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-B2082R
    Fursultiamine (Standard)
    Inhibitor
    Fursultiamine (Standard) is the analytical standard of Fursultiamine. This product is intended for research and analytical applications. Fursultiamine is a vitamin B1 derivative, has anti-nociceptive and antineoplastic activity. Fursultiamine can be used for vitamin B1 deficiency, osteoarthritis (OA) and cancer research.
    Fursultiamine (Standard)
  • HY-N0738R
    Stachydrine hydrochloride (Standard)
    Inhibitor
    Stachydrine hydrochloride (Standard) is the analytical standard of Stachydrine hydrochloride. This product is intended for research and analytical applications. Stachydrine hydrochloride is the major active constituent of Leonurus artemisia, which is a potential therapy for cardiovascular diseases. Stachydrine can inhibit the NF-κB signal pathway. Anti-hypertrophic activities.
    Stachydrine hydrochloride (Standard)
  • HY-W062904
    Laquinimod sodium
    Inhibitor
    Laquinimod (ABR-215062) sodium, an orally available carboxamide derivative, is a potent immunomodulator which prevents neurodegeneration and inflammation in the central nervous system. Laquinimod sodium reduces astrocytic NF-κB activation to protect from Cuprizone-induced demyelination. Laquinimod sodium 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 sodium
  • HY-N0629R
    Maslinic acid (Standard)
    Inhibitor
    Maslinic acid (Standard) is the analytical standard of Maslinic acid. This product is intended for research and analytical applications. Maslinic acid can inhibit the DNA-binding activity of NF-κB p65 and abolish the phosphorylation of IκB-α, which is required for p65 activation.
    Maslinic acid (Standard)
  • HY-144745
    HSR1304
    Inhibitor
    HSR1304 (Compound 5d) is a potent inhibitor of NFκB. The multifunctional transcription factor, nuclear factor-κB (NF-κB), is broadly involved in multiple human diseases, such as cancer and chronic inflammation. HSR1304 has the potential for the research of cancer diseases.
    HSR1304
  • HY-14654A
    Aspirin lithium
    Inhibitor
    Aspirin (Acetylsalicylic Acid) lithium 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 lithium induces apoptosis. Aspirin lithium inhibits the activation of NF-κB. Aspirin lithium also inhibits platelet prostaglandin synthetase, and can prevent coronary artery and cerebrovascular thrombosis.
    Aspirin lithium
  • HY-B0008A
    Sulindac sodium
    Inhibitor
    Sulindac (MK-231) is an orally active nonsteroidal anti-inflammatory agent. Sulindac also is an immunomodulatory agent. Sulindac can be used for the research of arthritis of the spine, gouty arthritis and kinds of cancer including colorectal cancer (CRC) and lung cancer.
    Sulindac sodium
  • HY-142119
    Penehyclidine
    Activator
    Penehyclidine, a anticholinergic agent, is a selective antagonist of M1 and M3 receptors. Penehyclidine activates NF-kβ in lung tissue and inhibits the release of inflammatory factors. Penehyclidine can alleviate the pulmonary inflammatory response in rats with chronic obstructive pulmonary disease (COPD) undergoing mechanical ventilation.
    Penehyclidine
  • HY-100507A
    Avadomide hydrochloride
    Inhibitor
    Avadomide hydrochloride (CC 122 hydrochloride) is the hydrochloride form of Avadomide (HY-100507). Avadomide hydrochloride is an orally active cereblon modulator. Avadomide hydrochloride modulates cereblon E3 ligase activity, inhibits NF-κB pathway, arrests the cell cycle at G1 phase, and thus induces apoptosis in cancer cell PDAC. Avadomide hydrochloride exhibits potent antitumor and immunomodulatory activities.
    Avadomide hydrochloride
  • HY-N0176S
    Dihydroartemisinin-d3
    Inhibitor
    Dihydroartemisinin-d3 is the deuterium labeled Dihydroartemisinin. Dihydroartemisinin is a potent anti-malaria agent.
