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-14592
    Tectochrysin
    Inhibitor 99.88%
    Tectochrysin (Techtochrysin) is one of the major flavonoids of Alpinia oxyphylla Miquel. Tectochrysin inhibits activity of NF-κB.
    Tectochrysin
  • HY-N0515
    Ophiopogonin D
    Inhibitor 99.54%
    Ophiopogonin D, isolated from the tubers of Ophiopogon japonicus, is a rare naturally occurring C29 steroidal glycoside. Ophiopogonin D is a CYP2J3 inducer that significantly inhibits Ang II induced NF-κB nuclear translocation, IκBα down-regulation, intracellular Ca2+ overload and activation of pro-inflammatory cytokines by increasing the expression of CYP2J2/EETs and PPARα in human umbilical vein endothelial cells (HUVECs). Ophiopogonin D has been used to treat inflammatory and cardiovascular diseases for thousands of years.
    Ophiopogonin D
  • HY-126382
    Hesperidin methylchalcone
    Inhibitor ≥98.0%
    Hesperidin methylchalcone (Hesperidin methyl chalcone) is an orally active flavonoid that has analgesic, anti-inflammatory and antioxidant properties. Hesperidin methylchalcone exhibits vasoprotective activity. Hesperidin methylchalcone inhibits oxidative stress, cytokine production and NF-κB activation. Hesperidin methylchalcone can be used for the research of gout disease.
    Hesperidin methylchalcone
  • HY-N0747
    Oxypeucedanin
    Inhibitor 99.50%
    Oxypeucedanin is a furanocoumarin derivative found in Angelica dahurica. Oxypeucedanin is an orally active PI3K/AKT/NF-κB, MAPK, and ROS inhibitor. Oxypeucedanin induces cell cycle arrest and apoptosis. Oxypeucedanin inhibits hKv1.5 channel currents (IC50: 76 nM). Oxypeucedanin exhibits anticancer, anti-inflammatory, antioxidant and antiarrhythmic activities.
    Oxypeucedanin
  • HY-133987
    AP-1/NF-κB activation inhibitor 1
    Inhibitor 99.03%
    AP-1/NF-κB activation inhibitor 1 is a potent AP-1 and NF-κB mediated transcriptional activation inhibitor (IC50=1 μM), without blocking basal transcription driven by the β-actin promoter. AP-1/NF-κB activation inhibitor 1 has a similar inhibitory effect on the production of IL-2 and IL-8 levels in stimulated cells.
    AP-1/NF-κB activation inhibitor 1
  • HY-B1278
    D-α-Tocopherol acetate
    Inhibitor 98.32%
    D-α-Tocopherol acetate (D-Vitamin E acetate) can be hydrolyzed to d-alpha-tocopherol (VE) and absorbed in the small intestine.
    D-α-Tocopherol acetate
  • HY-148013
    K284-6111
    Inhibitor 99.94%
    K284-6111 is an orally active inhibitor for protein chitinase 3-like 1 (CHI3L1). K284-6111 reduces the expression of inflammatory proteins such as iNOS, COX-2, GFAP, and Iba-1, inhibits β-secretase and NF-κB, and suppresses Aβ production. K284-6111 ameliorates the Aβ1–42-induced mice memory impairment, and can be used in research about Alzheimer’s Diseases.
    K284-6111
  • HY-N0222
    Avicularin
    Inhibitor 99.80%
    Avicularin is an orally active flavonoid. Avicularin inhibits NF-κB (p65), COX-2 and PPAR-γ activities. Avicularin has anti-inflammatory, anti-infectious anti-allergic, anti-oxidant, hepatoprotective, and anti-tumor activities.
    Avicularin
  • HY-N1486
    Ursonic acid
    Inhibitor 98.15%
    Ursolic acid is a naturally occurring triterpenoid that has orally active. Ursolic acid induces the apoptosis of human cancer cells through multiple signaling pathways. Ursolic acid has anti-inflammatory and anticarcinogenic activity.
    Ursonic acid
  • HY-124179
    IT-901
    Inhibitor ≥99.0%
    IT-901 is an orally active and potent NF-κB subunit c-Rel inhibitor with an IC50 of 0.1 μM, 3 μM for NF-κB DNA binding and c-Rel DNA binding, respectively. IT-901, a bioactive naphthalenethiobarbiturate derivative, has the potential for human lymphoid tumors and ameliorate graft-versus-host disease (GVHD).
    IT-901
  • HY-B0808
    Oxaprozin
    Inhibitor 99.95%
    Oxaprozin is an orally active and potent COX inhibitor, with IC50 values of 2.2 μM for human platelet COX-1 and and 36 μM for IL-1-stimulated human synovial cell COX-2, respectively. Oxaprozin also inhibits the activation of NF-κB. Oxaprozin induces cell apoptosis. Oxaprozin shows anti-inflammatory activity. Oxaprozin-mediated inhibition of the Akt/IKK/NF-κB pathway contributes to its anti-inflammatory properties.
    Oxaprozin
  • HY-P1847A
    IKKγ NBD Inhibitory Peptide TFA
    98.20%
    IKKγ NBD Inhibitory Peptide TFA is a highly specific inhibitor NF-κB inhibitor. IKKγ NBD Inhibitory Peptide TFA 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 TFA could significantly suppresses inflammation and ameliorate the cerebral ischemia-induced neurological deficits.
