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-N1333
    Rubioncolin C
    Inhibitor
    Rubioncolin C exerts anti-tumor activity by inducing apoptotic and autophagic Cell Death and inhibiting the NF-κB and Akt/mTOR/P70S6K Pathway in Human Cancer Cells.
    Rubioncolin C
  • HY-N0705R
    Curculigoside (Standard)
    Inhibitor
    Curculigoside (Standard) is the analytical standard of Curculigoside. This product is intended for research and analytical applications. Curculigoside is the main saponin in C. orchioide, exerts significant antioxidant, anti-osteoporosis, antidepressant and neuroprotection effects. Curculigoside possesses significant anti-arthritic effects in vivo and in vitro via regulation of the JAK/STAT/NF-κB signaling pathway.
    Curculigoside (Standard)
  • HY-N0256R
    Hederagenin (Standard)
    Inhibitor
    Hederagenin (Standard) is the analytical standard of Hederagenin. This product is intended for research and analytical applications. Hederagenin is a triterpenoid saponin with orally active and antitumor activity. Hederagenin can inhibit the expression of iNOS, COX-2, and NF-κB in cells induced by LPS stimulation. Hederagenin also increases ROS production in cancer cells, disrupts mitochondrial membrane potential, and induces apoptosis. Hederagenin also sensitizes cancer cells to Cisplatin (HY-17394) and Paclitaxel (HY-B0015), enhancing induced apoptosis. Hederagenin also has preventive potential against alcoholic liver injury.
    Hederagenin (Standard)
  • HY-N10312
    Yadanzigan
    Inhibitor
    Yadanzigan (YDZG) is an anti-inflammatory agent and a NLRP3 inhibitor. Yadanzigan specifically inhibits NLRP3 activation via inhibiting NF-κB pathway and Reactive Oxygen Species production. Yadanzigan also moderates LPS (HY-D1056)-induced acute lung injury (ALI) in mice.
    Yadanzigan
  • HY-P991475
    MG-1131
    Activator
    MG-1131 is a human monoclonal antibody (mAb) targeting TIGIT. MG-1131 activates NF-κB signaling in T cells and enhances NK-mediated tumor killing activity in a PVR-dependent manner. MG-1131 blocks TIGIT to increase IFN-γ secretion. MG-1131 can be used in anti-tumor immunity research. Recommended isotype control: Human IgG1 kappa, Isotype Control (HY-P99001).
    MG-1131
  • HY-W550315
    Dimethyl diacetyl cystinate
    Inhibitor
    Dimethyl diacetyl cystinate (DACDM) is a potent NF-κB inhibitor. Dimethyl diacetyl cystinate shifts the intracellular redox balance toward the oxidized state by increasing intracellular oxidized glutathione (GSSG) content, competitively blocking the binding of activated NF-κB to DNA, thereby inhibiting the production of inflammatory factors such as IL-1κ. Dimethyl diacetyl cystinate is promising for research of UVB-induced skin inflammation and related oxidative stress diseases.
    Dimethyl diacetyl cystinate
  • HY-146561
    S-HP210
    Modulator 98.12%
    S-HP210 is a potent and selective glucocorticoid receptor (GR) with an IC50 value of 1.92 μM for NF-κB transrepression (TR). S-HP210 represses the LPS-induced transcription of a variety of proinflammatory genes such as IL-1β, IL-6 and COX-2. S-HP210 is nontoxic at effective doses against mouse fibroblasts 3T3 cells.
    S-HP210
  • HY-N0587R
    Demethylzeylasteral (Standard)
    Inhibitor
    Demethylzeylasteral (Standard) is the analytical standard of Demethylzeylasteral. This product is intended for research and analytical applications. Demethylzeylasteral is an orally active triterpenoid compound isolated from Tripterygium wilfordii, which has functions such as anti-inflammatory, anti-tumor, anti fertility, estrogen metabolism regulation, immune suppression, and immune system regulation .
    Demethylzeylasteral (Standard)
  • HY-145439
    Colistin adjuvant-1
    Inhibitor
    Colistin adjuvant-1 is a colistin adjuvant, shows increased colistin potentiation activity against Gram-negative bacteria. Colistin adjuvant-1 inhibits NF-κB with an IC50 of 0.209 μM.
