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

NF-κB

Nuclear factor-κB; Nuclear factor-kappaB

NF-κB

Related Products

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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-29268
    β-Carboline-1-carboxylic acid
    		Inhibitor
    β-Carboline 1-carboxylic acid is a β-carboline alkaloid with anti-inflammatory, antifibrotic, antitumor and antibacterial activities. β-Carboline 1-carboxylic acid is the cAMP phosphodiesterase (IC50: 96 µM) and indoleamine 2, 3-dioxygenase (IDO) inhibitor. β-Carboline 1-carboxylic acid is cytotoxic to tumor cells. β-Carboline 1-carboxylic acid inhibits inflammation through the NF-κb/p65 pathway and can reverse epithelial-mesenchymal transition (EMT). In addition, β-Carboline 1-carboxylic acid has strong inhibitory activity against S. aureus (IC50: 47.70 μg/mL) and E. coli (IC50: 19.17 μg/mL).
    β-Carboline-1-carboxylic acid
  • HY-W012977R
    3,3-Dimethyl-1-butanol (Standard)
    		Inhibitor
    3,3-Dimethyl-1-butanol (Standard) is the analytical standard of 3,3-Dimethyl-1-butanol (HY-W012977). This product is intended for research and analytical applications. 3,3-Dimethyl-1-butanol (DMB) is an orally active inhibitor of trimethylamine (TMA) and trimethylamine N-oxide (TMAO). 3,3-Dimethyl-1-butanol inhibits the signaling pathway of p65 NF-κB and TGF-β1/Smad3. 3,3-Dimethyl-1-butanol has potential applications in cardiovascular disease (CVD).
    3,3-Dimethyl-1-butanol (Standard)
  • HY-B0072S
    Tropisetron-d5
    		Inhibitor
    Tropisetron-d5 (SDZ-ICS-930-d5 (free base)) is deuterium labeled Tropisetron. Tropisetron (SDZ-ICS-930 free base) is an orally active anti-inflammatory and antiemetic agent. Tropisetron is 5-HT3R antagonists with a Ki of 5.3 nM. Tropisetron is also a partial agonist of α7 nicotinic receptor (α7 nAChR) with an EC50 of 1.3 μM. In addition, Tropisetron has antitumor and neuroprotective effects.
    Tropisetron-d<sub>5</sub>
  • HY-N0442R
    5-O-Methylvisammioside (Standard)
    		Inhibitor
    5-O-Methylvisammioside (4'-O-β-D-Glucosyl-5-O-methylvisamminol) (Standard) is the analytical standard of 5-O-Methylvisammioside. This product is intended for research and analytical applications. 5-O-Methylvisammioside is an orally active natural chromone glycoside and multiple biological activities. 5-O-Methylvisammioside inhibits ferroptosis by activating the Nrf2/HO-1 signaling axis. 5-O-Methylvisammioside alleviates intestinal barrier damage by inhibiting the ROS/NF-κB/NLRP3 pathway. 5-O-Methylvisammioside exerts a protective effect against acute liver injury by reducing ALT/AST, decreasing inflammatory infiltration, and inhibiting IκB-α phosphorylation and NF-κB nuclear translocation. 5-O-Methylvisammioside blocks the HMGB1/RAGE/MEK/ERK signaling axis to exert anti-tumor and anti-angiogenic effects. 5-O-Methylvisammioside improves depression-like behaviors by inhibiting Src kinase and the NF-κB pathway.
    5-O-Methylvisammioside (Standard)
  • HY-N13200
    Cranberry Extract
    		Inhibitor
    Cranberry Extract is the extract of Cranberry, with content of 25% -50% Proanthocyanidins. Cranberry Extract exhibits anti-virus and antimicrbiol activity. Cranberry Extract suppresses fungal growth and biofilm formation. Cranberry Extract reduces NF-κB p65 phosphorylation, and PI3K/AKT signaling; increases caspase-8/9 activity to induce apoptosis, modulates oxidative stress, inflammation, and lipid profiles. Cranberry Extract exerts antiproliferative effects and induces cell cycle arrest. Cranberry Extract can be used for the research of infection and cancers.
    Cranberry Extract
  • HY-13982R
    JSH-23 (Standard)
    		Inhibitor
    JSH-23 (Standard) is the analytical standard of JSH-23. This product is intended for research and analytical applications. JSH-23 is an NF-κB inhibitor which inhibits NF-κB transcriptional activity with an IC50 of 7.1 μM in lipopolysaccharide (LPS)-stimulated macrophages RAW 264.7. JSH-23 inhibits nuclear translocation of NF-κB p65 without affecting IκBα degradation.
    JSH-23 (Standard)
  • HY-48813
    Glycoursodeoxycholic acid 3-sulfate
    		Inhibitor
    Glycoursodeoxycholic acid 3-sulfate is a glycine-conjugated sulfated bile acid 3-sulfate, which is produced by SULT2A1-mediated sulfation of glycoursodeoxycholic acid (HY-N1424) in the liver. Glycoursodeoxycholic acid 3-sulfate attenuates the anti-inflammatory effect of glycoursodeoxycholic acid and impairs the inhibitory effect on the IL-17 and NF-κB signaling pathways. Glycoursodeoxycholic acid 3-sulfate shows a significant correlation with aortic flow velocity and BNP in patients with aortic stenosis. Glycoursodeoxycholic acid 3-sulfate is mainly used in related studies such as quantitative analysis, quality control and biochemical experiments; it often serves as a reagent for metabolomics analysis and can also be applied to research related to aortic stenosis.
