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-76006
    3-Hydroxybenzaldehyde
    Inhibitor 99.93%
    3-Hydroxybenzaldehyde (3-HBA) is a precursor compound for phenolic compounds like Protocatechuic aldehyde (PCA) (HY-N0295). 3-Hydroxybenzaldehyde, produced by 3-hydroxybenzyl-alcohol dehydrogenase, is a substrate of aldehyde dehydrogenase (ALDH) in rats and humans. 3-Hydroxybenzaldehyde has vasculoprotective effects in vitro and in vivo. 3-Hydroxybenzaldehyde is proming for research of atherosclerosis.
    3-Hydroxybenzaldehyde
  • HY-N2908
    Atraric acid
    Inhibitor 99.97%
    Atraric acid (Methyl atrarate) is a specific androgen receptor (AR) antagonist with anti-inflammatory and anticancer effects. Atraric acid represses the expression of the endogenous prostate specific antigen gene in both LNCaP and C4-2 cells. Atraric acid can also inhibit the synthesis of NO and cytokine, and suppress the MAPK-NFκB signaling pathway. Atraric acid can be used to research prostate diseases and inflammatory diseases.
    Atraric acid
  • HY-N0617
    Sanggenon C
    Inhibitor 98.46%
    Sanggenon C, a flavonoid, exerts protective effects against cardiac hypertrophy and fibrosis via suppression of the calcineurin/NFAT2 pathway. Sanggenon C inhibits mitochondrial fission to induce apoptosis by blocking the ERK signaling pathway. Sanggenon C inhibits inducible nitric oxide synthase expression in RAW264.7 cells, and TNF-α-stimulated cell adhesion and VCAM-1 expression, by suppressing NF-κB activity. Sanggenon C possesses antioxidant, anti-inflammatory and antitumor activities.
    Sanggenon C
  • HY-B1724
    Perflubron
    Inhibitor 99.92%
    Perflubron (Perfluorooctyl bromide) is a contrast medium for magnetic resonance imaging and sonography. Perflubron inhibits chemokine expression and NF-κB activation. Perflubron can be emulsified with egg phospholipids (EYP) and shows exceptionally fast excretion characteristics. Perflubron has anti-inflammatory, antiviral and cytoprotective effects.
    Perflubron
  • HY-W015883R
    Fumaric acid (Standard)
    Inhibitor
    Fumaric acid (Standard) is the analytical standard of Fumaric acid. This product is intended for research and analytical applications. Fumaric acid is an unsaturated dicarbonic acid, an intermediate product of the citric acid cycle that provides intracellular energy in the form of ATP. Fumaric acid exerts anti-inflammatory effects by inhibiting the NF-κB signaling pathway dependent on p38 MAPK. Fumaric acid can be used in the study of pregnancy-induced hypertension.
    Fumaric acid (Standard)
  • HY-B1449R
    Uridine (Standard)
    Inhibitor
    Uridine (Standard) is the analytical standard of Uridine. This product is intended for research and analytical applications.
    Uridine (Standard)
  • HY-107744
    Nalmefene
    Inhibitor 99.94%
    Nalmefene is a BBB-penetrable opioid receptor modulator. Nalmefene is an antagonist of MOR and DOR, and a partial agonist of KOR. Nalmefene has anti-inflammatory and neuroprotective activities. Nalmefene can be used in the research of reducing alcohol-dependent disorders.
    Nalmefene
  • HY-N0896
    Inulicin
    Inhibitor 99.94%
    Inulicin (1-O-Acetylbritannilactone) is an active compound that inhibits VEGF-mediated activation of Src and FAK. Inulicin (1-O-Acetylbritannilactone) inhibits LPS-induced PGE2 production and COX-2 expression, and NF-κB activation and translocation.
    Inulicin
  • HY-N0613
    Sauchinone
    Inhibitor 99.62%
    Sauchinone is a diastereomeric lignan isolated from Saururus chinensis (Saururaceae). Sauchinone inhibits LPS-inducible iNOS, TNF-α and COX-2 expression through suppression of I-κBα phosphorylation and p65 nuclear translocation. Sauchinone has anti-inflammatory and antioxidant activity.
    Sauchinone
  • HY-108910A
    Chymotrypsin (MS grade)
    Inhibitor
    Chymotrypsin (EC 3.4.21.1; Chymotrypsin A) (MS grade) is an orally effective inhibitor targeting molecules such as TLR4, NF-κB, MMP-1, TNF-α, IL-1β, and IL-6. Chymotrypsin (MS grade) downregulates the TLR4/NF-κB signaling pathway, inhibits the release of inflammatory factors, reduces cell infiltration and tissue damage, and also reduces the expression of tumor cell adhesion molecules (such as CD44 and CD54). It can also be specifically detected by fluorescent probes (such as NBD-3). Chymotrypsin (MS grade) has anti-inflammatory, hepatoprotective, joint damage-reducing, liver protection against lipotoxicity, and anti-tumor metastasis functions, and can be used in the research of diseases such as rheumatoid arthritis, non-alcoholic fatty liver disease, and melanoma metastasis. Chymotrypsin (MS grade) can be used in studies of inflammation, edema, and expectoration.
    Chymotrypsin (MS grade)
  • HY-N0919
    Yangonin
    Inhibitor 99.65%
    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-N0894
    Octahydrocurcumin
    Inhibitor 99.25%
    Octahydrocurcumin (Hexahydrobisdemethoxycurcumin) is an orally active anticancer and anti-inflammatory agent, and is the final hydrogenated metabolite of Curcumin (HY-N0005) in vivo. Octahydrocurcumin exerts its anti-tumor and anti-inflammatory effects by inducing the mitochondrial apoptosis pathway and inhibiting the TAK1-NF-κB-COX-2 pathway, respectively.
