Catalog No.
Product Name
Application
Product Information
Citations
-
NF-κB inhibitor
QNZ inhibits the activation of the transcription factor NF-κB and has been used to investigate NF-κB signaling.- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
-
NF-kB inhibitor
Withaferin A is a steroidal lactone present in W. somnifera that at 2-25 μM has been shown to bind to and induce aggregation of vimentin intermediate filaments in cultured endothelial cells and fibroblasts, causing apoptosis.- Chang-Mu Chen, .et al. , Phytomedicine, 2020, Dec;79:153352 PMID: 33007732
-
NF-κB inhibitor
JSH 23 is an inhibitor of NF-kB, blocking its translocation into the nucleus (IC50 = 7.1 uM)- Yu N, .et al. , Radiat Res, 2018, Apr;189(4):409-417 PMID: 29420126
-
NF-κB inhibitor
SC75741 is a potent NF-kB inhibitor with EC50 of 200 nM.- Yunshang Yang, .et al. , Biomed Pharmacother, 2023, Feb;158:114113 PMID: 36516692
- Yajun Li, .et al. , Cell Prolif, 2022, Oct;55(10) PMID: 35708050
- Crystal A Mendoza, .et al. , Antiviral Res, 2021, Jan;185:104993 PMID: 33296695
-
Apoptosis Inducer
Andrographolide is an interesting pharmacophore with anticancer and immunomodulatory activities and hence has the potential for being developed as a cancer therapeutic agent. - Parthenolide ((-)-Parthenolide) is a sesquiterpene lactone which occurs naturally in the plant feverfew (Tanacetum parthenium).
- Sulfasalazine is a drug for the treatment of rheumatoid arthritis and ulcerative colitis. Sulfasalazine is reported to suppress NF-κB activity.
-
mitochondria-targeted antioxidant
Demethyleneberberine is a natural mitochondria-targeted antioxidant. -
Autophagy inducer
Tomatidine hydrochloride acts as an anti-inflammatory agent by blocking NF-κB and JNK signaling. Tomatidine hydrochloride activates autophagy either in mammal cells or C elegans. -
NF-κB inhibitor
Urolithin B is one of the gut microbial metabolites of ellagitannins, and has anti-inflammatory and antioxidant effects. Urolithin B is also a regulator of skeletal muscle mass. -
traditional Chinese medicines
(±)-Praeruptorin A is the di-esterified product of cis-khellactone (CKL) and the major active ingredient in Peucedani Radix which consists of the dried roots of Peucedanum praeruptorumDunn (Apiaceae). (±)-Praeruptorin A has been widely employed as one of the famous traditional Chinese medicines (TCMs) for the treatment of cough with thick sputum and dyspnea, nonproductive cough and upper respiratory infections for centuries in China. (±)-Praeruptorin A has dramatically therapeutic effects on hypertension mainly through acting as a Ca2+-influx blocker. -
antithyroid agent
Methylthiouracil is an antithyroid agent. Methylthiouracil suppresses the production TNF-α and IL-6, and the activation of NF-κB and ERK1/2. -
antiinflammation agent
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. -
anticancer agent
Ursolic acid, a naturally occurring triterpenoid, induces the apoptosis of human cancer cells through multiple signaling pathways. -
NF-κB inhibitor
Cyclo(his-pro) (Cyclo(histidyl-proline)) is an orally active cyclic dipeptide structurally related to tyreotropin-releasing hormone. Cyclo(his-pro) could inhibit NF-κB nuclear accumulation. -
NF-κB inhibitor
WAY-204688 is an estrogen receptor (ER-α) selective, orally active inhibitor of NF-κB transcriptional activity with an IC50 of 122?±?30 nM for NF-κB-luciferase (NF-κB-luc) in HAECT-1 cells. -
NF-κB inhibitor
Edasalonexent (CAT-1004) is an orally bioavailable NF-κB inhibitor. -
NF-κB inhibitor
DMAPT (Dimethylamino Parthenolide), a water soluble analogue of Parthenolide (PTL), is an oral active NF-κB inhibitor, with a LD50 of 1.7 μM for cell population in AML cells. Has potential anti-cancer and anti-metastatic effect. -
NF-κB inhibitor
DHMEQ racemate is a NF-κB inhibitor. DHMEQ racemate is less active than (-)-DHMEQ. -
glutamate decarboxylase inhibitor
Chelidonic acid is a glutamate decarboxylase inhibitor, with a Ki of 1.2 μM. -
HMGB1 release inhibitor
Ethyl pyruvate is a simple derivative of the endogenous metabolite, pyruvic acid. Ethyl pyruvate is an anti-inflammatory agent. -
NF-κB Inhibitor
Micheliolide is a sesquiterpene lactone that functions as an NF-κB inhibitor. It exhibits significant anti-cancer and anti-inflammatory properties by attenuating high glucose-induced NF-κB activation and reducing the expression of inflammatory mediators such as MCP-1, TGF-β1, and FN in mouse mesangial cells. Additionally, Micheliolide inhibits LPS-induced NF-κB activation and the PI3K/Akt/p70S6K pathways, making it a valuable tool for studying inflammatory disease models, including colitis-associated cancer and rheumatic arthritis. -
