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Catalog No.
Product Name
Application
Product Information
Citations
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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
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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
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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
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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
- Parthenolide ((-)-Parthenolide) is a sesquiterpene lactone which occurs naturally in the plant feverfew (Tanacetum parthenium).
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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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
Cathepsin B Inhibitor
(Rac)-Z-FA-FMK is a potent inhibitor of cathepsin B, exhibiting a Ki value of 1.5 μM. This compound also inhibits multiple caspases, specifically caspases 2, 3, 6, 7, and 9, with IC50 values ranging from 6.147 to 110.7 μM. Additionally, (Rac)-Z-FA-FMK demonstrates antiviral activity by inhibiting the main protease involved in SARS-CoV-2 replication with an IC50 of 11.39 μM. It further attenuates the increase in IL-1β levels induced by LPS and represses NF-κB transactivation in macrophages, making it useful for research in inflammation and viral pathogenesis. -
MDM2 Inhibitor
LQFM030 is a novel small molecule inhibitor of MDM2, primarily targeting the MDM2-p53 interaction to promote cellular apoptosis. It demonstrates concentration-dependent cytotoxicity in K562 cells with an IC50 value of 0.28 mM, inducing G0/G1 phase cell cycle arrest and enhancing Caspase activity. LQFM030 also downregulates the expression of key oncogenes and proteins, including MDM2, MDMX, p73, MYC, and NF-κB. This compound is particularly valuable in cancer research, especially in the study of leukemia. -
Hsp90 Inhibitor
GUT-70 is a tricyclic coumarin that functions as a potent Hsp90 inhibitor. It activates caspases 2, 3, 8, and 9, leading to apoptosis in leukemic cells. Additionally, GUT-70 effectively inhibits HIV-1 replication in chronically infected cells by targeting the NF-κB signaling pathway. This compound is suitable for research applications involving leukemia, mantle cell lymphoma (MCL), and HIV-1 infection studies. -
Proteasome Inhibitor
TP-110 is a selective proteasome inhibitor that targets the protease-like activity of the 20S proteasome, leaving trypsin-like and peptidyl-glutamyl peptide hydrolysis activities unaffected. This compound effectively disrupts the NF-κB signaling pathway, leading to activation of caspases 3, 8, and 9, and subsequent PARP cleavage, while decreasing levels of anti-apoptotic proteins cIAP-1 and XIAP. TP-110 induces G2/M phase cell cycle arrest and promotes apoptosis in cancer cells, making it a valuable tool for researching various malignancies, including prostate cancer and multiple myeloma. -
NLRP3 Inhibitor
Tabersonine is a selective and orally active inhibitor of the NLRP3 inflammasome, targeting the NACHT domain to modulate its ATPase activity and prevent oligomerization. This mechanism effectively inhibits ASC speck formation and blocks caspase-1 activation, leading to reduced secretion of pro-inflammatory cytokines, including IL-1β. Additionally, Tabersonine interferes with K63-linked ubiquitination of TRAF6, disrupting NF-κB, PI3K/Akt, and p38 MAPK signaling pathways. It is primarily utilized in research on NLRP3-mediated inflammatory diseases, such as acute lung injury, sepsis, and peritonitis, as well as in studies related to liver cancer. -
TNFα inhibitor
Aloeresin G is a chromone glycoside derived from Aloe, demonstrating inhibitory activity against TNFα. It attenuates TNFα-induced NF-κB transcriptional activity, exhibiting an IC50 value of 40.02 μM. This compound is valuable for research focused on inflammatory pathways and the modulation of immune responses. -
DK/PI3K/BRD4 Inhibitor
