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Catalog No.
Product Name
Application
Product Information
Citations
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Survivin Inhibitor
MX107 is a selective survivin inhibitor known for its potent efficacy in suppressing the proliferation of triple-negative breast cancer (TNBC) cells. By inducing the degradation of survivin and inhibitor-of-apoptosis proteins (IAPs), MX107 effectively inhibits nuclear factor κB (NF-κB) activation in response to DNA damage. This compound enhances the tumoricidal effects of genotoxic treatments when used in conjunction with chemotherapeutic agents, making it a valuable tool in cancer research and therapy development. -
RIPK2 Inhibitor
CSLP43 is a selective inhibitor of RIPK2, demonstrating an IC50 of 19.9 nM against human RIPK2. By binding to the ATP-binding pocket of RIPK2, CSLP43 disrupts its interaction with the BIR2 domain of XIAP and cIAP1, effectively inhibiting RIPK2 ubiquitination and regulating NOD1- and NOD2-dependent inflammatory signaling pathways, as well as NF-κB activation. This compound is particularly relevant for research investigating Crohn's disease, Blau syndrome, early-onset sarcoidosis, and early-onset inflammatory bowel disease, due to its selectivity for the NOD1/NOD2 signaling pathway without affecting RIPK1 or RIPK3 activity. -
NF-κB Inhibitor/p53 Activator
CBLC100 is an NF-κB inhibitor and a p53 activator that exhibits potent anticancer properties. By targeting FACT, CBLC100 induces cytotoxicity through both p53-dependent apoptotic and non-apoptotic pathways. This compound is particularly relevant for research applications centered on cancers, including fibrosarcoma, making it a valuable tool for studying tumorigenesis and therapeutic responses. -
p53-MDM2 Inhibitor
p53-MDM2-IN-2 is an orally active inhibitor targeting the p53-MDM2 interaction, exhibiting a Ki value of 0.25 μM. This compound demonstrates antitumor activity through the inhibition of the NF-κB signaling pathway. It is valuable in research studies focusing on cancer therapy and elucidating the molecular mechanisms of tumor suppression. -
p53-MDM2 Inhibitor
p53-MDM2-IN-3 is a potent p53-MDM2 inhibitor with a Ki value of 0.25 μM, demonstrating oral bioavailability. This compound exhibits significant antitumor activity through its inhibition of the NF-κB signaling pathway. It serves as a valuable tool for cancer research, particularly in studies focused on targeting the p53-MDM2 interaction and the subsequent effects on tumor proliferation and survival. -
Herbicide/Microtubule inhibitor
Ethalfluralin is a dinitroaniline herbicide that functions as a microtubule inhibitor. By disrupting intranuclear spindle formation, Ethalfluralin effectively obstructs nuclear division and cytokinesis in parasites. This compound also enhances phosphorylation of NF-κB and P38 MAPK while inhibiting the PI3K/AKT signaling pathway, leading to impaired mitochondrial functionality, apoptosis, endoplasmic reticulum stress, autophagy, and increased reactive oxygen species (ROS) production. Ethalfluralin is particularly relevant for research applications in toxoplasmosis and related parasitic diseases. -
NLRP3 Inhibitor
NLRP3-IN-78 is a potent inhibitor of the NLRP3 inflammasome, demonstrating a 46.72% inhibition rate in GSDMD-induced pyroptosis at a concentration of 5 μM. This compound effectively binds to the NLRP3 protein, hindering GSDMD-NT oligomerization and cleavage while also suppressing upstream NF-κB signaling. NLRP3-IN-78 serves as a valuable tool for investigating anti-inflammatory mechanisms and the role of NLRP3 in various disease models. -
EPAC2 Inhibitor
MAY0132 is a potent and selective inhibitor of the EPAC2 pathway, exhibiting an IC50 of 0.4 μM. This compound significantly impedes the replication of human metapneumovirus (HMPV), adenovirus (AdV), and respiratory syncytial virus (RSV), while also decreasing cytokine and chemokine production induced by viral infections. Furthermore, MAY0132 inhibits NF-κB activation, underscoring its utility in research focused on antiviral mechanisms and respiratory virus pathogenesis. -
TRPA1 Inhibitor
Aurothiomalate disodium acts as a TRPA1 inhibitor, effectively blocking NF-κB activation and inhibiting iNOS expression. This compound fosters the M2 transformation of macrophages and enhances the expression of TREM-2 and arginase-1. Aurothiomalate disodium is applicable in research concerning liver fibrosis, cirrhosis, and arthritis, providing insights into inflammation and tissue repair mechanisms. -
CDK8/19 Inhibitor
Senexin A hydrochloride is a selective inhibitor of cyclin-dependent kinases 8 and 19 (CDK8 and CDK19), with an IC50 of 280 nM for CDK8. It specifically targets and inhibits p21-induced transcription, while sparing other biological functions of p21. In addition, Senexin A hydrochloride effectively suppresses CMV-GFP induction and the p21 stimulatory activity of NF-κB-dependent promoters, making it a valuable tool for studying transcriptional regulation and cell signaling pathways. -
