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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
Art. -Nr. Produktname Wirkung Reinheit Chemical Structure
  • HY-183799
    GSI526
    		Inhibitor
    GSI526 is a IRAK4 PROTAC degrader (DC50=40.17 nM, Dmax=97%; THP-1) based on the VHL ubiquitin-proteasome system. GSI526 inhibits IRAK4-mediated NF-κB and MAPK inflammatory signaling pathways, and induces IRAK4 degradation in myeloid cells. GSI526 is applicable to inflammation-related research.
    GSI526
  • HY-RS11829
    RELB Human Pre-designed siRNA Set A
    		Inhibitor

    RELB Human Pre-designed siRNA Set A contains three designed siRNAs for RELB gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    RELB Human Pre-designed siRNA Set A
  • HY-P2358A
    PSMα3 TFA
    		Inhibitor
    PSMα3 TFA is an inhibitor of NF-κB p65 and p38 MAPK. PSMα3 TFA forms membrane pores and binds to residues of human insulin B chain to inhibit insulin aggregation. PSMα3 TFA forms α-type amyloid-like fibrils to exert cytotoxic effects, and acts as a functional amyloid virulence determinant of Staphylococcus aureus. PSMα3 TFA is applicable to research related to spondyloarthritis, rheumatoid arthritis, insulin-derived amyloidosis, and Staphylococcus aureus infection.
    PSMα3 TFA
  • HY-171895
    12-Nitrolinoleate
    		Inhibitor
    12-Nitrolinoleate (12-Nitro-9-cis,12-cis-octadecadienoic acid) is an activator for peroxisome proliferator-activated receptor γ (PPARγ). 12-Nitrolinoleate is a nitrated form of linoleic acid. 12-Nitrolinoleate can be formed upon exposure to acidified nitrate and found in human red blood cells and plasma. 12-Nitrolinoleate can activate PPARγ-dependent gene expression in MCF-7 cells expressing PPARγ with an EC50 = 0.045 μM. 12-Nitrolinoleate is able to inhibit LPS (HY-D1056)-induced NF-κB transcription in RAW 264.7 cells. 12-Nitrolinoleate can inhibit IL-6, TNF-α and CCL2 induced by LPS.
    12-Nitrolinoleate
  • HY-185344
    Ratutrelvir
    		Inhibitor
    Ratutrelvir is a NF-κB p65 inhibitor. Ratutrelvir blocks the translocation of NF-κB p65 from the cytoplasm to the nucleus, reduces the phosphorylation levels of NF-κB p65 and IκBα, and inhibits the DNA-binding activity of NF-κB p65. Ratutrelvir inhibits the migration and invasion abilities of breast cancer cells, and reduces their viability and colony-forming capacity. Ratutrelvir can be used for the research of luminal A breast cancer.
    Ratutrelvir
  • HY-179378
    XRF-1021
    		Inhibitor
    XRF-1021 is an orally active HIPK2 inhibitor (IC50 = 0.18 μM). XRF-1021 reduces the expression of fibrotic markers in TGF-β1 stimulated NRK-49F and HK-2 cells, including Fibronectin, Collagen I and α-SMA. XRF-1021 blocks TGF-β, NF-κB, p53, Wnt/β-catenin, and Notch signaling. XRF-1021 reduces renal injury and fibrosis in vivo. XRF-1021 can be used for the research of chronic kidney disease.
    XRF-1021
  • HY-B0705
    Desflurane
    Desflurane is an airway irritant, acts as an anesthesia agent.
    Desflurane
  • HY-N3364
    Lucidone
    		Inhibitor
    Lucidone, an anti-inflammatory agent that can be isolated from the fruit of Lindera erythrocarpa Makino. Lucidone inhibits LPS-induced NO and PGE2 production in RAW 264.7 mouse macrophages. Lucidone also decreases TNF-α secretion, iNOS and COX-2 expression. Lucidone prevents NF-κB translocation and inhibits JNK and p38MAPK signals. Lucidone also has inhibitory activity against Dengue virus (DENV) (EC50=25 μM).
    Lucidone
  • HY-N13614
    Centaurein
    		Activator
    Centaurein, a flavonoid, is an IFN-γ promoter enhancer. Centaurein up-regulates the activity of NFAT and NF-κB enhancers. Centaurein increases the IFN-γ expression in T and NK cells and the serum IFN-γ level in mice. Centaureidin completely relaxes the contractions in intact rat aortic rings. Centaurein effectively protects mice against Listeria infection[1][2][3][4].
    Centaurein
  • HY-W791754
    Paeonolsilate sodium
    		Inhibitor
    Paeonolsilate (sodium) can inhibit ox-LDL-induced macrophage foam cell formation and inflammation in atherosclerosis. Paeonolsilate (sodium) inhibits NF-κB activation and oxidative stress response induced by ox-LDL. Paeonolsilate (sodium) can be studied in anti-atherosclerosis research.
