Bay11-7082 / InvivoGen, Bayer - LARVOL DELTA

Acteoside-containing caffeic acid is bioactive functional group of antifibrotic effect by suppressing inflammation via inhibiting AHR nuclear translocation in chronic kidney disease. (PubMed, Acta Pharmacol Sin) - "However, ATS did not affect AHR expression in IAA-induced NRK-52E cells treated with BAY 11-7082. Therefore, ATS was identified as an AHR antagonist that ameliorated CKD by improving NF-κB/Nrf2 signalling axis. Conclusively, ATS holds promise as a chemical scaffold for the development of new antifibrotic agents."

Journal • Chronic Kidney Disease • Fibrosis • Glomerulonephritis • IgA Nephropathy • Immunology • Inflammation • Nephrology • Renal Disease • AHR • NFE2L2 • RELA

The role of ADAR1-mediated A-to-I RNA editing and non-editing functions in radioresistance of esophageal squamous cell carcinoma. (ASCO 2025) - "Inhibition of NF-κB with BAY 11-7082 reduced cell death following RT in ADAR1-knockdown KYSE410 cells, indicating a key role for NF-κB in pyroptosis triggered by ADAR1 loss... Our study underscores the potential of ADAR1 as a therapeutic target for overcoming radioresistance in ESCC through the modulation of pyroptosis, offering a new perspective for the development of targeted therapies."

Esophageal Cancer • Esophageal Squamous Cell Carcinoma • Melanoma • Oncology • Squamous Cell Carcinoma • ADAR • ANXA5 • BIRC3 • GSDME • IL18 • IL1B

Effect of fusobacterium nucleatum on NF-κB/HIF-1α/CCL20 pathway and M2 macrophages infiltration in esophageal squamous cell carcinoma. (ASCO 2025) - "Using BAY11-7082 could decline both CCL20 and HIF-1α level triggered by F. nucleatum. Fusobacterium nucleatum promotes esophageal squamous cell carcinoma progression via NF-κB/HIF-1α/CCL20 pathway-mediated migration of M2-like macrophages into the tumour micro-environment and deteriorates the suppression of the local immune micro-environment within the tumor. Such bacteria may be a biomarker to predict the efficacy of immunotherapy in ESCC."

IO biomarker • Esophageal Cancer • Esophageal Squamous Cell Carcinoma • Infectious Disease • Oncology • Squamous Cell Carcinoma • CCL20 • CCR6 • CD68 • HIF1A • MRC1

Expression and Purification of Human Stem Cell Factor and Its Effect on the Growth of A549 Cells. (PubMed, Protein J) - "Further, NF-κB pathway blockade was achieved through treatment with BAY11-7082, and it was observed to decrease the A549 cell activity promoted by the purified proteins. These findings provided insights into the biological role of SCF in the development of NSCLC."

Journal • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • KIT

NF-kappaB is involved exclusively under inflammatory conditions in the regulation of cathelicidin 3 expression in bovine mammary glands through phosphorylation of p65. (PubMed, J Anim Sci) - "Additionally, the effects of NF-κB inhibitor (BAY 11-7082, 10 μmol/L) or NF-κB activator (NF-κB activator-1, 1 μmol/L) on cultured dairy cow mammary epithelial cells were assessed...Additionally, decreased blood glucose concentration promotes CATHL3 mRNA expression. These findings provide novel insights into the molecular mechanisms of bovine mastitis and potential targets for therapeutic intervention."

Journal • NFKB1 • RELA

Impact of Nuclear Factor Kappa B Inhibition on Neutrophil Extracellular Trap Induced Pro-inflammatory Cytokine Production In Vitro (ATS 2025) - "The 16HBES1 cells, an immortalized human bronchial epithelial cell line, were exposed to NETs or media control for 18 hours +/- 2.5uM BAY 11-7082 (NF-κB inhibitor)... Preliminary data suggests that NETs may drive IL-8 production via another pathway, but inhibition of NF-κB resulted in a decrease in TNFα production in 16HBES1 cells exposed to NETs. NF-κB could be a potential target for therapies aiming to control immune dysregulation in CF patients that leads to respiratory failure. Future studies will explore the mechanism by which NF-κB drives inflammation in 16HBES1 cells and in other cell lines."

