NF-κB
NF-κB regulates innate and adaptive immunity, inflammatory responses, immune-cell survival, activation, and differentiation[1]. Mechanistically, canonical NF-κB signaling depends on phosphorylation-induced proteasomal degradation of IκB proteins, releasing cytosolic NF-κB dimers for transcriptional control[2]. In inflammation models, NF-κB induces cytokines, chemokines, adhesion molecules, and inflammasome-related responses, linking pathway activation to chronic inflammatory disease and cancer research[1][3][4]. Compared with related isoforms, mammalian NF-κB includes RelA/p65, RelB, c-Rel, p50/NF-κB1, and p52/NF-κB2, and RelA loss causes embryonic lethality with liver apoptosis, whereas p50 loss produces immune-response defects without developmental abnormalities[2][5][6]. For experimental applications, NF-κB inhibitors, including IKK-targeting agents and BAY 11-7082, help test pathway dependence in inflammatory signaling, but broad pathway targeting requires careful interpretation because NF-κB also supports normal immune physiology[4][7].
References:
- [1]. Liu T, et al. NF-κB signaling in inflammation. Signal Transduct Target Ther. 2017;2:17023–. [Content Brief]
- [2]. Oeckinghaus A, et al. The NF-kappaB family of transcription factors and its regulation. Cold Spring Harb Perspect Biol. 2009 Oct;1(4):a000034. [Content Brief]
- [3]. Lawrence T. The nuclear factor NF-kappaB pathway in inflammation. Cold Spring Harb Perspect Biol. 2009 Dec;1(6):a001651. doi: 10.1101/cshperspect.a001651. Epub 2009 Oct 7. PMID: 20457564; PMCID: PMC2882124. et al. The nuclear factor NF-kappaB pathway in inflammation. Cold Spring Harb Perspect Biol. 2009 Dec;1(6):a001651. [Content Brief]
- [4]. Yu H, et al. Targeting NF-κB pathway for the therapy of diseases: mechanism and clinical study. Signal Transduct Target Ther. 2020 Sep 21;5(1):209. [Content Brief]
- [5]. Beg AA, et al. Embryonic lethality and liver degeneration in mice lacking the RelA component of NF-kappa B. Nature. 1995 Jul 13;376(6536):167-70. [Content Brief]
- [6]. Sha WC, et al. Targeted disruption of the p50 subunit of NF-kappa B leads to multifocal defects in immune responses. Cell. 1995 Jan 27;80(2):321-30. [Content Brief]
- [7]. Lee J, et al. BAY 11-7082 is a broad-spectrum inhibitor with anti-inflammatory activity against multiple targets. Mediators Inflamm. 2012;2012:416036. [Content Brief]
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NF-κB Inhibitors
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NF-κB Activators
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NF-κB Modulators
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NF-κB Ligand
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NF-κB Related Products (1455)
Related Products (1455)
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Antibodies (24)
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Tofacitinib-13C,d3
0 ImagesCat. No.: HY-40354S2Synonyms: Tasocitinib-13C,d3; CP-690550-13C,d3Tofacitinib-13C,d3 (Tasocitinib-13C,d3; CP-690550-13C,d3) is the deuterated, 13C-labeled Tofacitinib (HY-40354). Tofacitinib (Tasocitinib) is an orally active, blood-brain barrier permeable selective inhibitor of JAK1/JAK3. Tofacitinib blocks the JAK-STAT/NF-κB signaling pathway, inhibits cytokine signal transduction, phosphorylation of STAT1/STAT5, and suppresses innate and adaptive immune responses. Tofacitinib can be used in research related to major depressive disorder, rheumatoid arthritis, pulmonary diseases, systemic lupus erythematosus, and immune-mediated liver injury.
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Ephemeranthol A
0 ImagesCat. No.: HY-N17888CAS No.: 135545-86-7Ephemeranthol A is a phenanthrene compound with anticancer and anti-inflammatory activities. Ephemeranthol A exerts significant anti-inflammatory effects in macrophages by inhibiting the NF-κB and MAPK signaling pathways. Ephemeranthol A induces apoptosis and inhibits metastasis of lung cancer cells by suppressing the FAK/Akt signaling and EMT processes. Ephemeranthol A can be used for the research of acute and chronic inflammatory diseases and non-small cell lung cancer.
