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-N2255
    Crebanine
    		Inhibitor 99.83%
    Crebanine is an isoquinoline-like alkaloid that can be derived from Stephania. Crebanine is an antagonist of the α7-nAChR with an IC50 of 19.1 μM. Crebanine suppresses the proliferation, migration, and invasion of cancer cells, triggers reactive oxygen species (ROS) burst, and promotes apoptosis. Crebanine inhibits the AKT/FoxO3a, NF-κB and MAPK signaling pathways. Crebanine attenuates NOX2 hyperactivation, exhibits antioxidant properties by reducing reactive oxygen species and peroxidation in microglia cells. Crebanine inhibits voltage-dependent Na+ current in guinea-pig ventricular myocytes. Crebanine has high inhibitory activity against gram-positive animal pathogenic bacteria. Crebanine ameliorates ischemia-reperfusion brain damage in middle cerebral artery occlusion and reperfusion (MCAO/R) rats. Crebanine significantly improves Scopolamine (HY-N0296)-induced cognitive deficits in ICR mice. Crebanine can be used for the study of hepatocellular carcinoma (HCC), cerebral ischemia and Alzheimer's disease.
    Crebanine
  • HY-118020A
    Loliolide
    		Inhibitor 99.92%
    Loliolide (Loliolid) is a β-carotene metabolite. Loliolide reduces caspase 3, 8, 9 expression, enhances PI3K, AKT, SIRT1, inhibits ROS, apoptosis, and blocks NF-κB p65 nuclear translocation. Loliolide protects mitochondria, reduces oxidative stress, and increases cell viability in neuroblastoma cells. Loliolide can be used for the research of UV-induced skin damage and Parkinson’s disease.
    Loliolide
  • HY-A0068
    Aurothioglucose
    		Inhibitor
    Aurothioglucose (Gold thioglucose), containing monovalent gold ion, is a potent active-site inhibitor of TrxR1 (thioredoxin reductase 1), with an IC50 of 65 nM. Aurothioglucose inhibits the DNA binding of NF-κB in vitro. Aurothioglucose shows anti-HIV and anti-rheumatic activities.
    Aurothioglucose
  • HY-123936
    SR12343
    		Inhibitor 99.66%
    SR12343 is a IKK/NF-κB inhibitor and a mimetic of the NF-κB essential modulator (NEMO)-binding domain (NBD). SR12343 inhibits TNF-α- and LPS-induced NF-κB activation by blocking the interaction between IKKβ and NEMO. SR12343 suppresses LPS-induced acute pulmonary inflammation in mice. SR12343 extends the healthspan of naturally aged and accelerated aging mice. SR12343 can be used for research on inflammatory and degenerative diseases.
    SR12343
  • HY-W160560
    4-Vinylsyringol
    		Inhibitor 98.49%
    4-Vinylsyringol is a phenolic compound with potential antioxidant and anti-inflammatory activities, which can be isolated from rapeseed oil.
    4-Vinylsyringol
  • HY-124813
    PDZ1i
    		Inhibitor 99.29%
    PDZ1i (113B7) is a inhibitor of MDA-9/Syntenin, with selective binding to the PDZ1 domain. PDZ1i inhibits radiation-induced invasion of glioblastoma (GBM) cells, radiosensitizes GBM cells, and impairs GBM-related signaling pathways (including Src/EphA2, EGFRvIII/FAK, and NF-κB). PDZ1i reduces radiation-induced secretion of invasion-related proteases (MMP-2, MMP-9, ADAM9). PDZ1i shows anti-tumor effects in nude mice bearing intracranial U1242-luc xenografts or GBM xenografts. PDZ1i can be used for the study of glioblastoma (GBM), breast cancer and prostate cancer.