NF-κB Inhibitor
Aristolochic acid A is a potent NF-κB inhibitor derived from the plant extracts of Aristolochia and Asarum species. This compound effectively diminishes the activities of activator protein 1 (AP-1) and NF-κB, making it a valuable tool for studying signaling pathways related to inflammation and cancer. Additionally, Aristolochic acid A has been shown to downregulate BLCAP gene expression in human cell lines, highlighting its potential for investigating gene regulation mechanisms. -
Endogenous Metabolite
Ergothioneine is an endogenous metabolite that acts as a potent antioxidant. It functions primarily as a specific inhibitor of p38 MAPK and Akt, which are critical signaling pathways involved in cellular stress responses. Ergothioneine is utilized in research focused on neuroprotection, cell apoptosis, and oxidative stress, making it a valuable compound for investigations into cellular resilience and health. -
PROTAC IRAK Degrader
Zomiradomide is an orally bioavailable PROTAC degrader targeting IRAK4, with a DC50 of 6 nM, which effectively inhibits the NF-κB signaling pathway. In addition to its suppression of IRAK4, Zomiradomide functions as a molecular glue, facilitating the degradation of Ikaros with a DC50 of 1 nM and consequently activating the type I IFN signaling pathway. This dual action positions Zomiradomide as a valuable tool in research focused on immune modulation and inflammatory responses. -
STAT3/NF-κB Inhibitor
Triacetylresveratrol is an acetylated analog of Resveratrol that functions as an inhibitor of STAT3 and NF-κB signaling pathways. It effectively reduces the phosphorylation levels of STAT3 and NF-κB in a dose- and time-dependent manner in PANC-1 and BxPC-3 cancer cell lines. Its promising anticancer activity makes it a valuable tool for research in cancer biology and therapeutic development. -
PDE Inhibitor
Theophylline, a potent phosphodiesterase (PDE) inhibitor, primarily targets PDE3, leading to relaxation of airway smooth muscle and enhanced bronchodilation. This compound also functions as an adenosine receptor antagonist and exhibits anti-inflammatory properties by elevating IL-10 levels and inhibiting NF-κB translocation into the nucleus. Additionally, Theophylline has been shown to induce apoptosis in certain cell types. Its applications are particularly relevant in the research of asthma and chronic obstructive pulmonary disease (COPD). -
TNF Receptor Inhibitor
Muscone, a TNF receptor inhibitor, is derived from the traditional Chinese medicine musk. It effectively inhibits NF-κB signaling and NLRP3 inflammasome activation, resulting in a significant reduction of inflammatory cytokines such as IL-1β, TNF-α, and IL-6. This compound is valuable in research focused on inflammation, cardiac function restoration, and improving survival rates in various pathological conditions. -
Apoptosis Inducer
Sanguinarine chloride is a benzophenanthridine alkaloid that functions as an apoptosis inducer primarily through the generation of reactive oxygen species (ROS). This compound is known to activate key signaling pathways, specifically JNK and NF-κB, facilitating programmed cell death. Sanguinarine chloride is widely utilized in cancer research and studies investigating apoptotic mechanisms. -
Anti-asthmatic Agent
Verproside, 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). -
Non-steroidal Anti-inflammatory Agent
Gaultherin is an orally active non-steroidal anti-inflammatory agent that selectively inhibits key inflammatory pathways, including NF-κB, MAPK, COX-2 (IC50 = 0.35 mg/mL), LOX (IC50 = 0.56 mg/mL), and HYAL (IC50 = 28.58 μg/mL). This compound demonstrates anti-inflammatory, antipyretic, and analgesic activities, making it suitable for research into inflammation-related conditions. Additionally, Gaultherin exhibits modest direct antioxidant capacity, particularly in cell-based models, while sparing COX-1, thus reducing the likelihood of gastrointestinal side effects commonly associated with traditional non-steroidal anti-inflammatory drugs. -
NF-κB Inhibitor
Sciadopitysin is a biflavonoid that serves as a potent NF-κB inhibitor. Its primary mechanism involves the inhibition of RANKL-induced osteoclastogenesis, contributing to the prevention of bone loss. By suppressing NF-κB activation and lowering the expression levels of c-Fos and NFATc1, Sciadopitysin demonstrates significant potential for research applications focused on bone metabolism and related disorders. -
Anti-inflammatory Agent