Preclinical • Cystic Fibrosis • Genetic Disorders • Immunology • Oncology • Pulmonary Disease • Respiratory Diseases • CXCL8 • TNFA

Aryl hydrocarbon receptor deficiency upregulates intercellular adhesion molecule 1 in retinal pigment epithelial cells and contributes to retinal inflammation. (PubMed, Lab Invest) - "Introducing an AHR-green fluorescent protein into AHR-KO RPE cells or pre-treating the cells with pharmacological inhibitors targeting αvβ3 (cycloRGDfk), focal adhesion kinase (PF573228), phospholipase C (U73122), ERK1/2 (U0126), and NF-κB (Bay11-7082) prevented ICAM1 induction in AHR-KO RPE cells. These mice also displayed early-onset electroretinogram degeneration. Collectively, our data support the protective role of AHR in maintaining RPE cell physiology and retinal health."

Journal • Inflammation • Ocular Inflammation • Ophthalmology • AHR • ICAM1

Transcranial direct current stimulation alleviates chronic pain in knee osteoarthritis by modulating microglial and astrocytic polarization and neuroinflammation. (PubMed, Life Sci) - "These findings suggest that tDCS may alleviate KOA chronic pain through modulation of glial activation states and suppression of central neuroinflammation, highlighting its potential as a non-invasive therapeutic approach."

Journal • Immunology • Inflammation • Musculoskeletal Pain • Osteoarthritis • Pain • Rheumatology • IL18 • NLRP3 • TNFA

MTDH∆7-mediated mTOR activation drives doxorubicin resistance in triple-negative breast cancer: Relevance of mTORC1 inhibition on chemosensitization. (PubMed, Cell Signal) - "Inhibition of either mTORC1 by everolimus or NF-κB by BAY-11-7082 or CREB by H89 reversed these effects and mitigated MTDH∆7-mediated Dox efflux. In agreement, intriguingly, a positive correlation was observed between elevated MTDH∆7, mTORC1 activation, and ABC transporters level in human breast cancer patient cohort tumor samples. Collectively, MTDH∆7, by promoting mTOR signaling causes breast cancer chemoresistance, and that targeting MTDH∆7-mTOR signaling axis effectively enhances chemosensitization."

Journal • Breast Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer • ABCB1 • ABCC1 • ABCG2 • AMPK • MTDH

Quantitative Proteomic Analysis of Cardiac Xenograft Failure in a Pig-to-Non-Human Primate Model Identifies NF-κB as a Critical Immunomodulatory Target. (PubMed, Xenotransplantation) - "In summary, the proteomic analysis could help us to solve the mystery of cardiac xenograft failure, confirm the key pathways, and reveal a clear vision of future interventions. NF-κB inhibition effectively decreased immune cell infiltration and antibody deposition in myocardial tissue, suggesting its potential as a therapeutic strategy to enhance graft survival and reduce inflammation in cardiac xenotransplantation (CXTx)."

Journal • Preclinical • Cardiovascular • Hematological Disorders • Inflammation • Thrombosis • Transplantation • CDC37 • HSP90AB1 • MVP • PTX3

Selenoprotein S ablation-mediated pyroptosis contributes to liver damage resulting from selenium deficiency in chickens. (PubMed, Poult Sci) - "Following transfection, the introduction of N-acetylcysteine, BAY11-7082, or MCC950 alleviated the pyroptosis induced by SELS knockdown. However, MCC950 did not affect the NF-κB pathway, and both BAY 11-7082 and MCC950 were ineffective in reducing ROS accumulation. In conclusion, SELS deficiency leads to ROS generation and activation of the NF-κB pathway activation, ultimately inducing pyroptosis and the release of inflammatory factors."

Journal • GPX1 • NLRP3

SDC4 identified as an oncogenic target gene of NF-κB in TNFα-Induced tumor cells. (PubMed, Sci Rep) - "Immunofluorescence assay or qRT-PCR showed that the NF-κB inhibitor Bay11-7082 blocked TNFα-induced nuclear translocation of NF-κB, while both qRT-PCR and Western blot analyses showed Bay11-7082 could inhibit TNFα-induced upregulation of SDC4 at both mRNA and protein levels. Furthermore, SDC4 expression was positively correlated with NF-κB subunit RelA expression across 22 tumor types. In conclusion, this study identifies SDC4 as an oncogenic target gene of NF-κB, providing new insights for the development of anti-tumor therapies targeting the NF-κB pathway."

