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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IMD-biphenylC
0 ImagesCat. No.: HY-139719CAS No.: 2928463-42-5
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NF-κB-IN-3
0 ImagesCat. No.: HY-144744CAS No.: 1873311-82-0NF-κB-IN-3 (Compound 2) is a NF-κB inhibitor with an IC50 of 0.70 µM. NF-κB-IN-3 can be used as an antitumor agent.
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MyD88 degrader-1
0 ImagesCat. No.: HY-184470MyD88 degrader-1 is an orally active molecular glue degrader targeting MyD88, with a DC50 of 0.74 μM, and exhibits potent anti-inflammatory activity. MyD88 degrader-1 promotes ubiquitination and proteasomal degradation of MyD88, blocks the activation of the NF-κB signaling pathway, and downregulates the transcription of pro-inflammatory genes such as IL-6 and IL-1β. MyD88 degrader-1 alleviates symptoms in acute lung injury models. MyD88 degrader-1 can be used in studies related to acute lung injury.
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Verproside
0 ImagesCat. No.: HY-126232CAS No.: 50932-20-2Verproside, a catalpol derivative iridoid glycoside isolated from the genus Pseudolysimachion, represses TNF-α -induced MUC5AC expression by inhibiting NF-κB activation via the IKK/IκB signaling cascade. Verproside has potent anti-inflammatory, antioxidant, antinociceptive and anti-asthmatic activities. Verproside has the potential for the study of chronic obstructive pulmonary disease (COPD).
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(+)-Naloxone
0 ImagesCat. No.: HY-17417ECAS No.: 65700-73-4(+)-Naloxone is a TLR4 inhibitor and the dextrorotatory enantiomer of the non-opioid Naloxone (HY-17417A) that lacks opioid receptor binding activity. (+)-Naloxone binds to MD2, preventing LPS from binding to TLR4, thereby inhibiting TLR4 signaling, downstream NFκB activation, and proinflammatory cytokine synthesis. (+)-Naloxone crosses the placenta. (+)-Naloxone is used in the research of preterm birth.
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Ginsenoside Rb3 (Standard)
0 ImagesCat. No.: HY-N0041RCAS No.: 68406-26-8Synonyms: Gypenoside IV (Standard)Ginsenoside Rb3 (Standard) is the analytical standard of Ginsenoside Rb3. This product is intended for research and analytical applications. Ginsenoside Rb3 is extracted from steamed Panax ginseng C. A. Meyer. Ginsenoside Rb3 exhibits inhibitory effect on TNFα-induced NF-κB transcriptional activity with an IC50 of 8.2 μM in 293T cell lines. Ginsenoside Rb3 also inhibits the induction of COX-2 and iNOS mRNA.
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G721-0282
0 ImagesG721-0282 is an orally active CHI3L1 inhibitor. G721-0282 can reduce the expression of inflammatory proteins and cytokines. G721-0282 inhibits the activation of the NF-κB signaling pathway. G721-0282 inhibits neuroinflammation and reduces anxious behavior. G721-0282 significantly inhibits the proliferation of osteosarcoma (OS) cells by suppressing the STAT3 signaling pathway. G721-0282 induces OS cell apoptosis by upregulating pro-apoptotic protein levels and downregulating anti-apoptotic protein levels. G721-0282 can be used for researches on neuroinflammatory conditions and cancer.
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IAV-IN-5
0 ImagesCat. No.: HY-183313CAS No.: 3038861-11-6IAV-IN-5 is an orally active inhibitor of influenza A virus (IAV). IAV-IN-5 inhibits viral replication, blocks virus-induced apoptosis, oxidative stress and cytokine storm, and regulates host immune signaling pathways. IAV-IN-5 reduces viral load and inflammatory cytokine levels in lung tissues of IAV-infected mouse models, alleviates body weight loss and pulmonary pathological damage. IAV-IN-5 can be used in studies related to influenza A virus infection.
