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-161850
    ULK1-IN-3
    Agonist
    ULK1-IN-3 (Compound 8) is a novel chromone-based as a potential inhibitor of ULK1. ULK1-IN-3 inhibits cell cycle, autophagy and induces apoptosis, oxidative stress in colon cancer cell lines.
    ULK1-IN-3
  • HY-RS11824
    Rel Mouse Pre-designed siRNA Set A
    Inhibitor

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

    Rel Mouse Pre-designed siRNA Set A
  • HY-128447R
    Allyl methyl sulfide (Standard)
    Inhibitor
    Allyl methyl sulfide (Standard) is the analytical standard of Allyl methyl sulfide (HY-128447). This product is intended for research and analytical applications. Allyl methyl sulfide is an orally active organic sulfide. Allyl methyl sulfide is one of the main active ingredients in garlic volatile metabolites. Allyl methyl sulfide can be extracted from garlic. Allyl methyl sulfide enhances SOD activity, inhibits NF-κB signaling pathway, and upregulates pancreatic GLUT2 expression. Allyl methyl sulfide has significant antioxidant, anti-inflammatory and hypoglycemic activities. Allyl methyl sulfide can be used in the research of diabetes and its complications.
    Allyl methyl sulfide (Standard)
  • HY-N3188
    Niloticin
    Inhibitor ≥98.0%
    Niloticin, tetracyclic triterpenoid compound, is a osteoclastogenesis inhibitor. Niloticin shows anti-viral, antioxidative, and mosquitocidal activities. Niloticin inhibits osteoclastogenesis by blocking RANKL-RANK interaction and suppressing the AKT, MAPK, and NF-κB signaling pathways.
    Niloticin
  • HY-N2453R
    Convallatoxin (Standard)
    Inhibitor
    Convallatoxin (Standard) is the analytical standard of Convallatoxin. This product is intended for research and analytical applications. Convallatoxin is a cardiac glycoside isolated from Adonis amurensis Regel et Radde. Convallatoxin ameliorates colitic inflammation via activation of PPARγ and suppression of NF-κB. Convallatoxin is a P-glycoprotein (P-gp) substrate and recognized Val982 as an important amino acid involved in its transport. Convallatoxin is an enhancer of ligand-induced MOR endocytosis with high potency and efficacy. Anti-inflammatory and anti-proliferative properties.
    Convallatoxin (Standard)
  • HY-W754303
    Dihydroartemisinin-13C,d5
    Dihydroartemisinin-13C,d5 (Dihydroqinghaosu-13C,d5) is the deuterium labeled and 13C-labeled Dihydroartemisinin (HY-N0176). Dihydroartemisinin is a potent anti-malaria agent.
    Dihydroartemisinin-<sup>13</sup>C,d<sub>5</sub>
  • HY-W010270A
    Aurothiomalate disodium
    Inhibitor
    Aurothiomalate (disodium) is a TRPA1 inhibitor. Aurothiomalate (disodium) inhibits NF-κB activation and iNOS expression. Aurothiomalate (disodium) promotes M2 transformation of macrophages and increases the expression of TREM-2 and arginase-1. Aurothiomalate (disodium) can be used in the study of liver fibrosis/cirrhosis and arthritis.
    Aurothiomalate disodium
  • HY-B0678S
    Metaxalone-d3
    Inhibitor ≥98.0%
    Metaxalone-d3 is the deuterium labeled Metaxalone. 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-d<sub>3</sub>
  • HY-156247
    IVMT-Rx-3
    Inhibitor
    IVMT-Rx-3 is a inhibitor of SDCBP targeting of the PDZ1 and PDZ2 Domains of MDA-9/Syntenin. IVMT-Rx-3 blocks MDA-9/Syntenin interaction with Src, reduces NF-κB activation, and inhibits MMP-2/MMP-9 expression. IVMT-Rx-3 inhibits Melanoma Metastasis[1]
    IVMT-Rx-3
  • HY-N0231R
    Bavachalcone (Standard)
    Inhibitor
    Bavachalcone (Standard) is the analytical standard of Bavachalcone. This product is intended for research and analytical applications. Bavachalcone is a potent inducer of apoptosis. Bavachalcone exerts anticancer activity by promoting autophagy and apoptosis in HepG2 cells. Bavachalcone acts as an anti-neuroinflammatory and antidepressant through the NF-κB pathway. Bavachalcone inhibits osteoclasts by interfering with ERK and Akt signaling pathways and the expression of c-Fos and NFATc1. Bavachalcone exhibits a significant inhibitory effect on baculovirus-expressed BACE-1 in vitro.
    Bavachalcone (Standard)
  • HY-118101
    15-Deoxy-Δ12,14-prostaglandin A1
    Inhibitor
    15-Deoxy-Δ12,14-prostaglandin A1 is a deoxyanalog of prostaglandins that inhibits NF-κB signaling and induces apoptosis. 15-Deoxy-Δ12,14-prostaglandin A1 inhibits TNF-α-induced upregulation of inflammatory endothelial cell adhesion molecule (CAM) and avoids monocyte arrest.
