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-124281A
    9(S)-PAHSA
    Control
    9(S)-PAHSA is a S-enantiomer of 9-PAHSA. 9-PAHSA is an orally available anti-inflammatory lipid that lowers blood sugar and reduces inflammation.
    9(S)-PAHSA
  • HY-N8263
    Nepetoidin B
    Modulator
    Nepetoidin B, an anti-inflammatory agent, inhibits inflammation by modulating the NF-κB and Nrf2/HO-1 signaling pathways. Nepetoidin B also has antifungal and antibacterial activity. Nepetoidin B is a natural product that can be obtained from Salvia plebeia R. Br. Nepetoidin B can be used in anti-inflammatory and anti-infectious research.
    Nepetoidin B
  • 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-147377
    N-Salicyloyltryptamine
    Inhibitor
    N-Salicyloyltryptamine acts on voltage-dependent Na+, Ca2+, and K+ ion channels inhibitor. N-Salicyloyltryptamine inhibits K+ currents with an IC50 value of 34.6 μM (Ito). N-Salicyloyltryptamine also exhibits anticonvulsant, anti-inflammatory, analgesic, and vasorelaxation effect-.
    N-Salicyloyltryptamine
  • 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
  • HY-173129
    Anti-inflammatory agent 97
    Anti-inflammatory agent 97 (Compound 1l), an anti-inflammation agent, can also inhibit oxidative stress. Anti-inflammatory agent 97 can inhibit the colonic shortening and suppress inflammatory symptoms of the colonic tissue in the DSS (HY-116282C)-induced ulcerative colitis mice model. Anti-inflammatory agent 97 can regulate the inflammation-related TLR4/NF-κB signaling pathway and the oxidative stress-related Nrf2/HO-1 signaling pathway.
    Anti-inflammatory agent 97
  • HY-150587
    Anti-inflammatory agent 31
    Inhibitor
    Anti-inflammatory agent 31 (enone 17) is a kind of andrographolide derivatives, is a anti-inflammatory agent. Anti-inflammatory agent 31 inhibits NF-κB activation by upstream blockade of PI3K/Akt and ERK1/2 MAPK activation. Anti-inflammatory agent 31 shows recovery effective of the intracellular GSH levels and protective effect on liver.
    Anti-inflammatory agent 31
  • HY-N0603R
    20(S)-Ginsenoside Rg3 (Standard)
    Inhibitor
    20(S)-Ginsenoside Rg3 (Standard) is the analytical standard of 20(S)-Ginsenoside Rg3. This product is intended for research and analytical applications. 20(S)-Ginsenoside Rg3 is the main component of Panax ginseng C. A. Meyer. Ginsenoside Rg3 inhibits Na+ and hKv1.4 channel with IC50s of 32.2±4.5 and 32.6±2.2 μM, respectively. 20(S)-Ginsenoside Rg3 also inhibits Aβ levels, NF-κB activity, and COX-2 expression.
    20(S)-Ginsenoside Rg3 (Standard)
  • HY-161329
    NLRP3-IN-32
    Inhibitor
    NLRP3-IN-32 (compound 7a), a 3, 4-dihydronaphthalene-1(2H)-one derivative, is a potential NLRP3 inflammatory vesicles inhibitor. NLRP3-IN-32 can block the assembly and activation of NLRP3 inflammasome by down-regulating the expression of NLPR3 and apoptosis-associated speck-like protein containing a CARD (ASC), and inhibiting the production of reactive oxygen species (ROS) and other inflammatory mediators. NLRP3-IN-32 inhibits the phosphorylation of IκBα and NF-κB/p65 and the nuclear translocation of p65, thereby inhibiting NF-κB signaling.
    NLRP3-IN-32
  • HY-N2515R
    Ginsenoside Rk1 (Standard)
    Inhibitor
    Ginsenoside Rk1 (Standard) is the analytical standard of Ginsenoside Rk1. This product is intended for research and analytical applications. Ginsenoside Rk1 is a unique component created by processing the ginseng plant (mainly Sung Ginseng, SG) at high temperatures. Ginsenoside Rk1 has anti-inflammatory effect, suppresses the activation of Jak2/Stat3 signaling pathway and NF-κB. Ginsenoside Rk1 has anti-tumor effect, antiplatelet aggregation activities, anti-insulin resistance, nephroprotective effect, antimicrobial effect, cognitive function enhancement, lipid accumulation reduction and prevents osteoporosis. Ginsenoside Rk1 induces cell apoptosis by triggering intracellular reactive oxygen species (ROS) generation and blocking PI3K/Akt pathway.
