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-121955
    FW1256
    		Inhibitor
    FW1256 is a phenyl analogue and a slow-releasing hydrogen sulfide (H2S) donor. FW1256 inhibits NF-κB activity and induces cell apoptosis. FW1256 exerts potent anti-inflammatory effects and has the potential for cancer and cardiovascular disease treatment.
    FW1256
  • HY-100977
    Dimethoxycurcumin
    		Inhibitor 98.89%
    Dimethoxycurcumin is a derivative of curcumin that has anti-inflammatory and antioxidant activities.
    Dimethoxycurcumin
  • HY-N2590
    Lupenone
    		99.74%
    Lupenone is an orally active lupine-type triterpenoid that can be isolated from Musa basjoo. Lupenone Lupenone plays a role through the PI3K/Akt/mTOR and NF-κB signaling pathways. Lupenone has anti-inflammatory, antiviral, antidiabetic and anticancer activities.
    Lupenone
  • HY-164102
    TNF-α-IN-18
    		Inhibitor 98.94%
    TNF-α-IN-18 (Compound 61) is an inhibitor for TNF-α (IC50 of 1.8 μM), that inhibits TNF signaling pathway through block of NF-kB migration from cytoplasm to nucleus. TNF-α-IN-18 exhibits slight cytotoxicity to mouse fibroblast LM cell, with a CC50 >50 μM. TNF-α-IN-18 ameliorates the TNF- or Lipopolysaccharide (HY-D1056)-induced sepsis in mouse models. TNF-α-IN-18 protects mice from rheumatoid arthritis.
    TNF-α-IN-18
  • HY-N0427
    Phellodendrine
    		Inhibitor 99.60%
    Phellodendrine, a isoquinoline alkaloid, is one of important characteristic ingredients in the Phellodendron amurense. phellodendrine is against AAPH-induced oxidative stress through regulating the AKT/NF-κB pathway. Phellodendrine has good antioxidant, and anti-inflammatory effect .
    Phellodendrine
  • HY-P10030
    DPLG3
    		Inhibitor 99.18%
    DPLG3 is a specific chymotryptic-like β5i subunits inhibitor, with an IC50 of 4.5 nM. DPLG3 inhibits mouse i-20S with IC50 of 9.4 nM. DPLG3 downregulates the protein levels of NF-κB p50 and p65. DPLG3 can be used for immune disease research.
    DPLG3
  • HY-107566
    Conessine
    		Inhibitor 99.87%
    Conessine is an orally active and BBB-penetrable selective histamine H3 receptor antagonist. The pKi values of Conessine for rat and human H3 receptors are 7.61 and 8.27, respectively. Conessine is an inhibitor of the multidrug efflux pump system in Pseudomonas aeruginosa and can enhance the activity of antibiotics. Conessine has antimalarial activity. Conessine can also be used in the research of muscle atrophy.
    Conessine
  • HY-Y0586
    2,4,5-Trimethoxybenzoic acid
    		Inhibitor 99.98%
    2,4,5-Trimethoxybenzoic acid (Asaronic acid) is a compound identified in purple perilla extracts. 2,4,5-Trimethoxybenzoic acid inhibits LPS (HY-D1056)-induced inflammatory responses, inhibits the activation of NF-κB and STAT signaling pathways. 2,4,5-Trimethoxybenzoic acid inhibits M1 macrophage phenotype-mediated inflammation in diabetes.
    2,4,5-Trimethoxybenzoic acid
  • HY-N0492R
    α-Lipoic Acid (Standard)
    		Inhibitor 99.90%
    α-Lipoic Acid (Standard) is the analytical standard of α-Lipoic Acid. This product is intended for research and analytical applications. α-Lipoic Acid (Thioctic acid) is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid inhibits NF-κB-dependent HIV-1 LTR activation. α-Lipoic Acid induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells. α-Lipoic Acid can be used with CPUL1 (HY-151802) to construct the self-assembled nanoaggregate CPUL1-LA NA, which has improved antitumor efficacy than CPUL1.
    α-Lipoic Acid (Standard)
  • HY-12383
    Pelubiprofen
    		Inhibitor 99.27%
    Pelubiprofen is an orally active anti-inflammatory agent that inhibits COX enzyme activity (with IC50 values of 10.66 and 2.88 μM for COX-1 and COX-2, respectively). Pelubiprofen has significant anti-inflammatory and analgesic effects.