    15-Deoxy-Δ12,14-prostaglandin A1
  • HY-N0408R
    Picroside II (Standard)
    Inhibitor
    Picroside II (Standard) is the analytical standard of Picroside II. This product is intended for research and analytical applications. Picroside II, an iridoid compound extracted from Picrorhiza, exhibits anti-inflammatory and anti-apoptotic activities. picroside II alleviates the inflammatory response in sepsis and enhances immune function by inhibiting the activation of NLRP3 inflammasome and NF-κB pathways. Picroside II is an antioxidant, exhibits a significant neuroprotective effect through reducing ROS production and protects the blood-brain barrier (BBB) after cerebral ischemia-reperfusion (CI/R) injury. Picroside II has antioxidant, anti-inflammatory, immune regulatory, anti-virus and other pharmacological activities.
    Picroside II (Standard)
  • HY-B0808R
    Oxaprozin (Standard)
    Inhibitor
    Oxaprozin (Standard) is the analytical standard of Oxaprozin. This product is intended for research and analytical applications. Oxaprozin is an orally active and potent COX inhibitor, with IC50 values of 2.2 μM for human platelet COX-1 and and 36 μM for IL-1-stimulated human synovial cell COX-2, respectively. Oxaprozin also inhibits the activation of NF-κB. Oxaprozin induces cell apoptosis. Oxaprozin shows anti-inflammatory activity. Oxaprozin-mediated inhibition of the Akt/IKK/NF-κB pathway contributes to its anti-inflammatory properties.
    Oxaprozin (Standard)
  • HY-175026
    RIPK2-IN-8
    Inhibitor
    RIPK2-IN-8 is an orally active and highly selective RIPK2 inhibitor (IC50 = 11 nM). RIPK2-IN-8 is highly selective for RIPK2 over RIPK1 (IC50 > 30,000 nM) and has a moderate inhibitory effect on RIPK3 (IC50 = 44.61 nM). RIPK2-IN-8 inhibits the NOD2-RIPK2 signaling pathway and the expression of the inflammatory cytokines IL-6 and TNFα, thereby exerting anti-inflammatory effects. RIPK2-IN-8 has demonstrated anti-inflammatory and hepatoprotective effects in an acute liver injury (ALI) model and can be used in ALI research.
    RIPK2-IN-8
  • HY-P10350
    PapRIV
    Agonist
    PapRIV is an agonist of BV-2 microglial cells, capable of activating microglial cells through an NF-κB-dependent pathway. PapRIV induces the expression of pro-inflammatory cytokines such as IL-6 and TNFα and increases the production of reactive oxygen species (ROS). PapRIV can cross the blood-brain barrier.
    PapRIV
  • HY-142026
    Vitisin A
    Inhibitor
    Vitisin A has antioxidative, anticancer, antiapoptotic, neuroprotective and anti-inflammatory effects. Vitisin A inhibits LPS-induced NO and iNOS production via down-regulation of ERK1/2 and p38 and the NF-κB signal pathway. Vitisin A also inhibits adipocyte differentiation. Vitisin A is a resveratrol tetramer that can be isolated from Vitis vinifera roots.
    Vitisin A
  • HY-155759
    HMGB1-IN-2
    Inhibitor
    HMGB1-IN-2 (compound 15) is an inhibitor of highly conserved nuclear protein (HMGB1), showing NO inhibitory effect with IC50 value of 20.2 μM in RAW264.7 cells. HMGB1-IN-2 (30 μM) decreases the level of IL-1 β, TNF-α, caspase-1 p20, inhibits the phosphorylation of NF-κB p65, exhibits anti-apoptotic activity. HMGB1-IN-2 (15 mg/kg; ip) relives kidney injury in septic acute kidney injury mouse. HMGB1-IN-2 inhibits Huh7 cells and A549 cells with IC50s of 77.0 μM, and 82.0 μM, respectively.
    HMGB1-IN-2
  • HY-N8311
    Goshonoside F5
    Inhibitor
    Goshonoside F5 can be isolated from the unripe fruits of Rubus chingii. Goshonoside F5 has anti-inflammatory activity, and inhibits NF-κB and MAPK signaling pathway.
    Goshonoside F5
  • HY-N4093R
    Astringin (Standard)
    Inhibitor
    Astringin (trans-Astringin) (Standard) is the analytical standard of Astringin (HY-N4093). This product is intended for research and analytical applications. Astringin (trans-Astringin) is an orally active natural flavonoid compound. Astringin can inhibit the production of oxidative stress, inflammatory factors, etc. Astringin has multiple activities such as anti-oxidation, anti-inflammation, and anti-apoptosis. Astringin is also an inhibitor of ferroptosis. Astringin can be used in the research of diseases such as acute lung injury.
    Astringin (Standard)
  • HY-W754114
    Nalmefene Sulfate-d3
    Nalmefene Sulfate-d3 is the deuterium labeled Nalmefene (HY-107744). Nalmefene is a BBB-penetrable opioid receptor modulator. Nalmefene is an antagonist of MOR and DOR, and a partial agonist of KOR. Nalmefene has anti-inflammatory and neuroprotective activities. Nalmefene can be used in the research of reducing alcohol-dependent disorders.
    Nalmefene Sulfate-d<sub>3</sub>
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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