    Octahydrocurcumin
  • HY-14654S
    Aspirin-d3
    Inhibitor 99.84%
    Aspirin-d3 is the deuterium labeled Aspirin (HY-14654). Aspirin (Acetylsalicylic acid) is an orally active, potent and irreversible inhibitor of cyclooxygenase COX-1 and COX-2, with IC50 values of 5 and 210 μg/mL, respectively. Aspirin induces apoptosis. Aspirin inhibits the activation of NF-κB. Aspirin also inhibits platelet prostaglandin synthetase, and can prevent coronary artery and cerebrovascular thrombosis.
    Aspirin-d<sub>3</sub>
  • HY-113236
    p-Synephrine
    Inhibitor 99.90%
    p-Synephrine is an orally active alkaloid dietary supplement without indirect sympathomimetic activity or cardiovascular stimulatory activity. p-Synephrine stimulates AMPK phosphorylation and mediates Glut4 translocation to increase glucose consumption and lactate production in skeletal muscle cells. p-Synephrine also downregulates the p38 MAPK and NF-κB signaling pathways to inhibit pro-inflammatory cytokine production and alter oxidative metabolism. p-Synephrine exhibits low subchronic toxicity in mice. p-Synephrine can be applied to research related to systemic inflammatory response syndrome, obesity, and type 2 diabetes.
    p-Synephrine
  • HY-N0924
    (±)-Stylopine
    Inhibitor 99.86%
    (±)-Stylopine (Tetrahydrocoptisine) is an alkaloid compound. (±)-Stylopine can be isolated from the tubers of the plant Corydalis. (±)-Stylopine inhibits TNF-α, IL-6, and NO production, and attenuates phosphorylation of p38 MAPK, ERK1/2. (±)-Stylopine inhibits NF-κB expression. (±)-Stylopine exhibits anti-inflammatory activity. (±)-Stylopine has protective effects against foot edema, gastric ulcers, anxiety, depression, and acute lung injury.
    (±)-Stylopine
  • HY-N6893
    Ergolide
    Inhibitor 99.48%
    Ergolide is an orally active dual inhibitor targeting NF-κB/p65 and NLRP3. Ergolide blocks the NF-κB signaling pathway and the nuclear translocation of p65, and irreversibly binds to the NACHT domain of NLRP3 to inhibit inflammasome assembly. Ergolide significantly reduces the production of inflammatory mediators (e.g., NO, PGE2) and cytokines, induces cancer cell apoptosis, autophagy and ROS generation. Ergolide also enhances the anti-tumor effect of vincristine. Ergolide alleviates acute lung injury via an NLRP3-dependent mechanism, and effectively improves the survival rate and behavioral function of septic mice and inflammatory zebrafish models. Ergolide is used in the research of metastatic uveal melanoma, neurodegenerative diseases (such as Alzheimer's disease, Parkinson's disease), sepsis and acute lymphoblastic leukemia.
    Ergolide
  • HY-N2481
    Oroxylin A-7-O-glucuronide
    Inhibitor 99.83%
    Oroxylin A-7-O-glucuronide (oroxyloside) is an orally active flavonoid glucuronide and metabolite of Oroxylin A (HY-N0560). Oroxylin A-7-O-glucuronide can be extracted from the dried root of Scutellaria baicalensis. Oroxylin A-7-O-glucuronide exhibits prolyl oligopeptidase inhibitory activity. Oroxylin A-7-O-glucuronide inhibits the JNK pathway, upregulates PPARγ, and inhibits NF-κB p65 nuclear translocation. Oroxylin A-7-O-glucuronide reduces cytokine (IL-1β, IL-6) production. Oroxylin A-7-O-glucuronide exhibits anti-angiogenic, anti-tumor (glioma, liver cancer), anti-inflammatory, and hepatoprotective activities.
    Oroxylin A-7-O-glucuronide
  • HY-W016969
    2-Undecanone
    Inhibitor 99.90%
    2-Undecanone is an orally active organic ketone. 2-Undecanone exerts antibacterial effects by inhibiting bacterial chaperone systems and interfering with the refolding of heat-inactivated proteins. 2-Undecanone also ameliorates asthmatic inflammation and airway remodeling by blocking the NF-κB pathway, and activates the Nrf2 pathway to reduce oxidative damage and prevent lung cancer induced by Benzo[a]pyrene (HY-107377). 2-Undecanone can be used in research related to cancer, asthma and infections.
    2-Undecanone
  • HY-B2082
    Fursultiamine
    Inhibitor 99.71%
    Fursultiamine is a vitamin B1 derivative, has anti-nociceptive and antineoplastic activity. Fursultiamine can be used for vitamin B1?deficiency, osteoarthritis (OA) and cancer research.
    Fursultiamine
  • HY-N6046
    Kamebakaurin
    Inhibitor 99.64%
    Kamebakaurin is an orally active diterpenoid compound that can be isolated from Isodon excia (Maxin.). Kamebakaurin can inhibit NF-κB activation by directly targeting the DNA-binding activity of p50. Kamebakaurin can induce apoptosis and cell cycle arrest in tumor cells. Kamebakaurin has anti-inflammatory and anti-tumor activities.
    Kamebakaurin
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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