Journal • Oncology • NFKB1 • SDC4 • TNFA

Sialyllactose Attenuates Inflammation and Injury of Intestinal Epithelial Cells upon Enterotoxigenic Escherichia coli Infection. (PubMed, Int J Mol Sci) - "Notably, SL exhibited functional parallels to the NF-κB inhibitor BAY11-7082, jointly enhancing tight junction integrity via ZO-1 protein stabilization and inhibiting pro-inflammatory signaling through coordinated suppression of IκB-α/NF-κB phosphorylation cascades. The dual-action mechanism combines molecular interception of microbial attachment with intracellular modulation of the TLR4/MyD88/NF-κB pathway, effectively resolving both pathogenic colonization and inflammatory amplification. These findings position SL as a potential therapeutic application nutraceutical for livestock, with the capacity to address post-weaning porcine enteritis through functional feed formulations that synergistically enhance intestinal barrier resilience while curbing ETEC-mediated inflammatory pathogenesis."

Journal • Gastrointestinal Disorder • Infectious Disease • Inflammation • IL1B • IL6 • MYD88 • TJP1 • TLR4 • TNFA

FKBP51 protects hair cells of utricles from gentamicin-induced toxicity in vitro: possible relation to the activities of NF-κB signaling pathway. (PubMed, Food Chem Toxicol) - "In addition, mechanistic studies with 10 mM BAY 11-7082 showed that FKBP51 protected HCs against gentamicin-induced damage, at least in part, via blocking the NF-κB pathway activation. Taken together, our new findings suggest that FKBP51 might serve as a new target for the prevention of HCs of utricle from aminoglycoside-induced vestibular toxicity."

Journal • Preclinical • FKBP5

Interleukin-8 expression inversely predicts the therapeutic effectiveness of doxorubicin and paclitaxel on triple-negative breast cancer (AACR 2025) - "These findings demonstrated that IL-8 expression could be a useful indicator to predict the responsiveness of TNBC patients who are deciding to receive doxorubicin or paclitaxel therapy."

Breast Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer • CXCL8

In vitro and in vivo evidence on the association of pregnant PM2.5 exposure with preterm birth and potential role of placental miRNA-21 regulating TLR4/NF-κB and activating NLRP3 inflammasome. (PubMed, J Hazard Mater) - "BAY11-7082 and miRNA-21 mimic inhibited the PM2.5-activated TLR4/NF-κB signaling pathway and NLRP3 inflammasome. This study provides evidence on the potential molecular mechanism of miRNA-21-5p/TLR4/NF-κB signaling pathway in PM2.5-induced inflammatory response leading to PTB through NLRP3 inflammasome."

Journal • Preclinical • Inflammation • MIR21 • NLRP3 • TLR4

Cadmium induces the secretion of SASP factors regulated by MAPK and NF-κB signaling pathways in HEK293 cells: a possible mechanism of acute kidney damage induced by cadmium. (PubMed, Toxicology) - "However, NF-κB inhibitor BAY11-7082 and antioxidant NAC could inhibit these effects by suppressing NF-κB and MAPK signaling pathways. The present study revealed the specific mechanisms of Cd toxicity in HEK293 cells and provided useful information for elucidating the nephrotoxicity of Cd."

Journal • Inflammation • Nephrology

Uric acid reduces the expression of aquaporins in renal collecting ducts to increase urine output in hyperuricemia. (PubMed, Front Physiol) - "Blockade of NF-κB by its inhibitor Bay 11-7082 dramatically attenuated UA-suppressed expression of AQP2, AQP3 and AQP4. Furthermore, the luciferase reporter, CHIP and EMSA assays showed that NF-κB can directly bind to the promoter regions of AQP2, AQP3 and AQP4 genes to suppress their transcription. Our findings demonstrate that UA reduces the expression of AQP2, AQP3 and AQP4 in an NFκB-dependent manner, which contributes to the polyuria phenotype in the subjects with HUA."

Journal • Atherosclerosis • Cardiovascular • Chronic Kidney Disease • Coronary Artery Disease • Diabetes • Dyslipidemia • Genetic Disorders • Gout • Heart Failure • Hypertension • Hypertriglyceridemia • Inflammatory Arthritis • Metabolic Disorders • Nephrology • Obesity • Renal Disease • Rheumatology • Type 2 Diabetes Mellitus • AQP3

Norepinephrine promotes oxidative stress in vascular adventitial fibroblasts via PKC/NFκB-mediated NOX2 upregulation. (PubMed, Redox Rep) - "NE increased NADPH oxidase (NOX) 2 expression and superoxide level, which were almost abolished by NOX2 inhibitor GSK2795039 or α-adrenoceptor antagonist prazosin, but not significantly affected by NOX1 inhibitor ML171, NOX4 inhibitor GLX351322 or β-adrenoceptor antagonist propranolol. Either PKC inhibitor Go6983 or NFκB inhibitor BAY11-7082 attenuated NE-induced NOX activation, NOX2 upregulation, superoxide production, proliferation and migration. NE promotes oxidative stress by α-receptor/PKC/NFκB-mediated NOX2 upregulation, which contributes to proliferation and migration of VAFs."