    Dihydroartemisinin-d<sub>3</sub>
  • HY-170692
    Hypoglycemic agent 3
    Inhibitor
    Hypoglycemic agent 3 (Compound H26), a derivative of corosolic acid, exhibits lipid-lowering and significant hypoglycemic effects and can be used as a hypoglycemic agent. Hypoglycemic agent 3 inhibits insulin resistance by targeting MCCC1 and can be used in the study of type 2 diabetes.
    Hypoglycemic agent 3
  • HY-W097625
    6-Methoxyflavone
    Inhibitor 99.87%
    6-Methoxyflavone is a methoxyflavone that can be isolated from Pimelea simplex F. Muell. and P. decora Domin.. 6-Methoxyflavone exhibits anti-inflammatory effects and neuropathic pain relieving properties in chemotherapy-induced peripheral neuropathy (CIPN). 6-Methoxyflavone can be used in the research of nephritis.
    6-Methoxyflavone
  • HY-135702
    UBS109
    Inhibitor 99.20%
    UBS109, as a curcumin analogue, can promote the differentiation and mineralization of osteoblasts. UBS109 shows to regulate bone cell function by activating Smad and inhibiting NF-kB. UBS109 can be used in bone tissue engineering and osteoporosis research.
    UBS109
  • HY-170579
    Antioxidant agent-20
    Inhibitor
    Antioxidant agent-20 (Compound 3d) has potent anti-inflammatory and antioxidant activity. Antioxidant agent-20 reduces reactive oxygen species (ROS) and apoptosis in a dose-dependent manner. Antioxidant agent-20 exhibits photoprotective effect against UVB-irradiated human skin keratinocytes (HaCaT) (IC50=5.13 µM) via activation of Nrf2/HO-1 signaling and inhibition of NF-κB pathway.
    Antioxidant agent-20
  • HY-N2381R
    Menthone (Standard)
    Menthone (Standard) is the analytical standard of Menthone. This product is intended for research and analytical applications. Menthone, an orally active monoterpene that can be isolated from plants and Mentha oil with antibacterial, antitumor, antioxidation, and antivirus properties. Menthone is a main volatile component of the essential oil, and has anti-Inflammatory properties in Schistosoma mansoni infection and rheumatoid arthritis.
    Menthone (Standard)
  • HY-W012732R
    Isoquinoline (Standard)
    Inhibitor
    Isoquinoline (Standard) is the analytical standard of Isoquinoline. This product is intended for research and analytical applications. Isoquinoline is an analog of pyridine. Isoquinoline structural-based alkaloids, such as tropoloisoquinoline, phthalideisoquinoline, and naphthylisoquinoline has anti-cancer activities.
    Isoquinoline (Standard)
  • HY-N9149
    Cryptanoside A
    Inducer
    Cryptanoside A, a cardiac glycoside epoxide, can be isolated from the stems of Cryptolepis dubia. Cryptanoside A has potent cytotoxicity against cancer cells. Cryptanoside A also inhibits Na+/K+-ATPase activity. Cryptanoside A increases the expression of Akt and the p65 subunit of NF-κB.
    Cryptanoside A
  • HY-14654B
    Aspirin DL-lysine
    Inhibitor
    Aspirin DL-lysine (ASA DL-lysine) is a lysine-containing aspirin derivative. Aspirin DL-lysine inhibits cyclooxygenase (COX) in platelets, blocks the synthesis of thromboxane A2 (TXA2), and thus inhibits platelet aggregation and activation. Aspirin DL-lysine can be used to study thrombin generation in patients with unstable angina pectoris.
    Aspirin DL-lysine
  • HY-B0130AR
    Perindopril (erbumine) (Standard)
    Perindopril (erbumine) (Standard) is the analytical standard of Perindopril (erbumine). This product is intended for research and analytical applications. 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) (Standard)
  • HY-162092
    Multi-target Pt
    Inhibitor
    Multi-target Pt (IV), an antitumor agent, suppresses the IKKβ phosphorylation, IκBα phosphorylation and NF-κB p65 phosphorylation and nuclear translocation, leading to blocked the NF-kB signal pathway.
    Multi-target Pt
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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