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-N0809R
    Sesamolin (Standard)
    Inhibitor
    Sesamolin (Standard) is the analytical standard of Sesamolin. This product is intended for research and analytical applications. Sesamolin, isolated from Sesamum indicum, has antioxidative activity, Sesaminol inhibits lipid peroxidation and shows neuroprotection effect. Sesamolin potently inhibits MAPK cascades by preventing phosphorylation of JNK, p38 MAPKs, and caspase-3 but not ERK-MAPK expression.
    Sesamolin (Standard)
  • HY-P10854
    TAT-N15
    Inhibitor
    TAT-N15 is a p55PIK inhibitor with remarkable anti-inflammatory activity and neuroprotective effects. TAT-N15 can significantly inhibit the activation of IL-6, IL-8, Akt, and NF-κB pathways, as well as suppress the protein expression of phosphorylated STAT3 and NF-κB. By inhibiting the activation of Akt, STAT3, and NF-κB pathways, TAT-N15 is used in research on acute conjunctivitis, allergic rhinitis, chronic obstructive pulmonary disease (COPD), and stroke.
    TAT-N15
  • HY-RS09256
    Nfkb1 Rat Pre-designed siRNA Set A
    Inhibitor

    Nfkb1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Nfkb1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

    Nfkb1 Rat Pre-designed siRNA Set A
  • HY-139716
    IMD-catechol
    Modulator
    IMD-catechol is a novel imidazoquinolinone-NF-κB immunomodulator dimer that improves efficacy in a CT26 mouse colon carcinoma tumor model while eliciting minimal adjuvant toxicity.
    IMD-catechol
  • HY-122521
    Sootepin D
    Inhibitor
    Sootepin D (compound 6), a triterpene from the apical bud of Gardenia sootepensis, inhibits TNF-α-induced NF-κB activity with an IC50 of 8.3μM. Sootepin D has anti-inflammatory activity.
    Sootepin D
  • HY-P10469
    NBD-2
    Inhibitor
    NBD-2 is an inhibitor of the NEMO-IKKα/β interaction in the NF-κB signaling pathway. NBD-2 specifically inhibits the typical NF-κB signaling pathway in vitro and in vivo, reducing the inflammatory response in lipopolysaccharide (LPS) induced acute lung injury (ALI). NBD-2 exhibits significant anti-inflammatory activity. NBD-2 can be used to study diseases related to NF-κB signaling pathway, including autoimmune diseases, cancer, etc.
    NBD-2
  • HY-N0716BR
    Berberine sulfate (Standard)
    Inhibitor
    Berberine (sulfate) (Standard) is the analytical standard of Berberine (sulfate). This product is intended for research and analytical applications. Berberine sulfate is an alkaloid isolated from the Chinese herbal medicine Huanglian, as an antibiotic. Berberine sulfate induces reactive oxygen species (ROS) generation and inhibits DNA topoisomerase. Berberine sulfate has antineoplastic properties. The sulfate form improves bioavailability[1][2].
    Berberine sulfate (Standard)
  • HY-172088
    Tubulin/MMP-IN-3
    Inhibitor
    Tubulin/MMP-IN-3 (Compound 15j) is the dual inhibitor for tubulin polymerization and MMP, and inhibits MMP-2 and MMP-9 with IC50 of 21.13 μM and 19.24 μM. Tubulin/MMP-IN-3 inhibits NF-κB signaling pathway, causes mitochondrial dysfunction and the apoptosis through a mitochondrial-dependent pathway. Tubulin/MMP-IN-3 exhibits antiproliferative activity in a variety of cancer cells, arrests the cell cycle at G2/M phase, and exhibits antitumor efficacy in mouse models.
    Tubulin/MMP-IN-3
  • HY-162004
    NF-κB-IN-14
    Inhibitor
    NF-κB-IN-14 (compound 5e) significantly inhibits nitric oxide production in LPS-induced macrophages (IC50: 6.4 μM). NF-κB-IN-14 disrupts the TLR4-MyD88 protein interaction, leading to the suppression of the NF-κB signaling pathway suppression. NF-κB-IN-14 reduces ear edema and inflammation in an atopic dermatitis mouse model.
    NF-κB-IN-14
  • HY-B0516R
    Articaine hydrochloride (Standard)
    Inhibitor
    Articaine (Hoe-045) hydrochloride (Standard) is the analytical standard of Articaine hydrochloride (HY-B0516). This product is intended for research and analytical applications. Articaine (Hoe-045) hydrochloride is a selective inhibitor of voltage-gated sodium channels (such as rNav1.4, hNav1.7, and rNav1.8), with an IC50 of 15.8 μM for open-state Na+ channels, and IC50 of 40.6 μM and 378 μM for inactivated and resting-state Na+ channels, respectively. Articaine hydrochloride exerts local anesthetic activity by inhibiting Na+ influx to block nerve impulse conduction, and can also inhibit NF-κB activation and NLRP3 inflammasome pathways, exhibiting anti-inflammatory function. Articaine hydrochloride can be used in the study of dental local anesthesia and inflammatory-related diseases (such as acute kidney injury).
    Articaine hydrochloride (Standard)
  • HY-N10047
    7,8-Didehydrocimigenol
    Inhibitor
    7,8-Didehydrocimigenol is an active triterpenoid that can be isolated from Cimicifugae rhizoma. 7,8-Didehydrocimigenol inhibits TNF-α-induced VCAM-1 expression, inhibits NF-kB activity and phosphorylation of ERK1/2 and Akt, increases PPAR-γ expression. 7,8-Didehydrocimigenol can be used for the research of cardiovascular disorders such as atherosclerosis.
    7,8-Didehydrocimigenol
  • HY-N6032
    Esculentoside B
    Inhibitor
    Esculentoside B (Phytolaccoside B) is a natural product from the roots of Phytolacca acinosa Roxb. Esculentoside B is neurotoxic to zebrafish larvae, and impairs their central nervous system development. Esculentoside B inhibits inflammatory response and has antifungal activity.
    Esculentoside B
  • HY-RS11830
    Relb Mouse Pre-designed siRNA Set A
    Inhibitor