    IKKγ NBD Inhibitory Peptide TFA
  • HY-N2056
    11-​Keto-​beta-​boswellic acid
    Inhibitor 99.96%
    11-Keto-beta-boswellic acid (11-Keto-β-boswellic acid) is a pentacyclic triterpenic acid of the oleogum resin from the bark of the Boswellia serrate tree, popularly known as Indian Frankincense. 11-Keto-beta-boswellic acid has the anti-inflammatory activity is primarily due to inhibit 5-lipoxygenase (5-LOX) and subsequent leukotriene and nuclear factor-kappa B (NF-κB) activation and tumor necrosis factor alpha generation production.
    11-​Keto-​beta-​boswellic acid
  • HY-147972
    NF-κB/MAPK-IN-1
    Inhibitor 98.42%
    NF-κB/MAPK-IN-1 (compound 11a) is a potent inhibitor of NF-κB and MAPK pathway. NF-κB/MAPK-IN-1 shows inhibitory activity against NO production, with an IC50 of 6.96 µM. NF-κB/MAPK-IN-1 suppresses LPS-induced iNOS, COX-2, ERΚ and P38 signaling activation. NF-κB/MAPK-IN-1 can prevent LPS induced inflammatory response in macrophages. NF-κB/MAPK-IN-1 can be used for rheumatoid arthritis (RA) research.
    NF-κB/MAPK-IN-1
  • HY-W015490
    1,4-Naphthoquinone
    Inhibitor 99.97%
    1,4-Naphthoquinone is an inhibitor with broad-spectrum inhibitory activity targeting DNA polymerase, NF-κB and monoamine oxidase (MAO-A/B), with antibacterial and anti-biofilm efficacy. 1,4-Naphthoquinone is a competitive inhibitor of MAO-B (Ki=1.4 μM) and a non-competitive inhibitor of MAO-A (Ki=7.7 μM). 1,4-Naphthoquinone inhibits DNA polymerase pol α, β, γ, δ, ε, λ with IC50 ranging from 5.57-128 μM. 1,4-Naphthoquinone inhibits tumor cell proliferation, induces apoptosis and necrosis, and has anti-angiogenic and anti-inflammatory activities by inducing oxidative stress, depleting glutathione (GSH), inhibiting DNA polymerase-mediated DNA synthesis and blocking NF-κB nuclear translocation. 1,4-Naphthoquinone can be used in anti-bacterial , anti-tumor and anti-inflammatory studies, including inhibition of melanoma and colon cancer cell growth and endothelial cell function, as well as LPS-induced inflammation models.
    1,4-Naphthoquinone
  • HY-N1193
    Sulfuretin
    Inhibitor 99.36%
    Sulfuretin inhibits the inflammatory response by suppressing the NF-κB pathway. Sulfuretin can be used for the research of allergic airway inflammation. Sulfuretin reduces oxidative stress, platelet aggregation, and mutagenesis. Sulfuretin is a competitive and potent inhibitor of monophenolase and diphenolase activities with the IC50 of 13.64 μM.
    Sulfuretin
  • HY-N6031
    Dendrophenol
    Inhibitor 99.93%
    Dendrophenol (Moscatilin) is a NF-κB inhibitor that inhibits inflammation. Dendrophenol exerts potent cytotoxic effect against tumor cells and induces cell cycle arrest and apoptosis. Dendrophenol has antitumor activity. In addition, Dendrophenol can inhibit vascular calcification by inhibiting the activation of WNT3/β-catenin.
    Dendrophenol
  • HY-121389
    Hexadecanamide
    Inhibitor
    Hexadecanamide (Palmitamide), a fatty acid amide, has orally active anti-allergic, antioxidant, and neuroprotective effects. Hexadecanamide alleviate S. aureus-caused mastitis by depressing inflammatory response and maintaining blood-milk barrier integrity. Hexadecanamide depresses S. aureus-induced activation of the NF-κB pathway in mouse mammary epithelial cells (MMECs). Hexadecanamide activates PPARα. Hexadecanamide enhances sperm motility in vitro.
    Hexadecanamide
  • HY-N3021
    D-chiro-Inositol
    Inhibitor ≥98.0%
    D-chiro-Inositol is a stereoisomer of inositol that exhibits activities such as improving glucose metabolism, anti-tumor effects, anti-inflammatory properties, and antioxidant activity. D-chiro-Inositol effectively alleviates cholestasis by enhancing bile acid secretion and reducing oxidative stress. D-chiro-Inositol improves insulin resistance, lowers hyperglycemia and circulating insulin levels, reduces serum androgen levels, and ameliorates some metabolic abnormalities associated with X syndrome by mimicking the action of insulin. Additionally, D-chiro-Inositol can induce a reduction in pro-inflammatory factors (such as Nf-κB) and cytokines (such as TNF-α), thereby exerting anti-inflammatory effects. D-chiro-Inositol may be used in the study of liver cirrhosis, breast cancer, type 2 diabetes, and polycystic ovary syndrome.
    D-chiro-Inositol
  • HY-N0841
    Bruceine A
    Inhibitor 98.01%
    Bruceine A (Dihydrobrusatol) is a natural quassinoid. Bruceine A is an inhibitor of parasites, NF-κB, and PFKFB4 (Kd: 44 nM). Bruceine A is an activator of P38α MAPK. Bruceine A has antiparasitic activity. Bruceine A has antitumor activity and inhibits cancer cell migration. Bruceine A blocks the cell cycle and induces apoptosis. Bruceine A can be used in parasites, pancreatic cancer, and breast cancer research.
    Bruceine A
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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