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-N5142
    α-Terpineol
    		Inhibitor 99.47%
    α-Terpineol (with oral activity) can be found in Eucalyptus globulus Labill. α-Terpineol exhibits strong antimicrobial activity against periodontopathic and cariogenic bacteria.α-Terpineol possesses antifungal activity against T. mentagrophytes, and the activity might lead to irreversible cellular disruption. In addition, α-Terpineol exhibits antineuropathic and anti-inflammatory activities. α-Terpineol can be utilized in research related to diarrhea, neuropathic pain, infections, and inflammation.
    α-Terpineol
  • HY-101364A
    CHPG sodium salt
    		Activator 99.25%
    CHPG sodium salt is a selective mGluR5 agonist, and attenuates SO2-induced oxidative stress and inflammation through TSG-6/NF-κB pathway in BV2 microglial cells. CHPG sodium salt protects against traumatic brain injury (TBI) in vitro and in vivo by activation of the ERK and Akt signaling pathways..
    CHPG sodium salt
  • HY-W040055
    Neopterin
    		Inhibitor 99.84%
    Neopterin is an immune system activator metabolized by GTP and can be produced by activated macrophages. Neopterin has the potential to resist vascular inflammation and atherosclerosis. Neopterin inhibits the phosphorylation of NF-κB and promotes the expression of PPAR-γ, thereby suppressing the inflammatory response of vascular endothelial cells, reducing the formation of macrophage foam cells, and regulating the migration and proliferation of vascular smooth muscle cells. Neopterin can be used in research fields such as cardiovascular diseases (such as atherosclerosis), inflammation-related diseases and tumor immunomonitoring.
    Neopterin
  • HY-133987
    AP-1/NF-κB activation inhibitor 1
    		Inhibitor 98.08%
    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-B0808
    Oxaprozin
    		Inhibitor 99.94%
    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-Y0148
    10-Hydroxydecanoic acid
    		Inhibitor 98.77%
    10-Hydroxydecanoic acid (10-HDAA) is a saturated fatty acid derived from 10-hydroxy-trans-2-decenoic acid, which can be isolated from royal jelly. 10-Hydroxydecanoic acid exhibits various biological activities, including anti-inflammatory, insecticidal, anti-malarial, and anti-Leishmania properties, as well as enhancing antigen-specific immune responses. The anti-inflammatory effects of 10-Hydroxydecanoic acid are primarily mediated by inhibiting the activation of NF-κB and the translation of interferon regulatory factor 1 (IRF-1), which reduces the production of interleukin 6 (IL-6) and nitric oxide (NO) in inflammatory cells. Additionally, 10-Hydroxydecanoic acid alleviates neuroinflammatory responses through the p53-autophagy pathway and the p53-NLRP3 pathway. Finally, 10-Hydroxydecanoic acid enhances antigen-specific immune responses by promoting the effective uptake of antigens by microfold cells.
    10-Hydroxydecanoic acid
  • HY-N0919
    Yangonin
    		Inhibitor 99.79%
    Yangonin exhibits affinity for the human recombinant cannabinoid CB1 receptor with an IC50 and a Ki of 1.79 μM and 0.72 μM, respectively.
    Yangonin
  • HY-N0668
    Rubusoside
    		Inhibitor 98.58%
    Rubusoside is a diterpene glycoside that is also a sweetener and solubilizer with anti-angiogenic, anti-cancer, anti-obesity, anti-allergic and anti-asthmatic effects. Rubusoside attenuates airway hyperresponsiveness and reduces inflammatory cells in bronchoalveolar lavage fluid (BALF), reducing OVA (HY-W250978)-induced airway inflammation. Rubusoside also prevents palmitic acid-induced lipotoxicity in pancreatic INS-1 cells, reduces the transport of human glucose transporters GLUT-1 and fructose GLUT-5, and inhibits NF-κB and α-amylase (α-amylase).
