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-N10768
    1-Dehydro-[10]-gingerdione
    Inhibitor
    1-Dehydro-[10]-gingerdione directly inhibits IKKβ activity by targeting the activation loop of IKKβ, thus disrupting IKKβ-catalysed IκBα phosphorylation in macrophages stimulated with agonists. 1-Dehydro-[10]-gingerdione inhibits LPS (HY-D1056)-induced NF-κB transcriptional activity. 1-Dehydro-[10]-gingerdione has the potential for NF-κB-associated inflammation and autoimmune disorders research.
    1-Dehydro-[10]-gingerdione
  • HY-161266
    COX-2/NLRP3-IN-1
    Inhibitor
    COX-2/NLRP3-IN-1 (Compound 6k) is a COX-2/NLRP3 inhibitor with a IC50 of 1.53 μM for COX-2. COX-2/NLRP3-IN-1 exerts anti-inflammatory effects by inhibiting the NF-κB/NLRP3 signaling pathway.
    COX-2/NLRP3-IN-1
  • HY-N6246R
    Asperulosidic Acid (Standard)
    Inhibitor
    Asperulosidic Acid (Standard) is the analytical standard of Asperulosidic Acid. This product is intended for research and analytical applications. Asperulosidic Acid (ASPA), a bioactive iridoid glycoside, is extracted from the herbs of Hedyotis diffusa Willd. Asperulosidic Acid (ASPA) has anti-tumor, anti-oxidant, and anti-inflammatory activities. ASPA is related to the inhibition of inflammatory cytokines (TNF-α, IL-6) and mediators via suppression of the NF-κB and mitogen-activated protein kinase (MAPK) signaling pathways.
    Asperulosidic Acid (Standard)
  • HY-149087
    MR2938
    Inhibitor
    MR2938 is a potent AChE inhibitor, with an IC50 of 5.04 μM. MR2938 also suppresses NO production obviously (IC50 = 3.29 μM). MR2938 suppresses the neuroinflammation through blocking MAPK/JNK and NF-κB signaling pathways. MR2938 can be used for Alzheimer’s disease (AD) research.
    MR2938
  • HY-10071A
    Y-27632 hydrochloride hydrate
    Inhibitor 99.65%
    Y-27632 hydrochloride hydrate is a ROCK inhibitor with Ki values of 220 nM and 300 nM for ROCK1 and ROCK2, respectively. Y-27632 hydrochloride hydrate exerts anti-inflammatory and immunomodulatory effects in systemic lupus erythematosus models by inhibiting the ROCK/NF-κB pathway. Y-27632 hydrochloride hydrate enhances autophagy by inhibiting the AKT/mTOR pathway, thereby inducing apoptosis apoptosis in oral squamous cell carcinoma. Y-27632 hydrochloride hydrate induces the formation of tunneling nanotubes in ARPE-19 cells and significantly enhances mitochondrial transfer through these channels. Y-27632 hydrochloride hydrate promotes neurite outgrowth in PC12 cells by activating the Rac1/NOX1/ROS/AKT/PAK1 signaling cascade.
    Y-27632 hydrochloride hydrate
  • HY-182053
    Antiproliferative agent-76
    Inhibitor
    Antiproliferative agent-76 (Compound II-2) is an 8-sulfonamidoquinoline derivative and a selective anticancer agent. Antiproliferative agent-76 blocks the NF-κB and WNT signaling pathways. Antiproliferative agent-76 promotes cancer cell Apoptosis. Antiproliferative agent-76 exhibits anticancer activity against colorectal cancer and leukemia.
    Antiproliferative agent-76
  • HY-168482
    NF-κB/MAPK-IN-2
    Inhibitor
    NF-κB/MAPK-IN-2 (compound 14) is a potent NF-κB and MAPK Inhibitor. NF-κB/MAPK-IN-2 decreases the protein expression of p-p65, p-IκB, p-p38, p-JNK, and p-ERK. NF-κB/MAPK-IN-2 reduces the LPS-induced release of TNF-α and IL-6. NF-κB/MAPK-IN-2 inhibits nuclear translocation of p65 and c-Fos. NF-κB/MAPK-IN-2 has the potential for the research of sepsis.