    Paeonolsilate sodium
  • HY-N0307R
    Ciwujianoside B (Standard)
    		Inhibitor
    Ciwujianoside B (Standard) is the analytical standard of Ciwujianoside B. This product is intended for research and analytical applications. Ciwujianoside B is an orally active, blood-brain barrier penetrable radioprotective agent and memory enhancer. Ciwujianoside B reduces radiation-induced DNA damage, cell cycle arrest and apoptosis, downregulates NF-κB and the Bax/Bcl-2 ratio, and enhances the proliferative capacity of bone marrow cells. Ciwujianoside B enhances object recognition memory in normal mice and induces dendritic extension in primary cultured cortical neurons. Ciwujianoside B can be used in studies related to hematopoietic system radiation injury and memory enhancement.
    Ciwujianoside B (Standard)
  • HY-117616
    Laurotetanine
    		Inhibitor
    Laurotetanine ((+)-Laurotetanine) is an potent and orally active isoquinoline alkaloid and could be extracted from the roots of Litsea cubeba (Lour.) Pers. Laurotetanine exerts an anti-asthmatic effect by inhibition of IgE, histamine, and inflammatory reactions via down-regulating MUC5AC and NF-κB signaling pathways.
    Laurotetanine
  • HY-181765
    TLR4/NF-κB-IN-2
    		Inhibitor
    TLR4/NF-κB-IN-2 is an orally active TLR4/NF-κB inhibitor and Nrf2/HO-1 activator. TLR4/NF-κB-IN-2 combats oxidative stress and exerts anti-inflammatory effects by regulating the Nrf2/HO-1 and TLR4/NF-κB pathways. TLR4/NF-κB-IN-2 reduces Aβ aggregation and protects neurons. TLR4/NF-κB-IN-2 can be used in the research of Alzheimer's disease.
    TLR4/NF-κB-IN-2
  • HY-124922
    CBLC100
    		Inhibitor
    CBLC100 is an anticancer compound that targets FACT, while inhibiting NF-κB and activating p53. CBLC100 induces cytotoxicity through p53-dependent apoptotic and non-apoptotic pathways. CBLC100 is applicable to the research of cancers such as fibrosarcoma.
    CBLC100
  • HY-P992408
    MEDI-5083
    		Activator
    MEDI-5083 is an Fc fusion protein that targets CD40 and is a CD40 agonist. MEDI-5083 stimulates CD40 signaling via NF-κB activation. MEDI-5083 upregulates MHCII, CD80, and CD86 expression, induces pro-inflammatory cytokine secretion, and enhances IFN-γ secretion by memory CD8+ T cells. MEDI-5083 can be used for the research of melanoma, colon carcinoma, and advanced solid tumors[1][2].
    MEDI-5083
  • HY-N18190
    N-Desmethyldauricine
    		Inhibitor
    N-Desmethyldauricine is a NF-κB p65 inhibitor and apoptosis inducer. N-Desmethyldauricine reduces the protein expression level of p65, induces apoptosis, arrests the cell cycle at the G0/G1 phase, attenuates intercellular adhesion, and inhibits the growth of 3D spheroids of triple-negative breast cancer. N-Desmethyldauricine can be used in studies related to triple-negative breast cancer.
    N-Desmethyldauricine
  • HY-N19717
    Bartogenic acid
    		Inhibitor
    Bartogenic acid is an orally active NF-κB inhibitor, found in Barringtonia racemosa fruits. Bartogenic acid increases catalase, superoxide dismutase (SOD), and glutathione levels. Bartogenic acid inhibits lipid peroxidation and suppresses inflammation markers. Bartogenic acid can be used for the research of ovarian cancer, skin cancer, and inflammatory conditions.
    Bartogenic acid
  • HY-N18225
    β-Curcumene
    		Inhibitor
    β-Curcumene is a sesquiterpene compound. β-Curcumene has the potential to act as a SIRT1 activator and a NF-κB inhibitor. β-Curcumene possesses a spicy and ginger-like aroma, and can serve as a raw material for flavors, fragrances and cosmetics. β-Curcumene can be used in the research of type 2 diabetes.
    β-Curcumene
  • HY-N15691A
    (E)-Tadehaginoside
    (E)-Tadehaginoside is the E-isomer of Tadehaginoside (HY-N15691). Tadehaginoside, a phenylpropanoid glycoside, is a regulator of lipogenesis and glucose consumption. Tadehaginoside has antioxygenic property. Tadehaginoside mediates liver protection against oxidative stress injury and inflammation by regulating Nrf2 and NF-κB signaling pathways in hepatocytes. Tadehaginoside can be used for the study of obesity and diabetes.
    (E)-Tadehaginoside
  • HY-106981
    Orazipone
    		Inhibitor
    Orazipone (OR 1384) is a small molecule immunomodulator with strong anti-inflammatory properties. Orazipone exerts its immunomodulatory effect by forming reversible thiol complexes, which bind to intracellular signaling proteins and the thiol groups of glutathione. Orazipone exhibits potent anti-eosinophilic activity by inducing apoptosis. Orazipone inhibits activation of inflammatory transcription factors NF-kB and STAT 1 and decreases inducible iNOS expression and NO production in response to inflammatory stimuli. Orazipone reduces NADPH oxidase activity and thereby decreases ROS production. Orazipone has a protective effect in intestinal radiation injury.
    Orazipone
Art. -Nr. Produktname / 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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