2. Signaling Pathways
  3. NF-κB
  4. NF-κB

NF-κB

Nuclear factor-κB; Nuclear factor-kappaB

NF-κB

Related Products

PDF 4.06 MB

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-N0272
    Eleutheroside E
    		Inhibitor 99.58%
    Eleutheroside E is an important component of ginseng that can be taken orally. Eleutheroside E has anti-inflammatory and antioxidant properties, and it helps reduce apoptosis in heart cells caused by hypoxia-reoxygenation (H/R) damage. Eleutheroside E can improve type 2 diabetes, enhance cognitive function, and has neuroprotective effects.
    Eleutheroside E
  • HY-155998
    NF-κB-IN-11
    		Inhibitor 98.42%
    NF-κB-IN-11 (Compound 3i) is a NF-κB inhibitor. NF-κB-IN-11 inhibits TNF-α induced activation of NF-κB pathway, and inhibits nuclear translocation of NF-κB. NF-κB-IN-11 down-regulates the expression levels of phosphor-IKK, IκBα, and NF-κB p65. NF-κB-IN-11 has anti-inflammatory activity, and alleviates dextran sulfate sodium-induced colitis in mice. NF-κB-IN-11 (p.o.) shows a MTD more than 1852 mg/kg in mice acute toxicity assay.
    NF-κB-IN-11
  • HY-110195
    Smurf1-IN-A01
    		99.81%
    Smurf1-IN-A01 is a Smurf1 inhibitor. Smurf1-IN-A01 has anticancer activity and can be used for the research of osteoporosis and age-related macular degeneration.
    Smurf1-IN-A01
  • HY-P1181A
    Pam2CSK4 TFA
    		Activator 99.46%
    Pam2CSK4 TFA is a TLR2 agonist. Pam2CSK4 TFA induces the expression of iNOS and NO in macrophage cell lines via TBK1 and MyD88 molecules. Pam2CSK4 TFA activates the NF-κB and Bruton's tyrosine kinase signaling pathways in platelets, and promotes platelet-endothelial cell interactions. TLR2 activation triggered by Pam2CSK4 TFA expands myeloid-derived suppressor cells (MDSCs) and suppresses anti-tumor immune responses in the tumor microenvironment. Pam2CSK4 TFA acts as a Th2-polarizing adjuvant in mouse vaccine models against Leishmania major and Brugia malayi. Pam2CSK4 TFA can be used in the research of various diseases, including thromboinflammatory diseases, sepsis, atherosclerosis, heart failure, influenza, lymphoma, melanoma, cutaneous leishmaniasis and lymphatic filariasis.
    Pam2CSK4 TFA
  • HY-N0515
    Ophiopogonin D
    		Inhibitor 99.80%
    Ophiopogonin D can be 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 can inhibit isteoclastic differentiation in RAW264.7 cells. Ophiopogonin D has protective effect as an antioxidant in H2O2-induced endothelial injury. Ophiopogonin D blocks ERK signaling cascades. Ophiopogonin D alleviates high-fat diet-induced metabolic syndrome and changes the structure of gut microbiota in mice. Ophiopogonin D has been used against inflammatory, metabolic and cardiovascular diseases.
    Ophiopogonin D
  • HY-N0766
    Isorhynchophylline
    		Inhibitor 99.82%
    Isorhynchophylline is an alkaloid isolated from Crocus sativus with anticancer, antihypertensive, anti-inflammatory, and neuroprotective properties. Isorhynchophylline can be applied to cardiovascular and neurological disorders, and cancer studies.
    Isorhynchophylline
  • HY-N0408
    Picroside II
    		Inhibitor 99.91%
    Picroside II is an antioxidant with oral activity that can reduce the production of ROS and protect the blood-brain barrier (BBB) after CI/R injury, offering neuroprotective effects. Picroside II has antioxidant, immune-regulating, antiviral properties, and inhibits apoptosis. Picroside II alleviates the inflammatory response in sepsis by suppressing the activation of the NLRP3 inflammasome and NF-κB pathways.
    Picroside II
  • HY-14621
    Zingerone
    		Inhibitor 99.77%
    Zingerone (Vanillylacetone) is a nontoxic methoxyphenol isolated from Zingiber officinale, with potent anti-inflammatory, antidiabetic, antilipolytic, antidiarrhoeic, antispasmodic and anti-tumor properties. Zingerone alleviates oxidative stress and inflammation, down-regulates NF-κB mediated signaling pathways. Zingerone acts as an anti-mitotic agent, and inhibits the growth of neuroblastoma cells. Zingerone can cross the blood-brain barrier (BBB).
    Zingerone
  • 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-N4187
    Licochalcone D
    		Inhibitor 99.80%
    Licochalcone D, a flavonoid compound mainly existing in the root of Glycyrrhiza uralensis, is a potent and orally active inhibitor of NF-kappaB (NF-κB) p65. Licochalcone D possesses antioxidant, anti-inflammatory, anti-cancer properties.
    Licochalcone D
  • HY-N5063
    Plantainoside D
    		Inhibitor 99.15%
    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 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
  • HY-N7088
    Raffinose
    		Inhibitor 98.0%
    Raffinose (Melitose) regulates intestinal flora, inhibits TLR4-MyD88-NF-κB signaling pathway, and activates Nrf2 signaling pathway. Raffinose exhibits anti-inflammatory, antioxidant, and immunomodulatory activities. Raffinose is orally active.
    Raffinose
  • HY-N1419
    Vaccarin
    		Inhibitor 99.05%
    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-N0493
    Pectolinarigenin
    		Inhibitor 99.98%