CDK8 Inhibitor
CDK8-IN-15 is a selective inhibitor of cyclin-dependent kinase 8 (CDK8), exhibiting a potent IC50 of 57 nM. This compound enhances the thermal stability of CDK8 while effectively inhibiting NF-κB signaling pathways. CDK8-IN-15 demonstrates promising biological activity in an in vitro psoriasis model induced by TNF-α, alleviating inflammation and promoting the expression of anti-inflammatory markers such as Foxp3 and IL-10. This makes it a valuable tool for research into psoriasis and related inflammatory disorders. -
ACAT Inhibitor
ACAT-IN-7 is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor. This compound effectively inhibits ACAT activity, resulting in altered lipid metabolism and subsequent reduction in cholesterol esterification. ACAT-IN-7 is of particular interest in research exploring its potential role in inflammatory processes, as it inhibits NF-κB mediated transcription, which is crucial for various cellular responses. -
ACAT Inhibitor
ACAT-IN-2 is a selective inhibitor of acyl-Coenzyme A:cholesterol acyltransferase (ACAT). This compound effectively inhibits the NF-κB mediated transcriptional process, making it a valuable tool for research in cholesterol metabolism and inflammatory pathways. ACAT-IN-2 is primarily utilized in studies investigating dyslipidemia and its associated diseases, contributing to a deeper understanding of lipid regulation and associated pathophysiology. -
ACAT Inhibitor
ACAT-IN-10 is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor that provides valuable insights into lipid metabolism. This compound is particularly useful in studying the regulation of cholesterol esters and their implications in various diseases, including atherosclerosis and metabolic disorders. Additionally, ACAT-IN-10 exhibits weak inhibition of NF-κB-mediated transcription, making it a potential tool for investigating inflammatory pathways. -
ACAT Inhibitor
ACAT-IN-4 hydrochloride is a selective acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor. It disrupts cholesterol esterification, leading to a reduction in lipid accumulation in cells. This compound has significant implications for research in atherosclerosis, inflammation, and lipid metabolism, particularly through its ability to inhibit NF-κB mediated transcription. -
ACAT Inhibitor
ACAT-IN-9 is a selective acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor that effectively disrupts the synthesis of cholesteryl esters. By inhibiting ACAT activity, ACAT-IN-9 also attenuates NF-κB mediated transcription, which plays a critical role in inflammation and immune responses. This compound is utilized in research focusing on lipid metabolism, cardiovascular diseases, and inflammation pathways. -
ACAT Inhibitor
ACAT-IN-4 is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor that effectively impedes ACAT activity. This compound has been shown to inhibit NF-κB mediated transcription, making it a valuable tool for studying cholesterol metabolism and inflammatory responses. ACAT-IN-4 is suitable for research applications focusing on lipid regulation, atherosclerosis, and other related cardiovascular conditions. -
ACAT Inhibitor
ACAT-IN-10 dihydrochloride is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor. This compound exhibits weak inhibition of NF-κB mediated transcription, highlighting its potential role in modulating inflammatory processes. It is primarily utilized in research focused on lipid metabolism and its implications in various diseases, including atherosclerosis and metabolic disorders. ACAT-IN-10 dihydrochloride serves as a valuable tool for investigating the biochemical pathways regulated by ACAT activity. -
ACAT Inhibitor
ACAT-IN-6 is a potent acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor. This compound effectively inhibits NF-κB mediated transcription, making it a valuable tool for studying lipid metabolism and inflammatory pathways. ACAT-IN-6 is useful in research applications focused on cholesterol homeostasis and related diseases. -
ACAT Inhibitor
ACAT-IN-3 is an inhibitor of acyl-Coenzyme A:cholesterol acyltransferase (ACAT), targeting the cholesterol esterification pathway. This compound effectively inhibits NF-κB-mediated transcription, making it a valuable tool in studying pathways associated with inflammation and lipid metabolism. Its application in research may help elucidate the role of ACAT in various disease models, particularly those related to atherosclerosis and other metabolic disorders. -
ACAT Inhibitor
ACAT-IN-5 is a selective inhibitor of acyl-Coenzyme A:cholesterol acyltransferase (ACAT), a key enzyme involved in cholesterol metabolism. By inhibiting ACAT activity, ACAT-IN-5 has been shown to modulate NF-κB mediated transcription, thereby influencing inflammatory pathways and lipid metabolism. This reagent is vital for research applications exploring cholesterol homeostasis, atherosclerosis, and related metabolic disorders. -
CHI3L1 Inhibitor