    PDZ1i
  • HY-101402
    Cyclo(his-pro)
    		98.95%
    Cyclo(his-pro) (Cyclo(histidyl-proline)) is an orally active cyclic dipeptide structurally related to tyreotropin-releasing hormone. Cyclo(his-pro) could inhibit NF-κB nuclear accumulation. Cyclo(his-pro) can cross the brain-blood-barrier and affect diverse inflammatory and stress responses.
    Cyclo(his-pro)
  • HY-167832
    PT109
    		Inhibitor 99.20%
    PT109 is an orally active, blood-brain barrier permeable multi-kinase inhibitor. By inhibiting PTBP1, PT109 promotes the switch of pyruvate kinase isoform from PKM2 to PKM1, thereby effectively inhibiting the proliferation and migration of glioblastoma multiforme and inducing its reprogramming into oligodendrocytes. PT109 also targets and regulates key signaling molecules such as JNK, SGK1, GSK3β to exert neuroprotective effects including promoting neurogenesis, inducing synapse formation and alleviating neuroinflammation. In Alzheimer's disease models, PT109 exhibits significant efficacy in improving spatial learning ability, along with excellent in vivo pharmacokinetic properties. PT109 can be used to investigate metabolic reprogramming of glioblastoma multiforme and neuroprotective mechanisms of Alzheimer's disease.
    PT109
  • HY-114557
    NSC 90469
    		Inhibitor 99.41%
    NSC 90469 (3,5-Diiodo-L-thyronine) is an orally active thyroid hormone derivative. NSC 90469 inhibits JNK phosphorylation and NF-κB acetylation, blocks SIRT1 protein expression, induces elevated PGC-1α levels, and stimulates COX activity. NSC 90469 enhances UCP1-mediated thermogenesis, increases hepatic Dio1 activity, inhibits TSH levels and hypothalamic-pituitary-thyroid axis function, enhances lipid metabolism, and regulates energy metabolism via the mitochondrial pathway. NSC 90469 prevents blood glucose reduction, reduces urinary albumin excretion, inhibits renal matrix expansion, decreases TGF-β1 expression, and reduces renal fibronectin and type Ⅳ collagen deposition. NSC 90469 also increases energy expenditure and prevents diet-induced overweight. NSC 90469 can be used in studies related to diabetic nephropathy, hypothyroidism, non-alcoholic fatty liver disease, and diet-induced obesity.
    NSC 90469
  • HY-W041489
    Chelidonic acid
    		Inhibitor 99.91%
    Chelidonic acid is a component of Chelidonium majus L., used as an antimicrobial. Chelidonic acid also shows anti-inflammatory activity. Chelidonic acid has potential to inhibit IL-6 production by blocking NF-κB and caspase-1. Chelidonic acid is a glutamate decarboxylase inhibitor, with a Ki of 1.2 μM.
    Chelidonic acid
  • HY-N0687
    Vindoline
    		Inhibitor 99.95%
    Vindoline is an orally active vinca alkaloid. Vindoline can be extracted from the leaves of Catharanthus roseus. Vindoline has a weak inhibitory effect on the self-assembly of tubulin. Vindoline alleviates Apoptosis, inhibits p-p65 and p-ERK. Vindoline improves diabetes, bone loss, osteoarthritis, and kidney damage.
    Vindoline
  • HY-N0911
    Rehmannioside A
    		Inhibitor 99.96%
    Rehmannioside A is a compound that can be isolated from Rehmanniae radix. Rehmannioside A is an inhibitor of CYP3A4, 2C9 and 2D6, with IC50 values of 10.08, 12.62 and 16.43 μM, respectively. Rehmannioside A has anti-inflammatory, antioxidant, anti-apoptosis, anti-ferroptosis, cognitive improvement and neuroprotective activities. Rehmannioside A can be used for the research of nervous system and inflammation-related diseases.