Darutoside is an orally active diterpene compound that functions primarily as an anti-inflammatory agent. It exhibits notable analgesic properties and enhances wound healing by inhibiting COX-2 expression and the migration of inflammatory cells. Additionally, Darutoside modulates macrophage polarization towards the M2 phenotype through NF-κB pathway inhibition, thereby reducing inflammation. This compound has been shown to significantly alleviate acute gouty arthritis by regulating metabolic networks involved in inflammatory responses. -
GR Agonist
Flumethasone is a highly selective and potent glucocorticoid receptor (GR) agonist. It effectively activates GR, leading to the inhibition of nuclear factor kappa B (NF-κB) and subsequent reduction of pro-inflammatory cytokine production, such as TNF-α and IL-1β. Additionally, Flumethasone upregulates anti-inflammatory gene expression, particularly IL-10, and modulates metabolic enzyme activity, including tyrosine aminotransferase. This compound is valuable for research into inflammatory diseases, cancer, and endocrine regulation. -
Bacterial Inhibitor
Ceftiofur is a cell wall synthesis inhibitor targeting bacterial penicillin-binding proteins (PBPs). It demonstrates bactericidal activity by interfering with the peptidoglycan synthesis in bacterial cell walls, resulting in cell lysis. Additionally, Ceftiofur exhibits anti-inflammatory properties by inhibiting the activation of NF-κB and MAPKs, which decreases the secretion of pro-inflammatory cytokines such as TNF-α, IL-1β, and IL-6. This makes Ceftiofur a valuable reagent in research investigating bacterial infections and inflammation processes. -
Pro-apoptotic Compound
Dracorhodin perchlorate is a pro-apoptotic compound that targets multiple signaling pathways, inhibiting PI3K/Akt and NF-κB activation. This natural product derived from Dragon's blood upregulates p53 expression, activates caspases, and induces reactive oxygen species (ROS), leading to programmed cell death. It is also known to regulate TLR4, thereby promoting wound healing and offering therapeutic potential in diabetes management. Additionally, Dracorhodin perchlorate exhibits anti-tumor activity against various cancers, including prostate, breast, and cervical cancer, making it a valuable tool for cancer research. -
Insecticide
Azadirachtin is a triterpenoid compound with potent insecticidal properties. It induces apoptosis in insect cells via the mitochondrial pathway, acting through the modulation of the Bcl-2/Bax ratio and activation of Apaf-1 and caspase-3. Additionally, Azadirachtin has demonstrated anti-inflammatory effects by inhibiting the NF-κB signaling pathway, and exhibits a range of other biological activities, including anticancer and antimalarial effects. This compound is widely utilized in research applications focused on pest control and the study of apoptotic mechanisms. -
NF-κB Inhibitor
Cardamonin is a potent NF-κB inhibitor derived from cardamom. It exerts broad biological activity by targeting key signaling pathways, including mTOR, Akt, STAT3, Wnt/β-catenin, and COX-2. This compound has demonstrated significant anticancer, anti-inflammatory, antimicrobial, and antidiabetic properties, making it valuable for various research applications in cancer biology and inflammation studies. -
GRPR Antagonist
Aurantiamide is a selective antagonist of the Gastrin-Releasing Peptide Receptor (GRPR), demonstrating significant anti-inflammatory and neuroprotective properties. It effectively mitigates inflammation and oxidative stress in renal tissues by targeting GRPR-mediated pathways, including RIPK3/MLKL signaling and NF-κB activation, thereby providing protection against acute kidney injury and promoting endothelial function. Additionally, Aurantiamide inhibits M1 microglial polarization and NLRP3 activation, showcasing efficacy in improving outcomes in Alzheimer's disease mouse models. Its notable in vivo effectiveness extends to various acute kidney injury contexts, including ischemia/reperfusion, sepsis, and hypertension models. -
RIPK1 PROTAC Degrader
LD4172 is a selective RIPK1 PROTAC degrader that exhibits a Ki of 4.8 nM. It facilitates RIPK1 protein degradation through the formation of a ternary complex with RIPK1 and VHL E3 ligase, leading to ubiquitination and proteasomal degradation. LD4172 effectively inhibits TNF-induced classical NF-κB signaling in TRAF2-deficient cells, significantly reducing IκBα phosphorylation and IL-8 production. Additionally, it promotes apoptosis and immunogenic cell death in tumor cells, enhances tumor-infiltrating lymphocyte responses, and sensitizes tumors to anti-PD1 therapy, making it a valuable chemical probe for studying RIPK1-related functions in melanoma and colon cancer research. -
NLRP3 Inhibitor
