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-N0919
    Yangonin
    Inhibitor 99.79%
    Yangonin exhibits affinity for the human recombinant cannabinoid CB1 receptor with an IC50 and a Ki of 1.79 μM and 0.72 μM, respectively.
    Yangonin
  • HY-N2119
    Sciadopitysin
    Inhibitor 99.19%
    Sciadopitysin is a type of biflavonoids in leaves from ginkgo biloba. Sciadopitysi inhibits RANKL-induced osteoclastogenesis and bone loss by inhibiting NF-κB activation and reducing the expression of c-Fos and NFATc1.
    Sciadopitysin
  • HY-B0130A
    Perindopril erbumine
    99.98%
    Perindopril erbumine is an angiotensin-converting enzyme inhibitor. Perindopril erbumine modulates NF-κB and STAT3 signaling and inhibits glial activation and neuroinflammation. Perindopril erbumine can be used for the research of Chronic Kidney Disease and high blood pressure.
    Perindopril erbumine
  • HY-N0222
    Avicularin
    Inhibitor 99.80%
    Avicularin is an orally active flavonoid. Avicularin inhibits NF-κB (p65), COX-2 and PPAR-γ activities. Avicularin has anti-inflammatory, anti-infectious anti-allergic, anti-oxidant, hepatoprotective, and anti-tumor activities.
    Avicularin
  • HY-N0694
    Schisantherin A
    Inhibitor 99.87%
    Schisantherin A is a dibenzocyclooctadiene lignan. Schisantherin A inhibits p65-NF-κB translocation into the nucleus by IκBα degradation.
    Schisantherin A
  • HY-128423
    Tylvalosin tartrate
    Inhibitor 98.77%
    Tylvalosin (Acetylisovaleryltylosin) tartrate is an orally active, broad-spectrum macrolide antibiotic with antimicrobial activity. Tylvalosin tartrate is an antiviral agent useful in studying PRRSV infection. Tylvalosin tartrate induces apoptosis. Tylvalosin tartrate also has anti-inflammatory activity, relieves oxidative stress, and alleviates acute lung injury by inhibiting NF-κB activation.
    Tylvalosin tartrate
  • HY-N0766
    Isorhynchophylline
    Inhibitor 99.82%
    Isorhynchophylline is an alkaloid isolated from Crocus sativus with anticancer, antihypertensive, anti-inflammatory, and neuroprotective properties. Isorhynchophylline can be applied to cardiovascular and neurological disorders, and cancer studies.
    Isorhynchophylline
  • HY-108065A
    3'-Sialyllactose sodium
    Inhibitor ≥98.0%
    3'-Sialyllactose (3'-SL) sodium is a prebiotic, maintains immune homeostasis and exerts anti-inflammatory and anti-arthritic effects. 3'-Sialyllactose sodium is an ordinary carbohydrate with the lowest toxicity rating, it can be used for the research of inflammation.
    3'-Sialyllactose sodium
  • HY-133987
    AP-1/NF-κB activation inhibitor 1
    Inhibitor 99.03%
    AP-1/NF-κB activation inhibitor 1 is a potent AP-1 and NF-κB mediated transcriptional activation inhibitor (IC50=1 μM), without blocking basal transcription driven by the β-actin promoter. AP-1/NF-κB activation inhibitor 1 has a similar inhibitory effect on the production of IL-2 and IL-8 levels in stimulated cells.
    AP-1/NF-κB activation inhibitor 1
  • HY-N0602
    Ginsenoside Rg2
    Inhibitor 98.11%
    Ginsenoside Rg2 is one of the major active components of ginseng. Ginsenoside Rg2 inhibits VCAM-1 and ICAM-1 expressions stimulated with lipopolysaccharide (LPS). Ginsenoside Rg2 also reduces 1-42 accumulation.
    Ginsenoside Rg2
  • HY-P1832A
    PTD-p65-P1 Peptide TFA
    Inhibitor 99.14%
    PTD-p65-P1 Peptide TFA is a potent, selective nuclear transcription factor NF-κB inhibitor and derives from the p65 subunit of NF-κB amino acid residues 271-282, which selectively inhibits NF-κB activation induced by various inflammatory stimulation, down-regulate NF-κB-mediated gene expression and up-regulate apoptosis.
