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-N4327
    Eurycomalactone
    		Inhibitor 98.99%
    Eurycomalactone is an active quassinoid could be isolated from Eurycoma longifolia Jack. Eurycomalactone is a potent NF-κB inhibitor with an IC50 value of 0.5 μM. Eurycomalactone inhibits protein synthesis and depletes cyclin D1. Eurycomalactone enhances radiosensitivity through arrest cell cycle at G2/M phase and delayed DNA double-strand break repair. Eurycomalactone inhibits the activation of AKT/NF-κB signaling, induces apoptosis and enhances chemosensitivity to Cisplatin (HY-17394).
    Eurycomalactone
  • HY-168710
    TLR4/NF-κB-IN-1
    		Inhibitor 99.92%
    TLR4/NF-κB-IN-1 (Compound 7x) is an orally available inhibitor that specifically targets the TLR4/NF-κB signaling pathway, offering anti-inflammatory effects and the ability to cross the blood-brain barrier. TLR4/NF-κB-IN-1 can reduce acute neuroinflammation in mice caused by LPS (HY-D1056) and downregulate the expression of TLR4, P-NF-κB and P-IκB-α proteins.
    TLR4/NF-κB-IN-1
  • HY-124958
    NDMC101
    		Inhibitor 99.91%
    NDMC101 is a potent osteoclastogenesis inhibitor and inhibits osteoclast differentiation via down-regulation of NFATc1-modulated gene expression. NDMC101 is similar to the DPP4 substrate and is a significant inhibitor of early T-cell activation via DPP4 inhibition. NDMC101can be used for study of bone disorders, such as rheumatoid arthritis, and synovial inflammation et al.
    NDMC101
  • HY-N8884
    Coelonin
    		Inhibitor ≥98.0%
    Coelonin is a dihydrophenanthrene with anti-inflammation activity. Coelonin inhibits LPS-induced PTEN phosphorylation. Coelonin inhibits NF-κB activation and p27Kip1 degradation by regulating the PI3K/AKT pathway negatively. Coelonin can inhibit IκBα phosphorylation and degradation and increases the expression of IκBα protein.
    Coelonin
  • HY-N11768
    4-Methoxylonchocarpin
    		Inhibitor ≥98.0%
    4-Methoxylonchocarpin is an orally active anti-inflammatory agent. 4-methoxylonchocarpin inhibits the binding of LPS to Toll-like Receptor (TLR) TLR4 to inhibit NF-κB activation and TNF Receptor and IL-6 expression. 4-Methoxylonchocarpin also inhibits the phosphorylation of TGF-beta activated kinase 1 and TNBS-induced expression of IL-1β, IL-17A, and TNF. 4-methoxylonchocarpin can improve 2,4, 6-trinitrobenzene sulfonic acid (TNBS)-induced colitis mouse model.
    4-Methoxylonchocarpin
  • HY-N6065
    Praeruptorin A
    		99.57%
    Praeruptorin A is a main bioactive constituent of Peucedanum praeruptorum (also known as Bai-Hua Qian Hu). Praeruptorin A exerts anti-inflammatory effects in vitro through inhibition of NF-κB activation.
    Praeruptorin A
  • HY-106029
    4α-TPA
    		Control ≥99.0%
    4α-TPA is an inactive form of TPA, and is used as a negative control for TPA-activated events.
    4α-TPA
  • HY-B0026
    Ceftiofur hydrochloride
    		Inhibitor 98.43%
    Ceftiofur hydrochloride is a cell wall synthesis inhibitor that targets bacterial penicillin-binding proteins (PBPs) and has anti-inflammatory effects in endotoxemia. Ceftiofur hydrochloride exerts bactericidal effects by inhibiting the synthesis of bacterial cell wall peptidoglycan, leading to bacterial cell lysis. Ceftiofur hydrochloride also inhibits the activation of NF-κB and MAPKs, thereby reducing the secretion of pro-inflammatory cytokines such as TNF-α, IL-1β, and IL-6.
    Ceftiofur hydrochloride
  • HY-N3097
    Pellitorine
    		Activator 99.84%
    Pellitorine is a bioactive natural amide compound. Pellitorine can competitively antagonize the activation of TRPV1 by Capsaicin (HY-10448), thereby reducing pain signal transmission. Pellitorine improves cognitive dysfunction by upregulating the BDNF-ERK1/2-CREB and Nrf2-HO-1 pathways. Pellitorine exerts anti-inflammatory and anti-sepsis effects by inhibiting the release of high mobility group protein B1 (HMGB1) and the expression of RAGE/TLR4. Pellitorine exerts its antithrombotic effect by prolonging the clotting time, inhibiting the activity of clotting factors and thrombin. Pellitorine inhibits lipid peroxidation and resists ferroptosis by upregulating GPX4 and DHODH. Pellitorine kills Aedes aegypti mosquito larvae by inhibiting V-type H⁺-ATPase and aquaporin 4 (AaAQP4). Pellitorine exhibits anti-cancer activity (e.g., leukemia and breast cancer) and has inhibitory effects on certain bacteria.
