μM, respectively. Ginsenoside Rg3 also inhibits levels, NF-κB activity, and COX-2 expression.
nf-kappa-b-map.png

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.

Isoform Specific Products

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