    Rehmannioside A
  • HY-N1941
    Isosinensetin
    		Inhibitor 99.90%
    Isosinensetin is a flavonoid compound and an inhibitor of HIV-1 protease and PTP1B (IC50: 2.61 µM; Ki: 0.92 µM). Isosinensetin inhibits P-glycoprotein (P-gp) in MDR1-MDCKII cells. Isosinensetin has multiple activities such as anti-tumor, anti-viral, anti-inflammatory, and antioxidant effects. Isosinensetin can be used in the research of various diseases including cancer, inflammation, osteoporosis, diabetes, etc.
    Isosinensetin
  • HY-125911
    Gossypin
    		Inhibitor 98.29%
    Gossypin is an orally active flavone isolated from Hibiscus vitifolius. Gossypin has antioxidant, antiinflammatory, anticancer, anticataract, antidiabetic, and hepatoprotective activities. Gossypin inhibits NF-κB and NF-κB-regulated gene expression. Gossypin inhibits AURKA and RSK2. Gossypin inhibits invasion and induces apoptosis. Gossypin can be used for gastric cancer study.
    Gossypin
  • HY-B0780
    Fimasartan
    		Inhibitor 99.60%
    Fimasartan (BRA-657) is an orally effective angiotensin receptor AT1 non-peptide antagonist. Fimasartan has antihypertensive effects. Fimasartan improves neuroinflammation and brain injury mediated by NLRP3 inflammatome after intracerebral hemorrhage, and has neuroprotective effect. Fimasartan inhibits the expression of inducible nitric oxide synthase through the inactivation of NF-κB and activator protein-1.
    Fimasartan
  • HY-N6843
    Arnicolide D
    		Inhibitor 99.69%
    Arnicolide D is a sesquiterpene lactone that can be isolated from Centipeda minima. Arnicolide D is cytotoxic to tumor cells and can induce cell cycle arrest, apoptosis, and oncosis in tumor cells. Arnicolide D has anti-tumor activity.
    Arnicolide D
  • HY-N2485
    4'-Methoxyresveratrol
    		Inhibitor 99.48%
    4'-Methoxyresveratrol (4'-O-Methylresveratrol) is a polyphenol derived from Dipterocarpaceae, with antiandrogenic, antifungal and anti-inflammatory activities. 4'-Methoxyresveratrol alleviates AGE-induced inflammation through suppressing RAGE-mediated MAPK/NF-κB signaling pathway and NLRP3 inflammasome activation.
    4'-Methoxyresveratrol
  • HY-N0460
    1-Caffeoylquinic acid
    		Inhibitor 99.54%
    1-Caffeoylquinic acid is an effective NF-κB inhibitor, shows significant binding affinity to the RH domain of p105 with Ki of 0.007 μM. 1-Caffeoylquinic acid has anti-oxidative stress ability. 1-Caffeoylquinic acid is the Inhibitor for PD-1/PD-L1.
    1-Caffeoylquinic acid
  • HY-151262
    JAK-IN-23
    		Inhibitor 98.88%
    JAK-IN-23 is an orally active double inhibitor of JAK/STAT and NF-κB. JAK-IN-23 can inhibit JAK1/2/3 with IC50 values of 8.9 nM, 15 nM and 46.2 nM, respectively. JAK-IN-23 has potent inhibitory activities against interferon-stimulated genes (ISG) and NF-κB pathways with IC50 values of 3.3 nM and 150.7 nM, respectively. JAK-IN-23 has great anti-inflammatory that decreases the release of various proinflammatory factors. JAK-IN-23 can be used for the research of inflammatory bowel disease (IBD).
    JAK-IN-23
  • HY-N6857
    Armepavine
    		Inhibitor 99.53%
    Armepavine, found in Nelumbo nucifera, is an orally active NF-κB inhibitor. Armepavine attenuates expression of p-p65, α-SMA, p-JNK1/2, p-ERK1/2, p-p38α stimulated by TNF-α and LPS. Armepavine suppresses NF-κB nuclear translocation, IκBα phosphorylation, and collagen deposition. Armepavine can be used for the research of hepatic fibrosis and leukemia.
    Armepavine
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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