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Eudebeiolide B
0 ImagesCat. No.: HY-N11775CAS No.: 1934299-51-0Synonyms: Plebeiolide D
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DNH28
0 ImagesCat. No.: HY-175037DNH28 is a potent NF-κB and MAPK inhibitor with an IC50 of 0.93 μM against HepG2 cells. DNH28 promotes apoptosis by down-regulating the expression of Bcl-2, up-regulating the expression of BAX and Cleaved-caspase-3. DNH28 blocks the cell cycle and inhibits migration. DNH28 can be used for the study of hepatocellular carcinoma (HCC).
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STAT3/NF-κB-IN-3
0 ImagesCat. No.: HY-184736STAT3/NF-κB-IN-3 is an orally active STAT3/NF-κB inhibitor with anti-inflammatory and antioxidant activities, which specifically blocks the phosphorylation of NF-κB and STAT3 proteins. STAT3/NF-κB-IN-3 downregulates the expression of iNOS and NOX-2 in macrophages, reduces intracellular levels of ROS and MDA, and upregulates the expression of antioxidant genes at the same time. In a mouse model of acute liver failure induced by LPS/D-GalN, STAT3/NF-κB-IN-3 alleviates liver necrosis and inflammatory cell infiltration, and reduces the release of pro-inflammatory cytokines such as IL-6 and IL-12 via the TLR4 pathway. STAT3/NF-κB-IN-3 can be used in studies related to acute liver failure.
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Ginsenoside Re (Standard)
0 ImagesSynonyms: Ginsenoside B2(Standard); Panaxoside Re(Standard); Sanchinoside Re (Standard)Ginsenoside Re (Standard) is the analytical standard of Ginsenoside Re. This product is intended for research and analytical applications. Ginsenoside Re (Ginsenoside B2) is an extract from Panax notoginseng. Ginsenoside Re decreases the β-amyloid protein (Aβ). Ginsenoside Re plays a role in antiinflammation through inhibition of JNK and NF-κB.
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Oxaprozin potassium
0 ImagesCat. No.: HY-B0808ACAS No.: 174064-08-5Synonyms: Oxaprozinum potassium; Wy21743 potassiumOxaprozin potassium is an orally active and potent COX inhibitor, with IC50 values of 2.2 μM for human platelet COX-1 and and 36 μM for IL-1-stimulated human synovial cell COX-2, respectively. Oxaprozin potassium also inhibits the activation of NF-κB. Oxaprozin potassium induces cell apoptosis. Oxaprozin potassium shows anti-inflammatory activity. Oxaprozin potassium-mediated inhibition of the Akt/IKK/NF-κB pathway contributes to its anti-inflammatory properties.
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IMD-catechol
0 ImagesCat. No.: HY-139716CAS No.: 2928463-39-0
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Sootepin D
0 ImagesCat. No.: HY-122521CAS No.: 1154518-97-4Sootepin 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.
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BAY-356
0 ImagesCat. No.: HY-P992321BAY-356, a potent TWEAK receptor agonist, is an aglycosylated anti-TWEAK receptor antibody. BAY-356 triggers TWEAKR hyperactivation, activates NFκB and STAT1 pathways, and undergoes TWEAKR-dependent internalization. BAY-356 can be used for the research of colorectal cancer, bladder cancer, non-small cell lung cancer and pancreatic cancer[1][2].
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APH003
0 ImagesCat. No.: HY-184915CAS No.: 3065495-08-8APH003 is an orally active IRAK4 PROTAC degrader with a DC50 of 0.74 nM in human peripheral blood mononuclear cells (hPBMCs). APH003 recruits IRAK4 to CRBN to form a ternary complex, mediates the ubiquitination and degradation of IRAK4 via the ubiquitin-proteasome pathway, and inhibits the kinase activity of IRAK4. APH003 inhibits LPS- or IL-1β/LPS-induced phosphorylation of ERK, JNK and NF-κB. APH003 inhibits the secretion of TNF-α, IL-6, IL-8 and IL-13 by stimulated hPBMCs. APH003 exhibits anti-inflammatory activity in rat TNBS-induced intestinal inflammation models and mouse IL-33-induced skin inflammation models. APH003 can be used in research related to inflammatory bowel disease and skin inflammation.
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G721-0377
0 ImagesCat. No.: HY-183586CAS No.: 946336-44-3G721-0377 is a CHI3L1 modulator with a human Kd value of 45 μM. G721-0377 binds to CHI3L1 and modulates downstream signaling pathways. G721-0377 suppresses CHI3L1-induced NF-κB activation, decreases secretion of CHI3L1 and IL-6. G721-0377 can be used for the research of Alzheimer's disease.