    Ginsenoside Rk1 (Standard)
  • HY-N1380S3
    Guaiacol-d4
    Guaiacol-d4 is the deuterium labeled Guaiacol. Guaiacol, a phenolic compound, inhibits LPS-stimulated COX-2 expression and NF-κB activation. Anti-inflammatory activity.
    Guaiacol-d<sub>4</sub>
  • HY-163607
    SpiD3
    Inhibitor 98.24%
    SpiD3, a spirocyclic dimer, is an anticancer agent. SpiD3 markedly inhibits malignant B-cell proliferation and suppressed NF-κB activation independent of TME-associated stimuli. SpiD3 induces apoptosis and inhibits protein synthesis in chronic lymphocytic leukemia cells. SpiD3 can be used for study of chronic lymphocytic leukemia (CLL).
    SpiD3
  • HY-N11996
    Aloenin aglycone
    Aloenin aglycone (compound 13) is an NF-κB inhibitor that can be isolated from aloe exudate. Aloenin aglycone inhibits TNFα-induced NF-κB transcriptional activity (IC50: 18.7 μM). Aloenin aglycone (10 μM) also reduced inducible nitric oxide synthase (iNOS) and intercellular adhesion molecule 1 (ICAM-1) gene expression after treatment of HepG2 cells with 10 ng/mL TNFα.
    Aloenin aglycone
  • HY-B0678R
    Metaxalone (Standard)
    Inhibitor
    Metaxalone (Standard) is the analytical standard of Metaxalone. This product is intended for research and analytical applications. Metaxalone (AHR438; NSC170959) is an FDA-approved muscle relaxant. Metaxalone acts mainly on the central nervous system and achieves muscle relaxation by inhibiting polysynaptic reflex arcs. In addition, Metaxalone is an inhibitor of MAO-A, which has anti-inflammatory and antioxidant effects. Metaxalone inhibits IL-1β-induced inflammatory phenotype, modulates NF-κB and other related signaling pathways, and decreases MAO-A expression and activity in IL-1β-treated microglia.
    Metaxalone (Standard)
  • HY-E70291
    N-Acetylgalactosaminyltransferase 4
    Inhibitor
    N-Acetylgalactosaminyltransferase 4 (GALNT4) is a glycosyltransferase capable of inhibiting the activation of ASK1. By directly binding to ASK1, N-Acetylgalactosaminyltransferase 4 suppresses its N-terminal dimerization and subsequent phosphorylation, leading to robust inactivation of downstream JNK/p38 and NF-κB signals, and thereby improving the prognosis of liver surgery.
    N-Acetylgalactosaminyltransferase 4
  • HY-174382
    ROR1-IN-3
    Inhibitor
    ROR1-IN-3 (Compound 24d) is a potent and highly selective ROR1 kinase inhibitor (IC50 = 17.6 nM). ROR1-IN-3 demonstrates robust antitumor activity and inhibitory effect against ROR1 both in vitro and in vivo. ROR1-IN-3 has robust antiproliferative efficacy in vitro and in vivo. ROR1-IN-3 induces apoptosis in cancer cell lines. ROR1-IN-3 inhibits ROR1 downstream AKT/mTOR and NF-κB signaling pathway. ROR1-IN-3 can be studied in antitumor research.
    ROR1-IN-3
  • HY-131265
    Mesalamine impurity P
    Inhibitor
    Mesalamine impurity P is an impurity of Mesalamine (HY-15027). 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.
    Mesalamine impurity P
  • HY-N2526R
    Nervonic acid (Standard)
    Inhibitor
    Nervonic acid (Standard) is the analytical standard of Nervonic acid. This product is intended for research and analytical applications. Nervonic acid is a monounsaturated fatty acid with oral activity. Nervonic acid exerts anti-inflammatory activity by inhibiting NF-κB signaling. Nervonic acid can be used in the study of neurodegenerative diseases[1][2][3].
    Nervonic acid (Standard)
  • HY-N0141R
    Parthenolide (Standard)
    Inhibitor
    Parthenolide (Standard) is the analytical standard of Parthenolide. This product is intended for research and analytical applications. Parthenolide is a sesquiterpene lactone found in the medicinal herb Feverfew. Parthenolide exhibits anti-inflammatory activity by inhibiting NF-κB activation; also inhibits HDAC1 protein without affecting other class I/II HDACs.
    Parthenolide (Standard)
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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