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 Inducers
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NF-κB Ligand
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NF-κB Related Products (1438)
Related Products (1438)
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Antibodies (24)
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Phorbol 12-myristate 13-acetate
0 ImagesSynonyms: PMA; TPA; Phorbol myristate acetatePhorbol 12-myristate 13-acetate (PMA; TPA; Phorbol myristate acetate), a phorbol ester, is a dual SphK and protein kinase C (PKC) activator. Phorbol 12-myristate 13-acetate is a NF-κB activator. Phorbol 12-myristate 13-acetate induces differentiation in THP-1 cells (Validated by MedChemExpress).
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Bortezomib
0 ImagesSynonyms: PS-341; LDP-341; NSC 681239Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Bortezomib can be used for the study of multiple myeloma (MM). Bortezomib effectively inhibits TREM2 expression in tumor-associated macrophages (TAMs).
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BAY 11-7082
0 ImagesSynonyms: BAY 11-7821BAY 11-7082 is an IκBα phosphorylation and NF-κB inhibitor. BAY 11-7082 selectively and irreversibly inhibits the TNF-α-induced phosphorylation of IκB-α, and decreases NF-κB and expression of adhesion molecules. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 (IC50=0.19, 0.96 μM, respectively). BAY 11-7082 inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells.
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Tofacitinib
0 ImagesSynonyms: Tasocitinib; CP-690550Tofacitinib (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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JSH-23
0 ImagesJSH-23 is an NF-κB inhibitor which inhibits NF-κB transcriptional activity with an IC50 of 7.1 μM in lipopolysaccharide (LPS)-stimulated macrophages RAW 264.7. JSH-23 inhibits nuclear translocation of NF-κB p65 without affecting IκBα degradation.
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TAK-243
0 ImagesSynonyms: MLN7243TAK-243 (MLN7243) is a first-in-class, selective ubiquitin activating enzyme, UAE (UBA1) inhibitor (IC50=1 nM), which blocks ubiquitin conjugation, disrupting monoubiquitin signaling as well as global protein ubiquitination. TAK-243 (MLN7243) induces endoplasmic reticulum (ER) stress, abrogates NF-κB pathway activation and promotes apoptosis.
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Leupeptin hemisulfate
0 ImagesLeupeptin hemisulfate is a broad-spectrum protease inhibitor. By inhibiting the activation of the PTEN/PI3K/Akt/NF-κB/ERK1/2/p38 signaling pathway, Leupeptin hemisulfate 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 hemisulfate inhibits blood coagulation and tumorigenesis in mouse skin. Leupeptin hemisulfate can be used in research on chronic inflammatory diseases and skin tumorigenesis.
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Shikonin
0 ImagesShikonin is a major component of a Chinese herbal medicine named zicao. Shikonin is a potent TMEM16A chloride channel inhibitor with an IC50 of 6.5 μM. Shikonin is a specific pyruvate kinase M2 (PKM2) inhibitor and can also inhibit TNF-α and NF-κB pathway. Shikonin decreases exosome secretion through the inhibition of glycolysis. Shikonin inhibits AIM2 inflammasome activation.
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Hyaluronidase, Bovine testes
0 ImagesCat. No.: HY-107910CAS No.: 37326-33-3Synonyms: Hyaluronate 4-glycanohydrolase, Bovine testes; Hyaluronoglucosaminidase, Bovine testesHyaluronidase, Bovine testes (Hyaluronate 4-glycanohydrolase; Hyaluronoglucosaminidase) is an endoglycosidase that depolymerizes Hyaluronic acid (HA) (HY-B0633A) by cleavage of glycosidic bonds. Hyaluronidase degrades HA and activates membrane receptors that trigger pathways converging in NF-κB activation. Hyaluronidase is employed in the research of granulomatous foreign body reactions, soft-tissue necrosis caused by vascular compromise and uncomplicated nodules, overcorrection, inflamed nodules or tissue ischemia associated with HA filler injection.
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L-Glutamine-13C5
0 ImagesSynonyms: L-Glutamic acid 5-amide-13C5L-Glutamine-13C5 is the 13C-labeled L-Glutamine (HY-N0390). L-Glutamine is an orally active nutritional agent and cellular metabolism regulator. L-Glutamine is taken up in a Na+-dependent manner and targets multiple key molecules including glutaminase, mTORC1, NF-κB, STAT-3 and HIF-1α. L-Glutamine enhances glutaminolytic catabolism, drives the conversion of glutamate to α-ketoglutarate, thereby regulating gene expression, integrating metabolic signals, mediating glutamine flux and maintaining redox homeostasis. L-Glutamine also promotes cell proliferation, osteogenic differentiation and fracture healing, exerts neuroprotective and cardioprotective effects, and inhibits osteoarthritis. L-Glutamine can be applied to research related to osteoporosis, osteoarthritis, ischemic stroke and acute cantharidin-induced cardiotoxicity.
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Phytohemagglutinin
0 ImagesPhytohemagglutinin (PHA-M), the major seed lectin of the common bean, Phaseolus vulgaris, is a T-cell activator. Phytohemagglutinin stimulates human mononuclear leukocytes, inducing the expression of ChAT mRNA and potentiating ACh synthesis. Phytohemagglutinin induces dose- and time-dependent toxicity in THP-1 monocytes/macrophages, alters cellular morphology, causes organelle dysfunction, and increases the expression of NF-κB, COX2, IL-1β.
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Parthenolide
0 ImagesSynonyms: (-)-Parthenolide
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Sesame Oil
0 ImagesSesame Oil is a vegetable oil. Sesame Oil can be extracted from the seeds of Sesamum indicum L. Sesame Oil decreases NF-κB, aspartate aminotransferase, alanine aminotransferase, IL-1β, IL-4 and nitric oxide. Sesame Oil has antitumor activity against malignant melanoma. Sesame Oil has protective effects against liver damage caused by various agents such as Cisplatin (HY-17394) and Acetaminophen (HY-66005). Sesame Oil shows antinociceptive and anti-inflammatory activities.
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Tofacitinib citrate
0 ImagesSynonyms: Tasocitinib citrate; CP-690550 citrateTofacitinib citrate (Tasocitinib citrate) is an orally active, blood-brain barrier permeable selective inhibitor of JAK1/JAK3. Tofacitinib citrate blocks the JAK-STAT/NF-κB signaling pathway, inhibits cytokine signal transduction, phosphorylation of STAT1/STAT5, and suppresses innate and adaptive immune responses. Tofacitinib citrate 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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Hesperetin
0 ImagesHesperetin is a natural flavanone that can be found in citrus, and acts as a potent and orally active broad-spectrum inhibitor against human UGT activity. Hesperetin induces apoptosis via p38 MAPK activation. Hesperetin displays a range of bioactivities including antioxidant, anti-inflammatory, and anti-cancer. Hesperetin is found to induce cell-cycle arrest at G2/M phase. Hesperetin can reduce Bcl-2 and enhance BaxM. Hesperetin induces apoptosis through inhibiting NF-κB receptor.
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Withaferin A
0 ImagesWithaferin A is a steroidal lactone isolated from Withania somnifera, inhibits NF-kB activation and targets vimentin, with potent antiinflammatory and anticancer activities. Withaferin A is an inhibitor of endothelial protein C receptor (EPCR) shedding.
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Betulinic acid
0 ImagesBetulinic acid is a natural pentacyclic triterpenoid, acts as a eukaryotic topoisomerase I inhibitor, with an IC50 of 5 μM, and possesses anti-HIV, anti-malarial, anti-inflammatory and anti-tumor properties. Betulinic acid can cross the blood-brain barrier.