Journal • Cardiovascular • Hypertension • NFKB1 • NOX4

Deficiency of IL-7R attenuates abdominal aortic aneurysms in mice by inhibiting macrophage polarization towards M1 phenotype through the NF-κB pathway. (PubMed, Mol Med) - "In short, this study showed that IL-7R promotes the infiltration and migration of macrophages by regulating M1 macrophage polarization, possibly in part via activation of the NF-κB pathway, which may be associated with the development of AAAs."

Journal • Preclinical • Cardiovascular • Inflammation • ELANE • IL7

Structural characterization, derivatization, and bioactivities of secondary metabolites produced by termite-associated Streptomyces lannensis BYF-106. (PubMed, Microbiol Spectr) - "Furthermore, urdamycin Y (1) exhibited potent inhibition on NO production, with an IC50 value of 4.8 µM, which was comparable to that of Bay11-7082 with an IC50 value of 2.1 µM...Urdamycin Y (1) exhibited a strong inhibitory effect on NO production, and most of the tested metabolites showed significant cytotoxic activity. These findings indicate that the metabolites of BYF-106 may offer promising avenues for the exploration and development of new bioactive drugs."

Journal

Lactic acid bacteria target NF-κB signaling to alleviate gastric inflammation. (PubMed, Food Funct) - "Treatment with the NF-κB inhibitor BAY 11-7082 further decreased tumor necrosis factor-α (TNF-α), interleukin-8 (IL-8), and interleukin-1β (IL-1β) levels, confirming the inhibitory effect of L. plantarum ZJ316 on the NF-κB pathway...In summary, administration of L. plantarum ZJ316 demonstrated robust anti-inflammatory effects against H. pylori infection by suppressing NF-κB signaling and promoting favorable changes in the gastric microbiota composition. Therefore, L. plantarum ZJ316 holds promise as a novel functional food for protecting the body against H. pylori infection."

Journal • Gastric Cancer • Infectious Disease • Inflammation • Oncology • Solid Tumor • CXCL8 • IL10 • IL1B • NFKBIA • PGC • TNFA

TAB2 Promotes Immune Escape and Chemoresistance Through NF-κB Pathway Activation in Cervical Cancer. (PubMed, J Cell Mol Med) - "We investigated the role of TAB2 in CC using cisplatin-resistant and parental cell lines...NF-κB pathway involvement was examined using the BAY 11-7082 inhibitor...Our findings reveal TAB2 as a critical regulator of both chemoresistance and immune escape in CC through NF-κB pathway activation. This suggests TAB2 as a potential therapeutic target for overcoming treatment resistance in CC."

IO biomarker • Journal • Cervical Cancer • Oncology • Solid Tumor • PD-L1

IRE1α/TRAF2/NF-κB pathway promotes apoptosis via regulating inflammatory cytokines and aggravates brain injury after SAH. (PubMed, J Stroke Cerebrovasc Dis) - "The IRE1α/TRAF2/NF-κB signal pathway was activated and promoted apoptosis by promoting the expression of inflammatory cytokines after SAH."

Journal • CNS Disorders • Hematological Disorders • Subarachnoid Hemorrhage • Vascular Neurology • CASP3 • HSPA5 • IL1B • IL6 • TNFA

Inhibition of AGTR1 attenuates cell proliferation after glaucoma filtration surgery via NF-κB pathway-mediated G0/G1-phase cell cycle arrest. (PubMed, Exp Cell Res) - "Furthermore, the addition of BAY 11-7082, a blocker of the NF-κB pathway, resulted in further inhibition of Ki67, Cyclin D, and Cyclin E expressions and an increase in the percentage of HTFs in the G0/G1 phase. In conclusion, our findings indicate that AGTR1 inhibition can attenuate HTF proliferation by leading to cell cycle arrest in the G0/G1 phase through the NF-κB pathway. Targeting AGTR1 is a feasible strategy for mitigating cell proliferation following GFS."

Journal • Glaucoma • Ophthalmology • CDKN1A • TGFB1