    Rubusoside
  • HY-N1419
    Vaccarin
    		Inhibitor 98.47%
    Vaccarin is an orally active flavonoid glycoside with multiple biological functions. Vaccarin promotes neovascularization by activating AKT and ERK. Vaccarin activates the AMPK signaling pathway to improve insulin resistance and steatosis. Vaccarin is a MAPK, NF-κB, and NFAT inhibitor, effectively blocking RANKL-induced osteoclastogenesis.
    Vaccarin
  • HY-N0602
    Ginsenoside Rg2
    		Inhibitor 98.11%
    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 Aβ1-42 accumulation.
    Ginsenoside Rg2
  • 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-N0440
    Germacrone
    		Inhibitor 99.76%
    Germacrone is a sesquiterpene compound with multiple biological activities. Germacrone inhibits the H1N1 and H3N2 influenza A virus and the influenza B virus. Germacrone blocks the progressionof arthritis by regulating Th1/Th2 balance and inhibiting NF-κB signaling. Germacrone can arrest the cell cycle at G0/G1 and G2/M phases and induce apoptosis in breast cancer cells. Germacrone inhibits 5α-reductase and has anti-androgenic effect. Germacrone has neuroprotective functions and can be used for the study of traumatic brain injury (TBI). Germacrone also has antioxidant activity.
    Germacrone
  • HY-B0130A
    Perindopril erbumine
    		99.98%
    Perindopril erbumine is an angiotensin-converting enzyme inhibitor. Perindopril erbumine modulates NF-κB and STAT3 signaling and inhibits glial activation and neuroinflammation. Perindopril erbumine can be used for the research of Chronic Kidney Disease and high blood pressure.
    Perindopril erbumine
  • 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-N0231
    Bavachalcone
    		Inhibitor 99.90%
    Bavachalcone is a potent inducer of apoptosis. Bavachalcone exerts anticancer activity by promoting autophagy and apoptosis in HepG2 cells. Bavachalcone acts as an anti-neuroinflammatory and antidepressant through the NF-κB pathway. Bavachalcone inhibits osteoclasts by interfering with ERK and Akt signaling pathways and the expression of c-Fos and NFATc1. Bavachalcone exhibits a significant inhibitory effect on baculovirus-expressed BACE-1 in vitro.
    Bavachalcone
  • HY-124179
    IT-901
    		Inhibitor 99.32%
    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-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 99.89%
    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
  • HY-N0726
    Dracorhodin perchlorate
    		Inhibitor 99.14%
    Dracorhodin perchlorate (Dracohodin perochlorate) is a natural product that can be obtained from the natural active molecule Dragon's blood. Dracorhodin perchlorate inhibits PI3K/Akt and NF-κB activation, upregulates p53 expression, activates caspase, produces ROS, and promotes Apoptosis. Dracorhodin perchlorate regulates the TLR4. Dracorhodin perchlorate promotes wound healing, improves diabetes. Dracorhodin perchlorate has anti-tumor activity against prostate cancer, breast cancer, cervical cancer and other cancers.
    Dracorhodin perchlorate
  • HY-N5063
    Plantainoside D
    		Inhibitor 99.92%
    Plantainoside D, a phenylethanoid glycosides, is a IKK-β inhibitor with diverse biological activities. Plantainoside D shows inhibitory activity of angiotensin-converting enzyme (ACE) with an IC50 of 2.17 mM. Plantainoside D significantly reduces the release of glutamate from nerve terminals in the cerebral cortex of rats by inhibiting the voltage-dependent calcium channel (VDCCs) and protein kinase C (PKC) signaling cascade. Plantainoside D significantly alleviates cell apoptosis by inhibiting the generation of ROS and the activation of b>NF-κB. Plantainoside D significantly improves acute lung injury (ALI) induced by sepsis by regulating the Sirt3/NLRP3 signaling pathway. Plantainoside D can be used for the study of neuroprotection, antioxidant, anti-inflammation, antihypertension.
    Plantainoside D
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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