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-N1489
    14-Deoxy-11,12-didehydroandrographiside
    Inhibitor
    14-Deoxy-11,12-didehydroandrographiside is a compound isolated from A. paniculate.
    14-Deoxy-11,12-didehydroandrographiside
  • HY-15122AR
    Sinomenine hydrochloride (Standard)
    Inhibitor
    Sinomenine hydrochloride (Standard) is the analytical standard of Sinomenine hydrochloride. This product is intended for research and analytical applications. Sinomenine hydrochloride (Cucoline hydrochloride), an alkaloid extracted from Sinomenium acutum, is a blocker of the NF-κB activation. Sinomenine also is an activator of μ-opioid receptor.
    Sinomenine hydrochloride (Standard)
  • HY-N0250R
    Saikosaponin D (Standard)
    Inhibitor
    Saikosaponin D (Standard) is the analytical standard of Saikosaponin D. This product is intended for research and analytical applications. Saikosaponin D is a triterpene saponin isolated from Bupleurum, with anti-inflammatory, anti-bacterial, anti-tumor, and anti-allergic activities; Saikosaponin D inhibits selectin, STAT3 and NF-kB and activates estrogen receptor-β.
    Saikosaponin D (Standard)
  • HY-N0602R
    Ginsenoside Rg2 (Standard)
    Inhibitor
    Ginsenoside Rg2 (Standard) is the analytical standard of Ginsenoside Rg2. This product is intended for research and analytical applications. Ginsenoside Rg2 is one of the major active components of ginseng. Ginsenoside Rg2 inhibits VCAM-1 and ICAM-1 expressions stimulated with lipopolysaccharide (LPS). Ginsenoside Rg2 also reduces 1-42 accumulation.
    Ginsenoside Rg2 (Standard)
  • HY-163829
    TLR2 agonist 1
    Agonist
    TLR2 agonist 1 (Compound R-7d) is an agonist for human toll-like receptor 2 (TLR 2) with an EC50 of 116 pM. TLR2 agonist 1 enhances NF-κB promoter activation through TLR2/TLR1 heterodimers.
    TLR2 agonist 1
  • HY-N10768
    1-Dehydro-[10]-gingerdione
    Inhibitor
    1-Dehydro-[10]-gingerdione directly inhibits IKKβ activity by targeting the activation loop of IKKβ, thus disrupting IKKβ-catalysed IκBα phosphorylation in macrophages stimulated with agonists. 1-Dehydro-[10]-gingerdione inhibits LPS (HY-D1056)-induced NF-κB transcriptional activity. 1-Dehydro-[10]-gingerdione has the potential for NF-κB-associated inflammation and autoimmune disorders research.
    1-Dehydro-[10]-gingerdione
  • HY-161266
    COX-2/NLRP3-IN-1
    Inhibitor
    COX-2/NLRP3-IN-1 (Compound 6k) is a COX-2/NLRP3 inhibitor with a IC50 of 1.53 μM for COX-2. COX-2/NLRP3-IN-1 exerts anti-inflammatory effects by inhibiting the NF-κB/NLRP3 signaling pathway.
    COX-2/NLRP3-IN-1
  • HY-N6246R
    Asperulosidic Acid (Standard)
    Inhibitor
    Asperulosidic Acid (Standard) is the analytical standard of Asperulosidic Acid. This product is intended for research and analytical applications. Asperulosidic Acid (ASPA), a bioactive iridoid glycoside, is extracted from the herbs of Hedyotis diffusa Willd. Asperulosidic Acid (ASPA) has anti-tumor, anti-oxidant, and anti-inflammatory activities. ASPA is related to the inhibition of inflammatory cytokines (TNF-α, IL-6) and mediators via suppression of the NF-κB and mitogen-activated protein kinase (MAPK) signaling pathways.
    Asperulosidic Acid (Standard)
  • HY-149087
    MR2938
    Inhibitor
    MR2938 is a potent AChE inhibitor, with an IC50 of 5.04 μM. MR2938 also suppresses NO production obviously (IC50 = 3.29 μM). MR2938 suppresses the neuroinflammation through blocking MAPK/JNK and NF-κB signaling pathways. MR2938 can be used for Alzheimer’s disease (AD) research.
    MR2938
  • HY-168482
    NF-κB/MAPK-IN-2
    Inhibitor
    NF-κB/MAPK-IN-2 (compound 14) is a potent NF-κB and MAPK Inhibitor. NF-κB/MAPK-IN-2 decreases the protein expression of p-p65, p-IκB, p-p38, p-JNK, and p-ERK. NF-κB/MAPK-IN-2 reduces the LPS-induced release of TNF-α and IL-6. NF-κB/MAPK-IN-2 inhibits nuclear translocation of p65 and c-Fos. NF-κB/MAPK-IN-2 has the potential for the research of sepsis.
    NF-κB/MAPK-IN-2
  • HY-175674
    NGI-235
    Inhibitor
    NGI-235 is a selective OST-A inhibitor that inhibits NF-κB inflammatory signaling by blocking TLR4 glycosylation.