    Pelubiprofen
  • HY-N7980
    Rubipodanone A
    		Activator 99.40%
    Rubipodanone A, a naphthohydroquinone dimer, shows cytotoxicity against A549, BEL-7402, HeLa, HepG2, SGC-7901 and U251 cells. Rubipodanone A also shows obvious activating effect at 20 and 40 μM for NF-κB.
    Rubipodanone A
  • HY-N0197R
    Baicalin (Standard)
    		Inhibitor
    Baicalin (Standard) is the analytical standard of Baicalin. This product is intended for research and analytical applications. Baicalin, as a flavonoid glycoside, is an allosteric carnitine palmityl transferase 1 (CPT1) activator. Baicalin reduces the expression of NF-κB.
    Baicalin (Standard)
  • HY-32735S
    Triptolide-d3
    		Inhibitor
    Triptolide-d3 is the deuterium labeled Triptolide. Triptolide is a diterpenoid triepoxide extracted from the root of Tripterygium wilfordii with immunosuppressive, anti-inflammatory, antiproliferative and antitumour effects. Triptolide is a NF-κB activation inhibitor[1][2][3][4][5][6].
    Triptolide-d<sub>3</sub>
  • HY-N0208
    Kaempferol-3-O-glucorhamnoside
    		Inhibitor 99.64%
    Kaempferol-3-O-glucorhamnoside, a flavonoid derived from plant Thesium chinense Turcz, inhibits inflammatory responses via MAPK and NF-κB pathways in vitro and in vivo.
    Kaempferol-3-O-glucorhamnoside
  • HY-P1860A
    TNF-α (31-45), human TFA
    		Activator
    TNF-α (31-45), human TFA is a potent NF-kB pathway activator. TNF-αis a proinflammatory cytokine that induces necrosis or apoptosis. TNF alpha stimulates NF-κB pathway via TNFR2 promotes cancer growth, invasion, and metastasis.
    TNF-α (31-45), human TFA
  • HY-111954
    (+)-Erinacin A
    		99.97%
    (+)-Erinacin A (Erinacine A) is a cyanoditerpenoid isolated from Hericium erinaceus with anticancer, anti-inflammatory and neuroprotective activities. (+)-Erinacin A can induce cancer cell death by activating extrinsic and intrinsic apoptosis pathways. (+)-Erinacin A can also inhibit the expression of NO synthase (iNOS) and the production of nitrotyrosine to exert inflammatory and neuroprotective effects, thereby reducing ischemic brain damage.
    (+)-Erinacin A
  • HY-106449
    Recoflavone
    		Inhibitor ≥98.0%
    Recoflavone (DA-6034 (free acid)), a synthetic derivative of the flavonoid Eupatilin (HY-N0783), is orally active. Recoflavone can inhibit the NF-κB pathway and induce [Ca(2+)]i increase in epithelial cells. Recoflavone exhibits activities such as anti-inflammation, anti-tumor effects, protection of gastric and intestinal mucosa, and promotion of secretion in the ocular surface and salivary glands. Recoflavone can be used for the research of diseases such as dry eye, gastric injury, and intestinal injury.
    Recoflavone
  • HY-N3796
    Echinulin
    		Activator 98.63%
    Echinulin (Echinuline) is a cyclic dipeptide carrying a triprenylated indole moiety. Echinulin contributes to the activation of T cell subsets, which leads to NF-κB activation.Echinulin exerts its immune roles by the NF-κB pathway.Echinulin has the potential to serve as a immunotherapeutic agent.
    Echinulin
  • HY-N2106
    Dehydroevodiamine
    		99.93%
    Dehydroevodiamine is a major bioactive quinazoline alkaloid isolated from Evodiae Fructus, has an antiarrhythmic effect in guinea-pig ventricular myocytes. Dehydroevodiamine inhibits LPS-induced iNOS, COX-2, prostaglandin E2 (PGE2) and nuclear factor-kappa B (NF-κB) expression in murine macrophage cells.
    Dehydroevodiamine
  • HY-13010S
    Laquinimod-d5
    		Inhibitor 98.25%
    Laquinimod-d5 (ABR-215062-d5) is deuterium labeled Laquinimod. Laquinimod (ABR-215062), an orally available carboxamide derivative, is a potent immunomodulator that prevents neurodegeneration and inflammation in the central nervous system. Laquinimod reduces astrocytic NF-κB activation to protect from Cuprizone-induced demyelination. Laquinimod has the potential for relapsing-remitting (RR) and chronic progressive (CP) forms of multiple sclerosis (MS; RRMS or CPMS) as well as neurodegenerative diseases research.
    Laquinimod-d<sub>5</sub>
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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