SRX3177 is a potent triple inhibitor targeting CDK4/6, PI3K, and BRD4, with IC50 values of <2.5 nM for CDK4, 3.3 nM for CDK6, 79 nM for PI3Kα, 83 nM for PI3Kδ, 3.18 μM for PI3Kγ, and 33 nM and 89 nM for BRD4 BD1 and BD2, respectively. It exhibits broad cytotoxic activity against cancer cells while sparing normal epithelial cells, highlighting its potential as a targeted cancer therapeutic with reduced toxicity. -
RelB inhibitor
RS47 is a potent and specific inhibitor of the non-canonical NF-κB signaling pathway, acting by disrupting the binding of RelB to its target DNA with a Kd of 1.1 μM. It effectively inhibits the growth of colorectal cancer (CRC) cells and B lymphomas, making it a valuable research tool for studying and potentially targeting cancers driven by hyperactive non-canonical NF-κB signaling. -
Osteoclast formation inhibitor
ABD56 is a bioactive compound that inhibits osteoclast formation and induces osteoclast apoptosis. Its mechanism of action involves suppression of the NFκB and ERK signaling pathways, making it a promising candidate for research in bone metabolism and osteolytic diseases. -
Endoplasmic Reticulum Stress Inhibitor
Tauroursodeoxycholate (Tauroursodeoxycholic acid; TDUCA) dihydrate is an inhibitor of endoplasmic reticulum (ER) stress that significantly downregulates pro-apoptotic molecules, including caspase-3 and caspase-12. Additionally, it suppresses ERK signaling, contributing to its cytoprotective and anti-apoptotic effects. -
NF-κB inhibitor
Asperulosidic Acid (ASPA) is a bioactive iridoid glycoside isolated from the herb Hedyotis diffusa Willd., exhibiting anti-tumor, antioxidant, and anti-inflammatory properties. Its anti-inflammatory effects are associated with the downregulation of proinflammatory cytokines such as TNF-α and IL-6, mediated through inhibition of the NF-κB and MAPK signaling pathways. -
NF-κB/FAK/MAPK inhibitor
Keracyanin chloride is an orally active anthocyanin compound with potent antioxidant, anti-inflammatory, and hypoglycemic properties. It exerts its biological effects by inhibiting the NF-κB/FAK/MAPK signaling pathways, which are central to inflammation, cell adhesion, and metabolic regulation. -
ACAT inhibitor
Enniatin B1 is a mycotoxin produced by Fusarium species, known for its diverse bioactivities. It functions as a moderate inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT), with an IC₅₀ of 73 μM in assays using rat liver microsomes, implicating a role in lipid metabolism modulation. Enniatin B1 is capable of crossing the blood-brain barrier, suggesting potential effects on central nervous system function. It also decreases the activation of ERK1/2 (p44/p42 MAPK) and moderately inhibits TNF-α-induced NF-κB activation, indicating anti-inflammatory and cell signaling modulatory properties. -
PDE4/NF-κB inhibitor
Sappanone A is an orally active homoisoflavone isolated from Caesalpinia sappan L., exhibiting notable anti-inflammatory and antioxidant properties. It functions as an inhibitor of phosphodiesterase 4 (PDE4) and NF-κB, key regulators of inflammatory signaling. Additionally, Sappanone A activates the Nrf2 pathway, leading to increased expression of the cytoprotective enzyme heme oxygenase-1 (HO-1). Sappanone A also inhibits RANKL-induced osteoclastogenesis, suggesting potential benefits in bone metabolism disorders. With its multifaceted bioactivity, Sappanone A holds significant promise for research in inflammation-related diseases, cardiovascular conditions, and bone health. -
NF-kB inhibitor
EF24 is a synthetic curcumin analogue and a potent NF-κB inhibitor with demonstrated oral bioavailability and strong antitumor activity. It exerts its anticancer effects, particularly in oral squamous cell carcinoma (OSCC), through deactivation of the MAPK/ERK signaling pathway. EF24 is effective against various cancer cell lines, with GI₅₀ values of 0.7 μM in melanoma and 0.8 μM in breast cancer cells. In MDA-MB-231 (breast cancer) and DU-145 (prostate cancer) cells, EF24 induces cell cycle arrest and apoptosis, accompanied by increased activation of caspase-3 and caspase-9. It also reduces the phosphorylation of MEK1 and ERK, further contributing to its pro-apoptotic and anti-proliferative effects. These properties make EF24 a promising compound for cancer therapy research. -