    NGI-235
  • HY-N0803S
    Myrcene-d6
    Inhibitor
    Myrcene-d6 is the deuterium labeled Myrcene. Myrcene (β-Myrcene) is a type of aromatic compound that inhibits TNFα and NF-κB activity. Myrcene has anti-invasive action, inhibits cell cycle, and leads to cancer cell apoptosis. Myrcene has strong blood protection effect, anti-inflammation, and anti-inflammatory activity.
    Myrcene-d<sub>6</sub>
  • HY-139714
    IMD-vanillin
    Modulator
    IMD-vanillin is a novel imidazoquinolinone-NF-κB immunomodulator dimers.
    IMD-vanillin
  • HY-N12959
    5,4'-Dihydroxy-6,8-dimethoxy-7-O-rhamnosyl flavone
    Inhibitor
    5,4'-Dihydroxy-6,8-dimethoxy-7-O-rhamnosyl flavone (DDR) is an anticancer agent that can be extracted from Indigofera ovata. 5,4'-Dihydroxy-6,8-dimethoxy-7-O-rhamnosyl flavone can inhibit the PI3K/AKT and NF-кB pathways, inhibit the invasion and migration of cancer cells, and has anticancer activity.
    5,4'-Dihydroxy-6,8-dimethoxy-7-O-rhamnosyl flavone
  • HY-N10638
    N-Acetyldopamine dimer-2
    Inhibitor
    N-Acetyldopamine dimer-2 (compound 2) is a N-acetyldopamine dimer that can be isolated from the yellow powder form Periostracum Cicadae with antioxidant and anti-inflammatory activities. N-Acetyldopamine dimer-2 inhibits oxidized low-density lipoprotein (LDL) oxidation, ROS generation, NO production, and NF-κB activity.
    N-Acetyldopamine dimer-2
  • HY-146560
    Xanthine oxidase-IN-6
    Inhibitor
    Xanthine oxidase-IN-6 (Compound 6c) is a potent, orally active, mixed-type xanthine oxidase (XOD) inhibitor with an IC50 value of 1.37 µM. Xanthine oxidase-IN-6 shows strong anti-hyperuricemia and renal protective activity.
    Xanthine oxidase-IN-6
  • HY-N0171AR
    Beta-Sitosterol (purity>98%) (Standard)
    Inhibitor
    Beta-Sitosterol (purity>98%) (Standard) is an analytical standard for Beta-Sitosterol (purity>98%). Beta-Sitosterol (purity>98%) is intended for research and analytical applications. Beta-Sitosterol (purity>98%) is orally active. Beta-Sitosterol exhibits multiple activities, including anti-inflammatory, anticancer, antioxidant, antimicrobial, antidiabetic, antioxidant enzyme, and analgesic. Beta-Sitosterol inhibits inflammation and impaired adipogenesis in bovine mammary epithelial cells by reducing levels of ROS, TNF-α, IL-1β, and NF-κB p65 and restoring the activity of the HIF-1α/mTOR signaling pathway. Beta-Sitosterol induces apoptosis in cancer cells through ROS-mediated mitochondrial dysregulation and p53 activation. Beta-Sitosterol exerts its anticancer effects in cancer cells by activating caspase-3, caspase-8, and caspase-9, mediating PARP inactivation, MMP loss, altered Bcl-2-Bax ratio, and cytochrome c release. Beta-Sitosterol modulates macrophage polarization and reduces rheumatoid inflammation in mice. Beta-Sitosterol inhibits tumor growth in multiple mouse cancer models. Beta-Sitosterol can be used in the research of arthritis, lung cancer, breast cancer and other cancers, diabetes, etc.
    Beta-Sitosterol (purity>98%) (Standard)
  • HY-124281A
    9(S)-PAHSA
    Control
    9(S)-PAHSA is a S-enantiomer of 9-PAHSA. 9-PAHSA is an orally available anti-inflammatory lipid that lowers blood sugar and reduces inflammation.
    9(S)-PAHSA
  • HY-N8263
    Nepetoidin B
    Modulator
    Nepetoidin B, an anti-inflammatory agent, inhibits inflammation by modulating the NF-κB and Nrf2/HO-1 signaling pathways. Nepetoidin B also has antifungal and antibacterial activity. Nepetoidin B is a natural product that can be obtained from Salvia plebeia R. Br. Nepetoidin B can be used in anti-inflammatory and anti-infectious research.
    Nepetoidin B
  • HY-116145
    MHY884
    Inhibitor
    MHY884 is a tyrosinase inhibitor that suppresses UVB-induced activation of NF-κB signaling pathway through the downregulation of oxidative stress. MHY884 suppresses oxidative stress in the melanoma cells and attenuates UVB-induced oxidative stress, resulting in reduced NF-κB activity in irradiated mice. MHY884 is promising for research of UVB-induced skin damage.
    MHY884
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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