    Glycoursodeoxycholic acid 3-sulfate
  • HY-13687R
    IKK 16 (Standard)
    		Inhibitor
    IKK 16 (Standard) is the analytical standard of IKK 16. This product is intended for research and analytical applications. IKK 16 hydrochloride is an orally active IKK inhibitor. IKK 16 hydrochloride shows IC50s of 40 nM, 70 nM, 200 nM, and 50 nM for IKK2, IKK complex, IKK1, and LRRK 2, respectively. IKK 16 hydrochloride is also a pan-PKD inhibitor, inhibiting PKD1, PKD2, and PKD3 with IC50s of 153.9, 115, and 99.7 nM, respectively. IKK 16 hydrochloride is also an ABCB1 inhibitor, interfering with the binding of ABCB1 to its substrates. IKK 16 hydrochloride protects against LPS (HY-D1056)-induced multiple organ dysfunction by reducing the acute inflammatory response induced by endotoxin exposure. IKK 16 hydrochloride can restore renal function and alleviate fibrosis in acute kidney injury. IKK 16 hydrochloride attenuates cardiac dysfunction associated with polymicrobial sepsis in mice with type 2 diabetes mellitus (T2DM) by inhibiting the NF-κB pathway.
    IKK 16 (Standard)
  • HY-135317E
    Emavusertib maleate
    		Inhibitor
    Emavusertib maleate (CA-4948 maleate) is the maleate salt form of Emavusertib (HY-135317). Emavusertib maleate is an orally active inhibitor for IRAK4 (IC50=57 nM) and FLT3. Emavusertib maleate inhibits NF-κB and MyD88 signaling pathways, reduces the generation of pro-inflammatory cytokines like IL-6 and IL-10, thereby exhibiting anti-inflammatory and anti-proliferative activities against cancer cells, leading to cell apoptosis. Emavusertib maleate exhibits antitumor activity in mouse model.
    Emavusertib maleate
  • HY-N0631R
    Cornuside (Standard)
    		Inhibitor
    Cornuside (Standard) is the analytical standard of Cornuside (HY-N0631). This product is intended for research and analytical applications. Cornuside is an iridoid glycoside with anti-allergic, anti-inflammatory, and neuroprotective activities. Cornuside exerts anti-allergic activity by downregulating the p38 MAPK, JNK, and NF-κB signaling pathways, and inhibits IgE-mediated histamine release from mast cells. Cornuside improves cognitive impairment in mice by inhibiting BACE1 activity (IC50 = 55.84 μg/mL) and enhancing ChAT activity. Cornuside inhibits LPS (HY-D1056)-induced inflammatory mediators, including iNOS, COX-2, PGE2, TNF-α, IL-6, and IL-1β, by suppressing NF-κB activation.
    Cornuside (Standard)
  • HY-100487R
    TAK-243 (Standard)
    		Inhibitor
    TAK-243 (Standard) is the analytical standard of TAK-243 (HY-100487). This product is intended for research and analytical applications. TAK-243 (MLN7243) is a first-in-class, selective ubiquitin activating enzyme, UAE (UBA1) inhibitor (IC50=1 nM), which blocks ubiquitin conjugation, disrupting monoubiquitin signaling as well as global protein ubiquitination. TAK-243 (MLN7243) induces endoplasmic reticulum (ER) stress, abrogates NF-κB pathway activation and promotes apoptosis.
    TAK-243 (Standard)
  • HY-B0531R
    Triflusal (Standard)
    		Inhibitor
    Triflusal (Standard) is the analytical standard of Triflusal (HY-B0531). This product is intended for research and analytical applications. Triflusal is an orally bioavailable, blood-brain barrier-permeable dual Cyclooxygenase-1 (COX-1)/cAMP phosphodiesterase inhibitor. Triflusal inhibits platelet aggregation, NF-κB activation, iNOS activity, and prostaglandin synthesis in ischaemic tissue. Triflusal stimulates neutrophil nitric oxide production, eNOS protein expression, and cNOS activity. Triflusal alleviates cerebral ischemic injury in rats and ameliorates pathological lesions and related gene expression in transgenic Alzheimer’s disease models. Triflusal can be used for the research of thromboembolic/ischemic cardiovascular and cerebrovascular diseases, and Alzheimer’s disease.
    Triflusal (Standard)
  • HY-N1431A
    Tabersonine hydrochloride
    		Inhibitor 98.55%
