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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. Nom du produit Effet Pureté Chemical Structure
  • 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-165386
    TU-100
    Inhibitor
    TU-100 is a Japanese herbal medicine. TU-100 exhibits anti-cancer effects by regulating cancer-associated fibroblasts (CAFs) in the TME. TU-100 can antagonize the M2 polarization phenotype of macrophages in the tumor microenvironment by suppressing the TLR4/NF-κB/STAT3 axis. TU-100 can inhibit the high expression of MMP-2, COX-2, and VEGF in TAMs.
    TU-100
  • HY-150038
    NOSH-aspirin
    Inhibitor
    NOSH-aspirin (NBS-1120) is an orally active hybrid molecule that releases nitric oxide and hydrogen sulfide. NOSH-aspirin inhibits pancreatic cancer cell proliferation and induces apoptosis. NOSH-aspirin inhibits cancer cell growth and suppresses NF-κB and FoxM1 in a mouse model of pancreatic cancer. NOSH-aspirin also alleviates motor deficits and dopaminergic neuron degeneration in a rat model of Parkinson's disease. NOSH-aspirin reduces neuroinflammation caused by microglial and astrocytic activation. NOSH-aspirin can be used in research on cancers such as pancreatic cancer and neurological diseases such as Parkinson's disease.
    NOSH-aspirin
  • 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-P992060
    Anti-Mouse CD20 Antibody (18B12)
    Inhibitor
    Anti-Mouse CD20 Antibody (18B12) is a B cell depleting agent that targets mouse CD20. Anti-Mouse CD20 Antibody (18B12) not only inhibits the growth of mesothelioma, lung cancer and thymoma, but also significantly enhances the efficacy of adenoviral tumor antigen vaccines and induces tumor regression by increasing the number of tumor-specific CD8+ T cells. Anti-Mouse CD20 Antibody (18B12) reduces B cell infiltration into the central nervous system of mice with experimental autoimmune encephalomyelitis, and delays motor dysfunction and neuronal death after spinal cord injury by alleviating inflammatory responses and tissue damage. Anti-Mouse CD20 Antibody (18B12) is widely applicable to research in fields related to mesothelioma, lung cancer, thymoma, experimental autoimmune encephalomyelitis and spinal cord injury.
    Anti-Mouse CD20 Antibody (18B12)
  • HY-134844
    Ciapavir
    Activator
    Ciapavir (SBI-0953294) is a HIV-1 latency-reversing agent. Ciapavir reverses latent HIV-1 reservoir in vitro and in vivo without inducing systemic T cell activation or broad cytokine release. Ciapavir degrades cIAP1 and activates non-canonical NF-κB pathway. Ciapavir can be used for the research of HIV-1 infection.
    Ciapavir
  • HY-N6032
    Esculentoside B
    Inhibitor 99.88%
    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-180119
    IKKβ-IN-5
    Inhibitor
    IKKβ-IN-5 is an orally active and selective IKKβ inhibitor with an IC50 of 7.5 nM. IKKβ-IN-5 directly inhibits IKKβ phosphorylation and attenuates NF κB mediated inflammatory and survival signals while promoting autophagy flux. IKKβ-IN-5 exhibits a 6-fold selectivity forIKKβ over the homologous kinase IKKα. IKKβ-IN-5 exerts robust antiproliferative effects through a dual mechanism involving G₂/M phase cell cycle arrest and autophagy activation, even under inflammatory stimulation in vitro. IKKβ-IN-5 demonstrates favorable pharmacokinetics and suppresses tumor growth in vivo. IKKβ-IN-5 can be used for colorectal cancer and potentially other inflammation driven malignancies research.
    IKKβ-IN-5
  • 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
  • HY-118522
    TP-110
    Inhibitor
    TP-110 is a proteasome inhibitor. TP-110 specifically inhibits the protease-like activity of the 20S proteasome, but does not affect the trypsin-like or peptidyl-glutamyl peptide hydrolysis activity. TP-110 inhibits the NF-κB pathway, activates caspase-8, -9, and -3, and causes PARP cleavage, significantly reducing the levels of cIAP-1 and XIAP. TP-110 causes cell cycle arrest at the G2/M phase and promotes apoptosis of cancer cells. TP-110 can be used in cancer research of prostate cancer and multiple myeloma, etc.
    TP-110
  • HY-N0176S3
    Dihydroartemisinin-d5
    Inhibitor
    Dihydroartemisinin-d5 is deuterated labeled Dihydroartemisinin (HY-N0176). Dihydroartemisinin is a potent anti-malaria agent.
    Dihydroartemisinin-d<sub>5</sub>
  • HY-155821
    Anti-inflammatory agent 55
    Inhibitor
    Anti-inflammatory agent 55 (compound 9j) is a derivative of Coixol and has anti-inflammatory activity. Anti-inflammatory agent 54 inhibits the NF-κB pathway and downregulates the expression of iNOS, TNF-α, IL-6 and IL-1β. Anti-inflammatory agent 54 inhibits LPS-induced nitric oxide (NO) production in RAW264.7 macrophages (IC50: 0.8 μM) and exerts in vivo anti-inflammatory activity in a mouse auricular edema model.
    Anti-inflammatory agent 55
  • HY-117222
    AM-0216
    Inhibitor
    AM-0216 is a highly selective NF-κB-inducing kinase (NIK) inhibitor with a Ki value of 2 nM. AM-0216 is promising for research of NF-κB-dependent hematologic malignancies (e.g., multiple myeloma) and autoimmune diseases.
    AM-0216
Cat. No. Nom du produit / 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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