Catalog No.
Product Name
Application
Product Information
Citations
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TLR4/NF-kB/MAPK Inhibitor
TLR4/NF-κB/MAPK-IN-1 is an inhibitor targeting the TLR4/NF-κB/MAPK signaling pathways. It exhibits significant anti-neuroinflammatory activity by suppressing the activation of these pathways, leading to reduced inflammatory responses. This compound is particularly useful for research applications focusing on neuroinflammation and related neurodegenerative diseases. -
TLR4/NF-κB Inhibitor
Ligusticum cycloprolactam is a potent TLR4/NF-κB inhibitor with significant anti-inflammatory properties. It has been shown to alleviate renal injury by effectively disrupting the TLR4/NF-κB signaling pathway in both in vivo and in vitro models. In studies, Ligusticum cycloprolactam reduces serum uric acid levels, diminishes tubular damage, and decreases inflammatory infiltration and interstitial collagen deposition, leading to improved renal function. This compound serves as a valuable reagent for research into hyperuricemic nephropathy. -
TLR1/2 Agonist
SMU-C409 is a Toll-like receptor 1/2 (TLR1/2) agonist, exhibiting an EC50 of 65 nM in HEK-Blue hTLR2 cells. It activates the TLR1/2–MyD88–NF-κB signaling pathway, leading to increased secretion of pro-inflammatory cytokines TNF-α and IL-1β, which promotes robust immune cell activation. With low toxicity observed in vitro, SMU-C409 serves as a valuable tool for cancer immunotherapy research. -
TLR1/2 Heterodimer Agonist
SMU-C68 is a selective small-molecule agonist of the TLR1/2 heterodimer, with an EC50 value of 0.009 μM. It effectively activates the NF-κB and MAPK signaling pathways, leading to the release of pro-inflammatory cytokines such as TNF-α and IL-1β. This compound is a valuable tool for investigating mechanisms of inflammation and cancer biology in research applications. -
NF-κB Inhibitor
NF-κB-IN-14 is an NF-κB inhibitor that effectively modulates inflammatory responses by significantly inhibiting nitric oxide production in LPS-stimulated macrophages, with an IC50 of 6.4 μM. This compound disrupts the TLR4-MyD88 protein interaction, leading to the suppression of the NF-κB signaling pathway. Additionally, NF-κB-IN-14 has demonstrated efficacy in reducing ear edema and inflammation in a mouse model of atopic dermatitis, highlighting its potential utility in inflammatory research. -
Toll-like Receptor (TLR) Ligand
Ste2Cys is a diacylglycerol cysteine-type lipid molecule that serves as a ligand for Toll-like Receptor 2 (TLR2). It activates the NF-κB signaling pathway, leading to the upregulation of MHC II class molecules on the surface of mouse bone marrow-derived dendritic cells. This compound is valuable for research into the development of immunologic vaccines and enhancing immune responses. -
TLR2 Agonist
TLR2 Agonist 1 is a highly potent agonist for human toll-like receptor 2 (TLR2), exhibiting an EC50 of 116 pM. It activates NF-κB promoter activity through TLR2/TLR1 heterodimerization, making it a valuable tool for studying TLR-mediated immune responses. This compound is applicable in research focused on inflammation, innate immunity, and potential therapeutic strategies involving TLR pathways. -
MyD88 Inhibitor
LM9 is a selective inhibitor of MyD88, a key adaptor protein in the Toll-like receptor (TLR) signaling pathway. By blocking the binding of TLR4 to MyD88, LM9 disrupts MyD88 homodimer formation and subsequent activation of the NF-κB signaling pathway. This compound demonstrates significant anti-inflammatory effects, mitigating atherosclerosis and fibrosis in models of obesity-induced cardiomyopathy. LM9 is valuable for research focused on understanding the mechanisms of inflammation, fibrosis, and cardiovascular diseases. -
μ Opioid Receptor Antagonist
β-Funaltrexamine (β-FNA) is an irreversible and selective antagonist of the μ-opioid receptor. This compound demonstrates significant anti-inflammatory and neuroprotective properties by modulating TLR4 signaling, inhibiting cytokine-induced iNOS activation, and reducing neuroinflammation. Additionally, β-FNA influences NF-κB signaling and chemokine expression in human astrocytes and murine models. It is an important tool for research into neurodegenerative diseases, including stroke. -
Steroidal Alkaloid Glycoside
Esculeoside A is a spirosolane-type steroidal alkaloid glycoside that primarily targets NF-κB and Nrf2/Keap1 signaling pathways. This compound exhibits significant cardioprotective and hypoglycemic properties, regulating glucose metabolism and modulating lipid profiles. Research applications include the study of diabetic cardiomyopathy, type 2 diabetes, atopic dermatitis, tumors, and atherosclerotic diseases. Additionally, Esculeoside A inhibits dendritic cell maturation and T-cell proliferation, and exhibits anti-tumor activity against breast cancer and melanoma cells. -
TLR4/JNK/NF-κB Inhibitor
TLR4-IN-2 is an inhibitor targeting TLR4, JNK, and NF-κB pathways. It demonstrates anti-inflammatory properties by reducing nitric oxide production in LPS-stimulated RAW264.7 cells, with an IC50 of 23.2 µM. By inhibiting TLR4 expression and diminishing JNK phosphorylation, TLR4-IN-2 effectively suppresses NF-κB activation and the transcription of inflammation-related genes, leading to lower levels of iNOS, COX-2, and various inflammatory mediators. This compound shows potential for investigating therapeutic strategies in inflammatory diseases such as rheumatoid arthritis and other inflammatory disorders. -
NF-κB Inhibitor
Ergolide is a selective NF-κB/p65 and NLRP3 inhibitor that effectively disrupts the NF-κB signaling pathway and inhibits the nuclear translocation of p65. By irreversibly binding to the NACHT domain of NLRP3, Ergolie suppresses inflammasome assembly, significantly reducing the production of inflammatory mediators such as NO and PGE2. This compound promotes apoptosis in cancer cells, induces autophagy, and generates reactive oxygen species (ROS). Ergolide also enhances the therapeutic efficacy of vincristine and has been shown to alleviate acute lung injury in models of sepsis and inflammation, contributing to research in metastatic uveal melanoma, neurodegenerative diseases, and acute lymphoblastic leukemia. -
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.
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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.