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NF-κB-IN-14
0 ImagesCat. No.: HY-162004CAS No.: 3019972-01-8NF-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.
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TAT-N24
0 ImagesCat. No.: HY-P10797Purity: 99.83%TAT-N24 is a cell-penetrating peptide and also an inhibitor of p55PIK. TAT-N24 disrupts the interactions between p55PIK and p53, PCNA or Rb, blocks the p53-dependent ubiquitin-mediated degradation process, and inhibits the nuclear translocation and phosphorylation of NF-κB p65. TAT-N24 enhances MMS-induced p53-dependent cell apoptosis, inhibits DNA synthesis, reduces the expression of Cyclin D1, and induces cell cycle arrest at the G0/G1 or S phase. TAT-N24 inhibits the activation of NLRP3 and NLRC4 inflammasomes, reduces the expression of ZBP1-PANoptosome components, and suppresses PANoptosis. TAT-N24 can be used in research related to leukemia, colon cancer, cervical cancer, liver cancer, corneal neovascularization, restenosis and acute glaucoma.
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TP-110
0 ImagesCat. No.: HY-118522CAS No.: 688737-95-3TP-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.
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STAT3/NF-κB-IN-1
0 ImagesCat. No.: HY-175227STAT3/NF-κB-IN-1 is a potentSTAT3 and NF-κB inhibitor with IC50s of 5.86 (STAT3) and 4.22 μM (NF-κB) in 4T1 cells. STAT3/NF-κB-IN-1 is able to induce apoptosis via its upregulation on key apoptotic regulators; caspases-3/9, Bax and downregulation of Bcl-2. STAT3/NF-κB-IN-1 exerts considerable anticancer activity against breast cancer cell lines and reduces tumor volume in vivo. STAT3/NF-κB-IN-1 can be used for the study of breast cancer.
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Anti-neuroinflammation agent-4
0 ImagesCat. No.: HY-189271CAS No.: 3113312-38-9Anti-neuroinflammation agent-4 is a blood-brain barrier-penetrating inhibitor of IκBα, NLRP3, and NF-κB p65. Anti-neuroinflammation agent-4 exerts anti-neuroinflammatory effects by inhibiting IκBα phosphorylation, reducing NLRP3 and caspase-1 expression, and suppressing p65 phosphorylation and its nuclear translocation, thereby decreasing the release of inflammatory mediators such as ROS, NO, IL-1β, IL-6, TNF-α, and IL-18 in microglia. Anti-neuroinflammation agent-4 can be used for research on neuroinflammation.
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Meliatoosenin O
0 ImagesCat. No.: HY-N21586CAS No.: 1239945-87-9Meliatoosenin O is a limonoid found in the fruits of Melia toosendan. Meliatoosenin O inhibits TNF-α-induced NF-κB luciferase activation in HepG2-NF-κB-Luc cells.
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Leupeptin Ac-LL
0 ImagesCat. No.: HY-18234BCAS No.: 24365-47-7Leupeptin Ac-LL is a broad-spectrum protease inhibitor. By inhibiting the activation of the PTEN/PI3K/Akt/NF-κB/ERK1/2/p38 signaling pathway, Leupeptin Ac-LL significantly reduces LPS-induced NO and ROS production, mitochondrial membrane potential hyperpolarization, phagocytic activity, pro-inflammatory cytokine release, and M1 polarization in mouse peritoneal macrophages, and reverses autophagic flux impairment. It also decreases Concanavalin A (HY-P2149)-induced proliferation index of mouse splenic lymphocytes and the Th1/IL-10 and Th2/IL-10 cytokine ratios, thereby modulating innate and adaptive immune responses. Leupeptin Ac-LL inhibits blood coagulation and tumorigenesis in mouse skin. Leupeptin Ac-LL can be used in research on chronic inflammatory diseases and skin tumorigenesis.
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XRF-1021
0 ImagesCat. No.: HY-179378CAS No.: 2968523-32-0XRF-1021 is an orally active HIPK2 inhibitor (IC50 = 0.18 μM). XRF-1021 reduces the expression of fibrotic markers in TGF-β1 stimulated NRK-49F and HK-2 cells, including Fibronectin, Collagen I and α-SMA. XRF-1021 blocks TGF-β, NF-κB, p53, Wnt/β-catenin, and Notch signaling. XRF-1021 reduces renal injury and fibrosis in vivo. XRF-1021 can be used for the research of chronic kidney disease.