    Pellitorine
  • HY-162510
    SPDZi1
    		Inhibitor
    SPDZi1 is a potent and selective syntenin inhibitor that binds to PDZ1 and PDZ2 domains of syntenin. SPDZi1 binds to the syntenin PDZ tandem (STNPDZ) with a Kd of 3.6 μM. SPDZi1 suppresses glioblastoma and reduces the activation of NF-κB, a downstream effector of syntenin.
    SPDZi1
  • HY-N0073R
    Sarsasapogenin (Standard)
    		Inhibitor
    Sarsasapogenin (Standard) is the analytical standard of Sarsasapogenin. This product is intended for research and analytical applications. Sarsasapogenin is a sapogenin from the Chinese medical herb Anemarrhena asphodeloides Bunge, with antidiabetic, anti-oxidative, anticancer and anti-inflamatory activities.
    Sarsasapogenin (Standard)
  • HY-N8413
    Chlojaponilactone B
    		Inhibitor ≥98.0%
    Chlojaponilactone B is a lindenane-type sesquiterpenoid with anti-inflammatory properties. Chlojaponilactone B suppresses inflammatory responses by inhibiting TLR4 and subsequently decreasing reactive oxygen species (ROS) generation, downregulating the NF-κB, thus reducing the expression of the pro-inflammatory cytokines iNOS, NO, COX-2, IL-6 and TNF-α.
    Chlojaponilactone B
  • HY-123503
    Salicortin
    		Inhibitor
    Salicortin, a phenolic glycoside, has been isolated from many plants such as Populus and Salix species. Salicortin inhibits osteoclast differentiation and bone resorption by down-regulating JNK and NF-κB/NFATc1 signaling pathways. Salicortin has anti-amnesic, anti-adipogenic, and immune-modulatory activity.
    Salicortin
  • HY-N2192
    Swertianolin
    		Inhibitor 99.54%
    Swertianolin is a xanthone glycoside. Swertianolin can be isolated from plants of the Gentianaceae family (e.g., Gentiana campestris and Swertia punicea). Swertianolin inhibits p38 phosphorylation and NF-κB activation, and reduces NO and ROS production. Swertianolin exhibits anti-Helicobacter pylori activity with an IC50 of 6.1 μM and a minimum bactericidal concentration of 91.7 μM. Swertianolin modulates immune function in sepsis. Swertianolin is useful in the research of diseases such as Alzheimer's disease, hepatitis B, Helicobacter pylori infection, and sepsis.
    Swertianolin
  • HY-155765
    Anti-inflammatory agent 51
    		Inhibitor 98.08%
    Anti-inflammatory agent 51 (compound 11d) is an amide/sulfonamide derivative with anti-inflammatory activities. Anti-inflammatory agent 51 inhibits NF-κB activation, has the potential for acute lung injury and ulcerative colitis research.
    Anti-inflammatory agent 51
  • HY-N1365R
    Isoscopoletin (Standard)
    		Inhibitor
    Isoscopoletin (Standard) is the analytical standard of Isoscopoletin. This product is intended for research and analytical applications. Isoscopoletin (6-Hydroxy-7-methoxycoumarin) is an active constituent in Artemisia argyi leaves. Isoscopoletin shows substantial inhibition against cell proliferation, with IC50s of 4.0 μM and 1.6 μM for human CCRF-CEM leukaemia cells and multidrug resistant subline CEM/ADR5000, respectively. Isoscopoletin (6-Hydroxy-7-methoxycoumarin) possesses inhibitory activity against HBV replication. Isoscopoletin exhibits anti-inflammatory activity through inhibition of MAPK/NF-κB/STAT/AKT signaling pathway.
    Isoscopoletin (Standard)
  • HY-RS11823
    REL Human Pre-designed siRNA Set A
    		Inhibitor

    REL Human Pre-designed siRNA Set A contains three designed siRNAs for REL gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    REL Human Pre-designed siRNA Set A
  • HY-151876
    Glucocorticoid receptor modulator 1
    		Inhibitor 99.79%
    Glucocorticoid receptor modulator 1 is a highly potent and orally active non-steroidal selective glucocorticoid receptor modulator with an IC50 value of 9 nM and 130 nM for NF-κB and AP-1, respectively. Glucocorticoid receptor modulator 1 can effectively reduce the expression of inflammatory factors IL-6, IL-1β, TNF-α, also can relieve dermatitis in mice.
    Glucocorticoid receptor modulator 1
  • HY-125847
    Salvianolic acid F
    		Inhibitor 99.72%
    Salvianolic acid F is a KRAS inhibitor, especially for KRAS G12D. Salvianolic acid F inhibits NF-kB, MMP-9, and NO simultaneously. Salvianolic acid F inhibits cancer cell growth, invasion, and migration and induces apoptosis via the EP300/PI3K/AKT pathway in vitro. Salvianolic acid F inhibits the growth of KRAS-dependent lung cancer cells via the PI3K/AKT signaling pathway in vivo. Salvianolic acid F can be used in the research of various cancers, including KRAS G12D-driven non-small cell lung cancer (NSCLC) and ovarian cancer.
    Salvianolic acid F
  • HY-N1022
    11-Hydroxytephrosin
    		Inhibitor ≥98.0%
    11-Hydroxytephrosin is a potent inhibitor of NF-kappaB. NF-kappaB is known to play a crucial role in the regulation of genes controlling the immune system, apoptosis, tumor cell growth, and tissue differentiation.
    11-Hydroxytephrosin
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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