    Colistin adjuvant-1
  • HY-N3097R
    Pellitorine (Standard)
    Activator
    Pellitorine (Standard) is the analytical standard of Pellitorine (HY-N3097). 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 (Standard)
  • HY-N11777
    (−)-N-Hydroxyapiosporamide
    Inhibitor
    (−)-N-Hydroxyapiosporamide (NHAP), an alkaloid, is an NF-κB inhibitor with potent antitumor activity in vitro and in vivo. (−)-N-Hydroxyapiosporamide can be used for the research of colorectal cancer (CRC).
    (−)-N-Hydroxyapiosporamide
  • HY-N2585
    Isodeoxyelephantopin
    Inhibitor ≥98.0%
    Isodeoxyelephantopin is a sesquiterpene lactone isolated from Elephantopus scaber. Isodeoxyelephantopin induces ROS generation, suppresses NF-κB activation. Isodeoxyelephantopin also modulates LncRNA expression and exhibit activities against breast cancer.
    Isodeoxyelephantopin
  • HY-N0807R
    Swertiamarin (Standard)
    Modulator
    Swertiamarin (Standard) is the analytical standard of Swertiamarin. This product is intended for research and analytical applications. Swertiamarin is an orally active iridoid compound with hypoglycemic, hypolipidemic, anti rheumatic and antioxidant activities, which can be used in the research of diabetes and arthritis.
    Swertiamarin (Standard)
  • HY-N0492AR
    α-Lipoic Acid sodium (Standard)
    Inhibitor
    α-Lipoic Acid (sodium) (Standard) is the analytical standard of α-Lipoic Acid (sodium). This product is intended for research and analytical applications. α-Lipoic Acid (Thioctic acid) sodium is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid sodium inhibits NF-κB-dependent HIV-1 LTR activation[1][2][3]. α-Lipoic Acid sodium induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells[4]. α-Lipoic Acid sodium can be used with CPUL1 (HY-151802) to construct the self-assembled nanoaggregate CPUL1-LA NA, which has improved antitumor efficacy than CPUL1[5].
    α-Lipoic Acid sodium (Standard)
  • HY-P10897
    SjDX5-271
    Inhibitor
    SjDX5-271 is a small 3 kDa peptide. SjDX5-271 inhibits the TLR4/MyD88/NF-κB signaling pathway. SjDX5-271 induces cell polarization. SjDX5-271 alleviats hepatic inflammation. SjDX5-271 protects mice against liver ischemia-reperfusion injury.
    SjDX5-271
  • HY-161627
    Anemoside A3-methyl 6-aminohexanoate
    Inhibitor
    Anemoside A3-methyl 6-aminohexanoate (Compound A3-6) is a derivative of Pulchinenoside C (Anemoside B4) (HY-N0205). Anemoside A3-methyl 6-aminohexanoate inhibits pyruvate carboxylase (PC) with an IC50 of 0.058 μM, reprograms macrophage function, and alleviates DSS-induced colitis through inhibition of the NF-κB and NLRP3 inflammasome pathway. Anemoside A3-methyl 6-aminohexanoate exhibits a moderate in vivo pharmacokinetic characters compared with Anemoside B4.
    Anemoside A3-methyl 6-aminohexanoate
  • HY-RS11828
    Rela Rat Pre-designed siRNA Set A
    Inhibitor

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

    Rela Rat Pre-designed siRNA Set A
  • HY-142963
    TLR4/NF-κB/MAPK-IN-1
    TLR4/NF-κB/MAPK-IN-1 is a new type of antineuroinflammatory agent by suppressing TLR4/NF-kB/MAPK pathways.
    TLR4/NF-κB/MAPK-IN-1
  • HY-171579
    RS47
    Inhibitor
    RS47 (Compound 1a) is a selective inhibitor of the non-canonical NF-κB signaling pathway targeting RelB with a Kd of 1.1 μM. RS47 competitively blocks RelB binding to target DNA, inhibiting downstream gene (e.g., BCL3, PIM2) expression, thereby suppressing tumor cell proliferation. RS47 is promising for research of cancers with aberrant activation of the non-canonical NF-κB pathway, such as colorectal cancer and B lymphoma.
    RS47
  • HY-119731
    Antidesmone
    Inhibitor
    Antidesmone is a isoquinoline alkaloid that can be isolated from Antidesma membranaceum. Antidesmone can prevent acute lung injury in vivo via inhibiting MAPK and NF-κb activities.
    Antidesmone
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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