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

    Relb Mouse Pre-designed siRNA Set A
  • HY-N0591R
    Dehydrocostus Lactone (Standard)
    Inhibitor
    Dehydrocostus Lactone (Standard) ((-)-Dehydrocostus lactone (Standard)) is the analytical standard of Dehydrocostus Lactone (HY-N0591). This product is intended for research and analytical applications. Dehydrocostus Lactone is a natural sesquiterpene that can be isolated from Saussurea lappa. Dehydrocostus Lactone has multiple activities such as anti-inflammatory, antibacterial, anti-tumor, and immunomodulatory effects. Dehydrocostus Lactone has an MIC of 2 µg/mL against Mycobacterium tuberculosis. Dehydrocostus Lactone can also inhibit the killing activity of cytotoxic T lymphocytes and induce apoptosis in tumor cells.
    Dehydrocostus Lactone (Standard)
  • HY-176180
    PROTAC STING degrader-4
    Inhibitor
    PROTAC STING degrader-4 is a nitro-free covalent STING PROTAC degrader with a DC50 of 3.23 μM. PROTAC STING degrader-4 effectively inhibits STING as well as its downstream signaling, such as p-TBK1 and p-NF-κB (p-P65), and immune-inflammatory cytokines. PROTAC STING degrader-4 mitigates kidney and blood inflammation in Cisplatin (HY-17394)-induced acute kidney injury (AKI) mice model. Pink: STING ligand (HY-176183); Blue: CRBN ligase ligand (HY-103596); Black: linker (HY-176182); CRBN ligase ligand + linker: HY-176181
    PROTAC STING degrader-4
  • HY-W708917
    Lumichrome-d8
    Lumichrome-d8 is the deuterium labeled Lumichrome (HY-115385). Lumichrome, a photodegradation product of Riboflavin, is an endogenous compound in humans. Lumichrome inhibits human lung cancer cell growth and induces apoptosis via a p53-dependent mechanism. Lumichrom is the inhibitor for AKT/β-catenin signaling pathway.
    Lumichrome-d<sub>8</sub>
  • HY-B1328S1
    Pyridoxine-d3
    Inhibitor
    Pyridoxine-d3 is a deuterium labeled Pyridoxine. Pyridoxine (Pyridoxol) is a pyridine derivative. Pyridoxine exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway.
    Pyridoxine-d<sub>3</sub>
  • HY-P10797
    TAT-N24
    Inhibitor
    TAT-N24 is a cell-permeable TAT peptide as a p55PIK signaling inhibitor. TAT-N24 is effective for corneal neovascularization (CNV) and ocular inflammation by inhibiting the HIF-1α/NF-κB signaling pathway in corneal suture (CS). TAT-N24 also inhibits corneal neovascularization.
    TAT-N24
  • HY-14654C
    Aspirin calcium
    Inhibitor
    Aspirin calcium is an orally active, potent and irreversible inhibitor of cyclooxygenase COX-1 and COX-2, with IC50 values of 5 and 210 μg/mL, respectively. Aspirin calcium induces apoptosis. Aspirin calcium inhibits the activation of NF-κB. Aspirin calcium also inhibits platelet prostaglandin synthetase, and can prevent coronary artery and cerebrovascular thrombosis.
    Aspirin calcium
  • HY-112225
    Narasin sodium
    Narasin sodium is a cationic ionophore and coccidiostat agent. Narasin inhibits NF-κB signaling and induces tumor cells apoptosis. Narasin sodium has antimicrobial and anticancer activity.
    Narasin sodium
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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