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Esculeogenin A
0 ImagesCat. No.: HY-N18066CAS No.: 854381-37-6Esculeogenin A is the sapogenol of tomato saponin Esculeoside A (HY-N18067). Esculeogenin A is an orally active hepatoprotective, hypolipidemic, and antioxidant agent. Esculeogenin A regulates molecular targets like PPARα, SREBP1, Nrf2, NF-κB, ACAT1/ACAT2 to promote hepatic fatty acid oxidation, suppress de novo lipogenesis, enhance antioxidant defense, and inhibit inflammation. Esculeogenin A improves liver function, alleviates hyperlipidemia, and inhibits hepatic steatosis and foam cell formation, preventing nonalcoholic fatty liver disease in high-fat-diet-fed rats and reducing atherosclerotic lesions in apoE-deficient mice. Esculeogenin A can be used for the research of nonalcoholic fatty liver disease, atherosclerosis, and hyperlipidemia.
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Neuroprotective agent 18
0 ImagesCat. No.: HY-184935Neuroprotective agent 18 is a potent neuroprotective agent. Neuroprotective agent 18 inhibits the activity of NF-κB thereby significantly downregulating the expression of downstream pro-inflammatory mediators (TNF-α, IL-6) and inflammatory enzymes (COX-2) in the hippocampus. Neuroprotective agent 18 binds to AChE thereby partially inhibiting it and modulating cholinergic neurotransmission. Neuroprotective agent 18 can be used in research on Alzheimer's disease.
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Acutissimalignan B
0 ImagesCat. No.: HY-N17562CAS No.: 1005390-47-5Acutissimalignan B is a natural product. Acutissimalignan B can be isolated from Daphne kiusiana var. atrocaulis (Rehd.) F. Maekawa. Acutissimalignan B can reduce the mRNA expression of inflammatory cytokines (iNOS, TNF-α, IL-1β, and IL-6), inhibit the phosphorylation of IκBα, and inhibit the nuclear translocation of NK-κB p65. Acutissimalignan B shows anti-neuroinflammatory effects.
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SAP15
0 ImagesCat. No.: HY-P10462CAS No.: 1403753-45-6Synonyms: Synthetic anti-inflammatory peptide 15SAP15 (Synthetic anti-inflammatory peptide 15) is a synthetic anti-inflammatory peptide consisting of 15 amino acids designed from human beta-defensin 3. SAP15 has the ability to penetrate cells and is able to induce downregulation of intracellular inflammation. SAP15 inhibits inflammation by inhibiting the phosphorylation of HDAC5 and thereby reducing the phosphorylation of NF-κB p65. SAP15 inhibits HDAC5 and NF-κB p65 phosphorylation in LPS (HY-D1056)-induced macrophages. SAP15 increases the expression of aggrecan and type II collagen and decreases the expression of osteocalcin in LPS-induced chondrocytes. SAP15 can be used in the study of inflammation regulation and anti-inflammatory therapy of biomaterials.
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EC-70124
0 ImagesCat. No.: HY-124067CAS No.: 1185908-92-2EC-70124 is an orally active multikinase inhibitor targeting IKKβ and JAK2. EC-70124 blocks IkB phosphorylation and STAT3 (Tyr705) activation, suppressing NF-κB nuclear translocation and STAT3 transcriptional activity. EC-70124 reduces tumor growth and cancer stem cell (CSC) populations in prostate cancer cells and xenograft models. EC-70124 is promising for research of prostate cancer.
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PMX464
0 ImagesCat. No.: HY-108534CAS No.: 485842-97-5Synonyms: AW 464PMX464 (AW 464) is a thiol-reactive quinol compound and an inhibitor of the thioredoxin-thioredoxin reductase (Trx/TrxR) system, with an IC50 value of 6.5 μM against TrxR. PMX464 acts by irreversibly inhibiting the thioredoxin (Trx-1) system, blocking HIF-1α transcriptional activation and the NF-κB inflammatory pathway, inducing apoptosis, attenuating platelet function and inhibiting thrombosis, and specifically disrupting the trypanothione antioxidant metabolic network in parasites. PMX464 is used in research concerning malignant tumors (colorectal cancer, breast cancer, renal cancer, and leukemia), pulmonary inflammation, African sleeping sickness, and antithrombotic applications.