    NF-κB/MAPK-IN-2
  • HY-N17131
    24-O-Acetyllycoclavanol
    Inhibitor
    24-O-Acetyllycoclavanol (compound 1) is a triterpenoid anti-inflammatory agent that selectively targets the NF-κB and ERK1/2 signaling pathways. It exerts its anti-inflammatory activity by inhibiting lipopolysaccharide (LPS)-induced inducible nitric oxide synthase (iNOS) and COX-2 expression, reducing the production of inflammatory mediators such as nitric oxide (NO), IL-1β, and IL-8. 24-O-Acetyllycoclavanol can be used in research related to inflammatory bowel disease (IBD). 24-O-Acetyllycoclavanol can be biologically isolated from the ethyl acetate extract of Lycopodium clavatum.
    24-O-Acetyllycoclavanol
  • HY-N0803S
    Myrcene-d6
    Inhibitor
    Myrcene-d6 is the deuterium labeled Myrcene. Myrcene (β-Myrcene) is a type of aromatic compound that inhibits TNFα and NF-κB activity. Myrcene has anti-invasive action, inhibits cell cycle, and leads to cancer cell apoptosis. Myrcene has strong blood protection effect, anti-inflammation, and anti-inflammatory activity.
    Myrcene-d<sub>6</sub>
  • HY-B1773AR
    Sodium propionate (Standard)
    Inhibitor
    Sodium propionate (Standard) is the analytical standard of Sodium propionate. This product is intended for research and analytical applications. Sodium propionate is an orally active short-chain fatty acid. Sodium propionate can be produced by intestinal bacteria from the metabolism of dietary fiber. Sodium propionate increases PPAR-γ, inhibits NF-κB activation, and reduces COX-2 expression and NO production. Sodium propionate also induces Apoptosis and Autophagy. Sodium propionate reduces HSV-1-induced keratitis. Sodium propionate has anticancer effects against glioblastoma. Sodium propionate exhibits neuroprotective, antioxidant, and anti-inflammatory activities. Sodium propionate can be used in the research of spinal cord injury and Alzheimer's disease.
    Sodium propionate (Standard)
  • HY-N12959
    5,4'-Dihydroxy-6,8-dimethoxy-7-O-rhamnosyl flavone
    Inhibitor
    5,4'-Dihydroxy-6,8-dimethoxy-7-O-rhamnosyl flavone (DDR) is an anticancer agent that can be extracted from Indigofera ovata. 5,4'-Dihydroxy-6,8-dimethoxy-7-O-rhamnosyl flavone can inhibit the PI3K/AKT and NF-кB pathways, inhibit the invasion and migration of cancer cells, and has anticancer activity.
    5,4'-Dihydroxy-6,8-dimethoxy-7-O-rhamnosyl flavone
  • HY-N10638
    N-Acetyldopamine dimer-2
    Inhibitor
    N-Acetyldopamine dimer-2 (compound 2) is a N-acetyldopamine dimer that can be isolated from the yellow powder form Periostracum Cicadae with antioxidant and anti-inflammatory activities. N-Acetyldopamine dimer-2 inhibits oxidized low-density lipoprotein (LDL) oxidation, ROS generation, NO production, and NF-κB activity.
    N-Acetyldopamine dimer-2
  • HY-146560
    Xanthine oxidase-IN-6
    Inhibitor
    Xanthine oxidase-IN-6 (Compound 6c) is a potent, orally active, mixed-type xanthine oxidase (XOD) inhibitor with an IC50 value of 1.37 µM. Xanthine oxidase-IN-6 shows strong anti-hyperuricemia and renal protective activity.