    Pectolinarigenin is an orally active dual inhibitor of COX-2/5-LOX with anti-inflammatory, antioxidant, antitumor and neuroprotective activities. Pectolinarigenin exerts neuroprotective and anti-inflammatory effects on astrocyte inflammation via the NFκB and MAPK pathways. Pectolinarigenin inhibits LPS-induced phosphorylation of ERK1/2, N-FκB and p38MAPK, directly inhibits the enzymatic activity or binding of COX-2, 5-LOX and HIF-1α, and reduces the level of XIAP. Pectolinarigenin modifies Keap1 to promote nuclear accumulation of Nrf2, induces ARE-mediated antioxidant enzyme expression, and possesses direct free radical scavenging activity. Pectolinarigenin reduces the release of NO, proinflammatory mediators and leukotrienes, and increases the level of IL-10. Pectolinarigenin induces G2/M cell cycle arrest, apoptosis (Apoptosis) and autophagy (Autophagy) via the PI3K/AKT/mTOR signaling pathway. Pectolinarigenin reduces renal crystal deposition and inhibits melanin synthesis. Pectolinarigenin inhibits inflammation and alleviates allergy in mouse models of inflammation. Pectolinarigenin alleviates renal injury, inflammation and oxidative stress in mice by inhibiting HIF-1α activity. Pectolinarigenin can be used for the research of neurodegenerative diseases, inflammatory/allergic diseases, calcium oxalate nephrocalcinosis, gastric cancer, melasma, post-inflammatory diseases and chloasma.
    Pectolinarigenin
  • HY-N1500
    Pulegone
    		Inhibitor 99.57%
    Pulegone is a monoterpene ketone compound widely present in the essential oils of many plants. Pulegone can also be used as a bird repellent. Pulegone has multiple activities such as anti-inflammatory, antibacterial, antifungal, and anti-hyperalgesic effects. Pulegone is particularly effective against bacteria of the Salmonella species.
    Pulegone
  • HY-B1619
    Cromolyn
    		Inhibitor 99.97%
    Cromolyn (Cromoglycate) is an orally active GSK-3β inhibitor with an IC50 of 2.0 μM. Cromolyn is also a mast cell stabilizer that can inhibit the release of mediators from mast cells, regulate reflex bronchoconstriction, and reduce non-specific bronchial hyperreactivity, and Cromolyn can be used in the research of bronchial asthma. In addition, Cromolyn has multiple activities such as anti-inflammatory, anti-allergic, anti-histamine, anti-cancer, and neuroprotective effects.
    Cromolyn
  • HY-N2593
    Isorhapontigenin
    		Inhibitor 99.82%
    Isorhapontigenin is an orally active dietary polyphenol. Isorhapontigenin acts as a potent antioxidant that reduces the production of reactive oxygen species (ROS). Isorhapontigenin promotes the binding of JUN to the AP-1 site on the SESN2 promoter, induces SESN2 transcription, triggers MAPK8-dependent JUN activation, and upregulates the expression of PPAR-α, PGC-1α and CPT-1A to facilitate fatty acid oxidation. Isorhapontigenin induces autophagy, apoptosis and preadipocyte differentiation; it inhibits tumor growth, cell invasion, NF-κB transcriptional activity, the PI3K/Akt signaling pathway, STAT1 phosphorylation and MMP-2 expression. Isorhapontigenin alleviates oxidative stress, inflammatory cytokine release and triglyceride accumulation; it increases intracellular ATP levels and promotes Nrf2 nuclear translocation. Isorhapontigenin improves insulin sensitivity in adipose tissue and glucose tolerance, and reduces postprandial blood glucose, insulin and free fatty acid levels. Isorhapontigenin is applicable to research on bladder cancer, liver injury, chronic obstructive pulmonary disease, acute lung injury and type 2 diabetes.
    Isorhapontigenin
  • HY-159520
    Ofirnoflastum
    		Inhibitor 99.93%
    Ofirnoflastum (Ofirnoflast) is an orally active first-in-class allosteric NEK7 inhibitor with an IC50 of 46 nM. Ofirnoflastum binds an allosteric site adjacent to NEK7’s ATP-binding pocket, induces conformational shifts, disrupts NEK7-NLRP3 binding, blocks NLRP3 inflammasome assembly, spares NEK7’s physiological functions, and suppresses caspase-1, caspase-8, NF-κB, and TNF activity. Ofirnoflastum reduces pro-inflammatory cytokine production, suppresses ASC specks, IL-1β release, pyroptotic cell death, and leukemic burden, induces apoptosis and erythroid differentiation, restores hematopoiesis, and improves outcomes in colitis models. Ofirnoflastum can be used for the research of myelodysplastic syndromes, chronic myelomonocytic leukemia, and acute myeloid leukemia.
    Ofirnoflastum
  • HY-108039
    Bezisterim
    		Inhibitor
    Bezisterim (HE 3286; NE-3107) is a synthetic derivative of a natural anti-inflammatory steroid, β-AET. Bezisterim is an orally active partial NF-κB inhibitor. HE3286 reduces proinflammatory signals, including IL-6 and matrix metallopeptidase 3. Bezisterim freely penetrates the blood brain barrier in mice. Bezisterim can be used for the research of the ulcerative colitis, arthritis, experimental autoimmune encephalomyelitis. Bezisterim is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Bezisterim
  • HY-N6602
    α-Solanine
    		Inhibitor 99.89%
    α-solanine, a bioactive component and one of the major steroidal glycoalkaloids in Solanum nigrum, has been observed to inhibit growth and induce apoptosis in cancer cells.
    α-Solanine
Cat. No. Product Name / Synonyms Application Reactivity
All Rights Reserved.
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

Your Search Returned No Results.

Sorry. There is currently no product that acts on isoform together.

Please try each isoform separately.