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SHP2-IN-45
0 ImagesCat. No.: HY-178983CAS No.: 2949435-53-2SHP2-IN-45 (Compound 6) is a potent, highly selective, and orally active SHP2 allosteric inhibitor. SHP2-IN-45 significantly reduces the expressions of IL-6, TNF-α, IL-1β, and iNOS. SHP2-IN-45 inhibits the polarization of M1-type macrophages. SHP2-IN-45 can inhibit the NF-κB pathway. SHP2-IN-45 can be used in the research of sepsis and acute lung injury.
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Ginsenoside Rd (Standard)
0 ImagesSynonyms: Gypenoside VIII (Standard)Ginsenoside Rd (Standard) is the analytical standard of Ginsenoside Rd. This product is intended for research and analytical applications. Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively.
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6-O-p-Hydroxybenzoylglutinoside
0 ImagesCat. No.: HY-N9731CAS No.: 202337-44-86-O-p-Hydroxybenzoylglutinoside acts as a selective NF-κB inhibitor that suppresses the transcriptional activity of TNF-α-activated NF-κB (IC50=52.78 μM). 6-O-p-Hydroxybenzoylglutinoside shows no significant inhibitory activity against sEH, AChE, or BChE. 6-O-p-Hydroxybenzoylglutinoside is a caged chlorinated iridoid glycoside identified from the seeds of Catalpa bungei (Manchurian catalpa).
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GNE-5472
0 ImagesCat. No.: HY-175445CAS No.: 2417369-99-2GNE-5472 is a potent bifunctional ERα PRRTAC degrader, with its E3 ligand being a pan-IAP antagonist. GNE-5472 antagonizes cIAP1/2, activating the non-classical NF-κB pathway, resulting in a significant upregulation of TNFα expression. GNE-5472 inhibits the proliferation of breast cancer cells and induces cell apoptosis. GNE-5472 can be used for the study of breast cancer.
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CKD-712
0 ImagesCat. No.: HY-114214CAS No.: 626252-75-3CKD-712 is an orally active multi-target tetrahydroisoquinoline derivatived and a potent inhibitor of the NF-κB pathway. CKD-712 selectively inhibits MMP-9 with no effect on MMP-2, downregulates the expression of TNF-α, IL-6, cyclin A, cyclin B, CDK-1 and other proteins, and activates the PI3K/Akt signaling pathway. CKD-712 blocks the activation and nuclear translocation of NF-κB, downregulates inflammatory factors and pro-tumor metastatic proteins, and induces G2/M phase arrest in tumor cells and thereby inhibits the invasion of cancer cells. CKD-712 can be used for the research of sepsis, myocardial ischemia-reperfusion injury and non-small cell lung cancer.
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(9S,13R)-12-Oxo phytodienoic acid-d5
0 ImagesCat. No.: HY-118828ASCAS No.: 2692624-08-9Synonyms: (9S,13R)-12-OPDA-d5(9S,13R)-12-Oxo phytodienoic acid-d5 ((9S,13R)-12-OPDA-d5) is the deuterated-labeled (9S,13R)-12-Oxo phytodienoic acid (HY-118828A). (9S,13R)-12-Oxo phytodienoic acid ((9S,13R)-12-OPDA) is a mPGES-1 inhibitor and Nrf2 activator. (9S,13R)-12-Oxo phytodienoic acid selectively inhibits mPGES-1 expression and reduces inducible PGE2 production without affecting COX-1 or COX-2. (9S,13R)-12-Oxo phytodienoic acid inhibits the phosphorylation of IKKβ, IκBα, and NF-κB (p65), blocks the nuclear translocation of p65, increases the nuclear translocation of Nrf2, and upregulates HO-1 expression. (9S,13R)-12-Oxo phytodienoic acid inhibits the differentiation of M0 macrophages toward the M1 phenotype and promotes differentiation toward the M2 phenotype. (9S,13R)-12-Oxo phytodienoic acid decreases the levels of NO, PGE2, IL-1β, IL-6, iNOS, and PGD2. (9S,13R)-12-Oxo phytodienoic acid can be used for inflammation research.