    Tabersonine hydrochloride is a selective, orally active NLRP3 inhibitor. Tabersonine hydrochloride directly binds to the NACHT domain of NLRP3, inhibiting its ATPase activity and oligomerization, thereby blocking ASC spot formation and caspase-1 activation, and reducing the release of pro-inflammatory cytokines such as IL-1β. Tabersonine hydrochloride also inhibits K63-linked ubiquitination of TRAF6, blocking NF-κB, PI3K/Akt, and p38 MAPK signaling pathways. Tabersonine hydrochloride can inhibit inflammatory responses, induce apoptosis of liver cancer cells through mitochondrial pathways and death receptor pathways, reduce mitochondrial membrane potential, promote cytochrome c release, and activate caspase proteins. Tabersonine hydrochloride is mainly used in the study of NLRP3-driven inflammatory diseases (such as acute lung injury, sepsis, peritonitis) and tumors such as liver cancer.
    Tabersonine hydrochloride
  • HY-N10133
    Licoflavanone
    		Inhibitor
    Licoflavanone (3′-Prenylnaringenin) is a flavanone with antioxidant, anti-inflammatory and anticancer activities. Licoflavanone can be isolated from the leaf extract of Glycyrrhiza glabra. Licoflavanone downregulates the mTOR/PI3K/AKT signaling pathway to inhibit the proliferation, migration and invasion of cancer cells, while activates Bax, Bad and multiple caspase enzymes to induce apoptosis. Its anti-inflammatory effect is manifested by reducing the nuclear translocation of NF-κB, decreasing the phosphorylation levels of p38, JNK and ERK1/2, thereby inhibiting the expression of nitric oxide, proinflammatory cytokines, COX-2 and iNOS. Licoflavanone is used in studies on nasopharyngeal carcinoma and related mechanisms.
    Licoflavanone
  • HY-B1014R
    Acenocoumarol (Standard)
    		Inhibitor
    Acenocoumarol (Standard) is the analytical standard of Acenocoumarol. This product is intended for research and analytical applications. Acenocoumarol is an anticoagulant that functions as a Vitamin K antagonist. Acenocoumarol inhibits MAPK/ERK/JNK signaling pathway, reduces the nuclear translocation of NF-κB p65, activates Akt/GSK3β signaling pathway. Acenocoumarol induces apoptosis in cell A549, arrests cell cycle at S phase.
    Acenocoumarol (Standard)
  • HY-W005130R
    2,4,6-Trihydroxybenzaldehyde (Standard)
    		Inhibitor
    2,4,6-Trihydroxybenzaldehyde is an orally active NF- B inhibitor. 2,4,6-Trihydroxybenzaldehyde shows anti-tumor activity, anti-cancer cell proliferative activity and anti-obesity activity.
    2,4,6-Trihydroxybenzaldehyde (Standard)
  • HY-B0008R
    Sulindac (Standard)
    		Inhibitor
    Sulindac (Standard) is the analytical standard of Sulindac. This product is intended for research and analytical applications. Sulindac (MK-231) is an orally active nonsteroidal anti-inflammatory agent. Sulindac also is an immunomodulatory agent. Sulindac can be used for the research of arthritis of the spine, gouty arthritis and kinds of cancer including colorectal cancer (CRC) and lung cancer.
    Sulindac (Standard)
  • HY-163030
    LasB-IN-1
    		Inhibitor
    LasB-IN-1 (compound 5f) is a potent and orally active inhibitor of LasB (IC50 = 8.7 μM). LasB-IN-1 effectively attenuates elastase production and biofilm formation by P. aeruginosa while alleviating the inflammatory response through downregulating MAPK and NF-κB pathways. LasB-IN-1 is potential to be a novel anti-infective candidate against drug-resistant infections.
    LasB-IN-1
  • HY-N0253R
    Hederacoside C (Standard)
    		Inhibitor
    Hederacoside C (Standard) is the analytical standard of Hederacoside C. This product is intended for research and analytical applications. Hederacoside C (Kalopanaxsaponin B) is an ingredient that can be obtained mainly from ivy leaves. Hederacoside C mediates inflammation by inhibiting activation of MAPK/NF-κB and its downstream signaling pathway. Hederacoside C has anti-inflammatory and antibacterial activity.
    Hederacoside C (Standard)
  • HY-129440R
    N-(p-Coumaroyl) Serotonin (Standard)
    		Inhibitor
    N-(p-Coumaroyl) Serotonin (Standard) is the analytical standard of N-(p-Coumaroyl) Serotonin (HY-129440). This product is intended for research and analytical applications. N-(p-Coumaroyl) Serotonin is an orally active polyphenol found in safflower seeds with potent anti-inflammatory, antioxidant, and antitumor activities. N-(p-Coumaroyl) Serotonin suppresses NF‑κB, TLR4/MyD88 and MAPK signaling, activates NQO1/HO‑1 pathways, and inhibits pro‑inflammatory cytokines, iNOS and COX‑2 and ROS production. N-(p-Coumaroyl) Serotonin induces S‑phase arrest and apoptosis in glioblastoma cells, reduces atherosclerotic lesions, and alleviates renal and vascular injuries. N-(p-Coumaroyl) Serotonin acts as a vasodilator, regulates calcium dynamics. N-(p-Coumaroyl) Serotonin can be used for the research of neurodegenerative diseases, atherosclerosis, glioblastoma, and acute renal failure.
    N-(p-Coumaroyl) Serotonin (Standard)
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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