Microglial inhibitor
Inflachromene is a microglial inhibitor that exerts anti-inflammatory effects by directly binding to high mobility group box proteins HMGB1 and HMGB2. Through this interaction, it effectively downregulates the proinflammatory activities of HMGB proteins, leading to reduced microglial activation and neuronal damage. Inflachromene holds promise as a therapeutic candidate for the treatment of neuroinflammatory disorders, including neurodegenerative diseases and central nervous system injuries. -
NF-κB p65 Inhibitor
Licochalcone D is a naturally occurring flavonoid primarily found in the root of *Glycyrrhiza uralensis* (Chinese licorice). It functions as a potent and orally active inhibitor of the NF-κB p65 subunit, a key regulator of inflammation and cancer-related signaling pathways. Licochalcone D exhibits broad pharmacological properties, including antioxidant, anti-inflammatory, and anticancer activities, making it a promising candidate for research in inflammation-related diseases and oncology. -
PDE Inhibitor
Theophylline sodium acetate functions as a potent phosphodiesterase (PDE) inhibitor, specifically targeting PDE3 to promote the relaxation of airway smooth muscle. It also acts as an adenosine receptor antagonist and histone deacetylase (HDAC) activator, contributing to its anti-inflammatory properties by elevating IL-10 levels and inhibiting NF-κB translocation to the nucleus. Additionally, Theophylline sodium acetate is known to induce apoptosis, making it a valuable reagent for research on asthma and chronic obstructive pulmonary disease (COPD). -
NF-κB Inhibitor
CAY10512 is a potent NF-κB inhibitor that effectively suppresses the upregulation of NF-κB-sensitive proinflammatory microRNAs, including miRNA-9, miRNA-125b, miRNA-146a, and miRNA-155, in cerebrospinal fluid and extracellular environments. This compound significantly reduces the release of pro-inflammatory cytokines such as TNF-α, MCP-1, IL-8, and IL-6. CAY10512 is valuable for research applications focused on neuroinflammation, islet transplantation, and the regulation of microRNA. -
COX-1/2 Inhibitor
Cudraflavone B is a prenylated flavonoid that functions as a dual inhibitor of COX-1 and COX-2, demonstrating significant anti-inflammatory and anti-tumor activity. This compound inhibits the translocation of nuclear factor κB (NF-κB) in macrophages, leading to decreased tumor necrosis factor α (TNFα) gene expression and secretion. Additionally, Cudraflavone B induces the mitochondrial apoptotic pathway while activating MAPK signaling pathways, including p38 and ERK, and upregulating SIRT1 expression. These mechanisms contribute to its efficacy in attenuating the growth of human oral squamous cell carcinoma cells, making it a valuable tool for cancer research. -
sEH Inhibitor
sEH-IN-21 is a potent inhibitor of soluble epoxide hydrolase (sEH), displaying IC50 values of 0.1 nM for both human and mouse sEH isoforms. This compound effectively inhibits NF-κB signaling pathways and demonstrates significant anti-inflammatory activity by reducing the release of pro-inflammatory cytokines IL-6 and TNF-α. Additionally, sEH-IN-21 helps maintain intestinal barrier integrity, making it a valuable tool for research on inflammatory bowel disease (IBD) and related inflammatory conditions. -
NF-κB Inhibitor
Panaxytriol is a potent NF-κB inhibitor that effectively reduces the nuclear translocation of NF-κB. This mechanism leads to decreased production of pro-inflammatory cytokines, including TNF-α, IL-1β, and IL-6, as well as nitric oxide in response to LPS stimulation. Additionally, Panaxytriol promotes the upregulation of CYP3A4 through activation of the nuclear receptors PXR and CAR. Its ability to improve motor dysfunction in mouse models of brain inflammation makes Panaxytriol valuable for research into neurodegenerative diseases, such as Alzheimer's disease.