Tabersonine hydrochloride is a selective NLRP3 inhibitor that targets the NACHT domain of the NLRP3 protein, effectively inhibiting its ATPase activity and oligomerization. This action prevents ASC spot formation and caspase-1 activation, leading to a reduction in pro-inflammatory cytokine release, including IL-1β. Additionally, Tabersonine hydrochloride inhibits K63-linked ubiquitination of TRAF6, interfering with NF-κB, PI3K/Akt, and p38 MAPK signaling pathways. Its applications extend to the study of NLRP3-driven inflammatory conditions, such as acute lung injury, sepsis, and peritonitis, as well as in liver cancer research, where it induces apoptosis through mitochondrial and death receptor pathways. -
Anti-inflammatory/anti-cancer/anti-viral/anti-tuberculosis Agent
4-Methoxycinnamic acid ethyl ester is a bioactive natural compound that functions primarily as an anti-inflammatory, anti-cancer, anti-viral, and anti-tuberculosis agent. It demonstrates potent anti-inflammatory activity by inhibiting cyclooxygenases (COX-1 and COX-2) and NF-κB, resulting in reduced cytokine production. Additionally, 4-Methoxycinnamic acid ethyl ester effectively inhibits tumor cell proliferation, migration, and angiogenesis through the downregulation of VEGF expression. It also exhibits significant antiviral properties against dengue virus and antimicrobial activity against Mycobacterium tuberculosis, along with notable analgesic effects in preclinical models. -
TNF-α Inhibitor
TNF-α-IN-11 is a selective inhibitor of tumor necrosis factor alpha (TNF-α) with a dissociation constant (KD) of 12.06 μM. This compound effectively binds to TNF-α, preventing the activation of downstream caspase and NF-κB signaling pathways, as well as inhibiting the phosphorylation of IκBα and the subsequent nuclear translocation of NF-κB p65. TNF-α-IN-11 is suitable for research into TNF-α-mediated autoimmune conditions and the associated inflammatory processes. -
TLR4 Agonist
GlcNAc-MurNAc is a disaccharide that acts as a TLR4 agonist, exhibiting a binding affinity (Kd) of 383 μM for murine TLR4. This compound directly interacts with TLR4, subsequently activating the downstream NF-κB and IRF signaling pathways. Research indicates that GlcNAc-MurNAc ameliorates dextran sulfate sodium salt (DSS)-induced colitis in mice via a TLR4-dependent mechanism, making it a valuable tool for the investigation of inflammatory bowel disease. -
COX Inhibitor
Aspirin lithium is a potent, orally active, irreversible inhibitor of cyclooxygenase COX-1 and COX-2, exhibiting IC50 values of 5 and 210 μg/mL, respectively. This compound promotes apoptosis and inhibits the activation of NF-κB, making it valuable for studies on inflammation and cell death. Additionally, Aspirin lithium effectively inhibits platelet prostaglandin synthetase, providing potential protective effects against coronary artery and cerebrovascular thrombosis. -
RIPK2 Inhibitor
RIPK2-IN-6 is a selective inhibitor of RIPK2, effectively blocking its phosphorylation and subsequently inhibiting the NF-κB and MAPK signaling pathways. This compound exhibits significant anti-inflammatory and anti-fibrotic properties, demonstrated in Dextran sodium sulfate-induced colitis models in mice. RIPK2-IN-6 is valuable in research exploring therapeutic strategies for inflammatory and fibrotic diseases. -
Anti-inflammatory Agents
(±)-Naringenin is an orally bioavailable anti-inflammatory agent that modulates both acute and chronic inflammatory responses. Its biological activities include antioxidant, neuroprotective, hepatoprotective, and potential anti-cancer effects. (±)-Naringenin enhances vasodilation in endothelial cells via the activation of BKCa channels and demonstrates protective effects against experimental colitis by inhibiting the Toll-like receptor 4/NF-κB signaling pathway. This compound is relevant for research applications in sepsis, fulminant hepatitis, fibrosis, and cancer. -
Saturated Fatty Acid
10-Hydroxydecanoic acid (10-HDAA) is a saturated fatty acid that possesses notable anti-inflammatory properties. It exhibits a range of biological activities including anti-malarial, anti-Leishmania, and insecticidal effects, while also enhancing antigen-specific immune responses. Mechanistically, 10-HDAA inhibits NF-κB activation and interferon regulatory factor 1 (IRF-1) translation, leading to reduced levels of interleukin 6 (IL-6) and nitric oxide (NO) in inflammatory cells. Additionally, it plays a role in mitigating neuroinflammatory responses through the p53-autophagy and p53-NLRP3 pathways, making it a valuable reagent for studies in immunology and inflammation research.