    PTD-p65-P1 Peptide TFA
  • HY-N2534
    Karanjin
    Inhibitor 99.75%
    Karanjin is an orally active furanoflavonoid which can be isolated from several Leguminosae. Karanjin exhibits evident anti-diabetic, anti-cancer, anti-inflammatory, antioxidant, anticolitis, anti-ulcer, anti-Alzheimer properties and multiple insect repellent/insecticidal, acaricide properties, suggesting the potential of Karanjin to be applied to relevant research.
    Karanjin
  • HY-14592
    Tectochrysin
    Inhibitor 99.88%
    Tectochrysin (Techtochrysin) is one of the major flavonoids of Alpinia oxyphylla Miquel. Tectochrysin inhibits activity of NF-κB.
    Tectochrysin
  • HY-N0807
    Swertiamarin
    Modulator 99.03%
    Swertiamarin is an orally active natural product with hypoglycemic, lipid-lowering, anti-rheumatic, and antioxidant activities. Swertiamarin can regulate the levels of pro-inflammatory cytokines, MMP, and NF-κB, and promote osteoblast proliferation. Swertiamarin has antioxidant and hepatoprotective effects against carbon tetrachloride induced rat liver toxicity through the Nrf2/HO-1 pathway. Swertiamarin can attenuate inflammatory mediators by regulating JAK2/STAT3 transcription factors in adjuvant induced arthritis rats. Swertiamarin can be used in the research of diabetes and arthritis.
    Swertiamarin
  • HY-126382
    Hesperidin methylchalcone
    Inhibitor ≥98.0%
    Hesperidin methylchalcone (Hesperidin methyl chalcone) is an orally active flavonoid that has analgesic, anti-inflammatory and antioxidant properties. Hesperidin methylchalcone exhibits vasoprotective activity. Hesperidin methylchalcone inhibits oxidative stress, cytokine production and NF-κB activation. Hesperidin methylchalcone can be used for the research of gout disease.
    Hesperidin methylchalcone
  • HY-N1486
    Ursonic acid
    Inhibitor 98.15%
    Ursolic acid is a naturally occurring triterpenoid that has orally active. Ursolic acid induces the apoptosis of human cancer cells through multiple signaling pathways. Ursolic acid has anti-inflammatory and anticarcinogenic activity.
    Ursonic acid
  • HY-B0185R
    Lidocaine (Standard)
    Inhibitor 99.85%
    Lidocaine (Standard) is the analytical standard of Lidocaine. This product is intended for research and analytical applications. Lidocaine (Lignocaine) inhibits sodium channels involving complex voltage and using dependence. Lidocaine decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine is an amide derivative and has potential for the research of ventricular arrhythmia.
    Lidocaine (Standard)
  • HY-N2908
    Atraric acid
    Inhibitor 99.94%
    Atraric acid (Methyl atrarate) is a specific androgen receptor (AR) antagonist with anti-inflammatory and anticancer effects. Atraric acid represses the expression of the endogenous prostate specific antigen gene in both LNCaP and C4-2 cells. Atraric acid can also inhibit the synthesis of NO and cytokine, and suppress the MAPK-NFκB signaling pathway. Atraric acid can be used to research prostate diseases and inflammatory diseases.
    Atraric acid
  • HY-124179
    IT-901
    Inhibitor ≥99.0%
    IT-901 is an orally active and potent NF-κB subunit c-Rel inhibitor with an IC50 of 0.1 μM, 3 μM for NF-κB DNA binding and c-Rel DNA binding, respectively. IT-901, a bioactive naphthalenethiobarbiturate derivative, has the potential for human lymphoid tumors and ameliorate graft-versus-host disease (GVHD).
    IT-901
  • HY-13010
    Laquinimod
    Inhibitor 99.96%
    Laquinimod (ABR-215062), an orally available carboxamide derivative, is a potent immunomodulator which 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
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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