    Xanthine oxidase-IN-6
  • HY-10540
    Sotrastaurin acetate
    Inhibitor
    Sotrastaurin (AEB071) acetate is a selective, orally active PKC inhibitor. Sotrastaurin acetate inactivates NF-κB by inhibiting PKC α, β, θ, γ subtypes, thereby reducing the transcription levels of immune response-related genes. Sotrastaurin acetate effectively inhibits alloreactive T cell proliferation, conventional T cell activation, as well as the production of pro-inflammatory cytokines and B lymphocytes. Sotrastaurin acetate also maintains the functional and phenotypic stability of regulatory T cells, enhances Foxp3 expression and restores the balance of helper T lymphocytes. Sotrastaurin acetate can prolong the survival time of allografts, and alleviate inflammatory responses and myasthenic symptoms by reducing anti-AChR antibody levels. Sotrastaurin acetate is widely used in studies related to kidney transplantation, psoriasis and myasthenia gravis.
    Sotrastaurin acetate
  • HY-175850
    GSK-3β-IN-28
    Inhibitor
    GSK-3β inhibitor 28 is selective and non-competitivea glycogen synthase kinase-3β (GSK-3β) inhibitor with an IC50 of 14.82 nM. GSK-3β inhibitor 28 can upregulate the expression level of phosphorylated GSK-3β and downregulate the expression of p-NF-κB, P65, C-myc and Cyclin D1. GSK-3β inhibitor 28 can induce cells apoptosis, G1 phase arrest and inhibit migration. GSK-3β inhibitor 28 can be used for the research of cancer, such as colorectal cancer.
    GSK-3β-IN-28
  • HY-107272
    Chuanbeinone
    Inhibitor
    Chuanbeinone (22-Epidelavinone) is an orally active alkaloid found in Fritillaria pallidiflora. Chuanbeinone shows cytotoxicity against mutiple cancer cells and can induces apoptosis and S phase arrest. Chuanbeinone downregulates Bcl-2, upregulates Bax, and activates caspase-3. Chuanbeinone exerts anti-inflammatory and antitussive effects by reducing pro-inflammatory cytokine (IL-1β, IL-6 and TNF-α) production and mRNA expression, and inhibiting TRIF-, MyD88-, NF-κB-, and MAPK-dependent signaling pathways. Chuanbeinone inhibits AChE and BChE with IC50 values of 7.7 and 0.7 μM. Chuanbeinone can be used for the researches of lung carcinoma, cough, inflammatory diseases.
    Chuanbeinone
  • HY-116145
    MHY884
    Inhibitor
    MHY884 is a tyrosinase inhibitor that suppresses UVB-induced activation of NF-κB signaling pathway through the downregulation of oxidative stress. MHY884 suppresses oxidative stress in the melanoma cells and attenuates UVB-induced oxidative stress, resulting in reduced NF-κB activity in irradiated mice. MHY884 is promising for research of UVB-induced skin damage.
    MHY884
  • HY-180336
    LM9
    Inhibitor
    LM9 is a potent, orally active MyD88 inhibitor. LM9 blocks TLR4/MyD88 binding, MyD88 homodimer formation, and TLR4/MyD88/NF-κB signaling pathway activation. LM9 prevents atherosclerosis by regulating inflammatory responses and oxidative stress in macrophages. LM9 efficiently mitigates inflammatory responses and fibrosis in obesity-induced cardiomyopathy. LM9 can be used for fibrosis and atherosclerosis research.
    LM9
  • HY-RS11831
    Relb Rat Pre-designed siRNA Set A
    Inhibitor

    Relb Rat Pre-designed siRNA Set A contains three designed siRNAs for Relb gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

    Relb Rat Pre-designed siRNA Set A
  • HY-N11494
    Dauricumine
    Inhibitor
    Dauricumine is a chlorinated alkaloid that inhibits NF-κB ligand-induced differentiation of mouse bone marrow-derived macrophages into multinucleated osteoclasts.
    Dauricumine
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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