CHI3L1-IN-5 is a selective inhibitor of CHI3L1, exhibiting a KD value of 6 μM. This compound enhances astrocytic clearance by rejuvenating lysosomal function and promoting Aβ uptake, while simultaneously mitigating neuroinflammation through inhibition of the NF-κB pathway. CHI3L1-IN-5 is valuable for investigating its potential therapeutic applications in Alzheimer's disease research. -
NF-κB Inhibitor
(R)-(+)-Anatabine is an NF-κB inhibitor that acts to lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). As the less active R-enantiomer of Anatabine, it retains the ability to modulate α4β2 nAChR activity. This compound exhibits anti-inflammatory properties and is being investigated for its potential applications in the treatment of neurodegenerative disorders. -
Calcium Channel Inhibitor
Nothofagin is a dihydrochalcone that acts as a calcium channel inhibitor. By blocking calcium influx, it downregulates NF-κB translocation, providing a mechanism to modulate inflammatory responses. This compound exhibits antioxidant properties and has potential applications in research related to septic responses and vascular inflammation. -
NF-κB/MAPKs Inhibitor
Tetrahydropiperine is a selective inhibitor of NF-κB and MAPKs, while simultaneously activating the PI3K/Akt/mTOR pathway. This compound effectively reduces the production of pro-inflammatory cytokines, including TNF-α, IL-6, and nitric oxide, by inhibiting the nuclear translocation of NF-κB and the phosphorylation of ERK, JNK, and p38 MAPKs. Additionally, Tetrahydropiperine mitigates excessive autophagy, offering neuroprotective benefits against oxidative damage. Its diverse biological activities make it valuable for research focused on inflammatory conditions, such as endotoxemia and arthritis, as well as neurological disorders, including ischemic stroke. -
Anti-oxidant, Aromatase Inhibitor, Anabolic Agent
5-Methyl-7-methoxyisoflavone is an orally active antioxidant that primarily functions as an aromatase inhibitor. This compound disrupts testosterone metabolic pathways, making it useful in various anabolic applications. It exhibits enhanced potency in increasing muscle mass and endurance compared to other anabolic agents. Additionally, 5-Methyl-7-methoxyisoflavone supports fat loss, contributes to the maintenance of low cholesterol levels, and aids in strengthening bone density. The compound also acts as an inhibitor of NF-κB, further expanding its potential therapeutic applications. -
MALT1 Inhibitor
Z-VRPR-FMK is an irreversible inhibitor of the MALT1 protein. It effectively inhibits the growth and invasion of diffuse large B-cell lymphoma by blocking MALT1-induced NF-κB activation and matrix metalloproteinase (MMP) expression. This makes Z-VRPR-FMK a valuable tool for research investigating the role of MALT1 in oncogenesis and therapeutic strategies targeting NF-κB pathways. -
MALT1 Inhibitor
MALT1-IN-5 is a potent inhibitor of the MALT1 protease, targeting the NF-κB signaling pathway. This compound has demonstrated significant biological activity in disrupting MALT1-dependent signaling processes. MALT1-IN-5 is primarily utilized in cancer research to investigate the role of MALT1 in tumorigenesis and its potential as a therapeutic target. -
MALT1 Inhibitor
NVS-MALT1 is an allosteric inhibitor of the MALT1 protein, disrupting its activity and providing a valuable tool for studying MALT1-mediated signaling pathways. This compound demonstrates the ability to modulate NF-κB activation and enhance apoptosis in cancer cells, making it relevant for research in oncology and immune response. It is particularly useful in investigations focusing on B-cell lymphoma and other MALT1-associated diseases. -
MALT1 Inhibitor
RGT-068A is a selective and orally bioavailable inhibitor of MALT1 (Mucosa-associated lymphoid tissue lymphoma translocation protein 1). This compound demonstrates potent inhibitory activity against MALT1, which is essential for NF-κB signaling in various hematological malignancies and inflammatory diseases. RGT-068A serves as a valuable tool for research into therapeutic strategies targeting MALT1 in cancer and autoimmune disorders. -
NF-κB Inhibitor
SEMBL is a potent inhibitor of NF-κB, specifically targeting NF-κB-DNA binding to disrupt its transcriptional activity. This compound effectively reduces the secretion of NF-κB-dependent inflammatory cytokines and diminishes cancer cell migration and invasion by decreasing matrix metalloproteinase (MMP) expression. SEMBL is valuable for research in anticancer therapies and the study of inflammation-related pathways. -
NF-κB Nuclear Accumulation Inhibitor
Cyclo(his-pro) TFA is a cyclic dipeptide that functions as an NF-κB nuclear accumulation inhibitor. This compound is capable of crossing the blood-brain barrier, making it valuable for studying its effects on various inflammatory and stress-related pathways. Its ability to modulate NF-κB activity supports research in neuroinflammation and other related conditions. -
20S Proteasome Inhibitor
5-Amino-8-hydroxyquinoline is a non-competitive inhibitor of the 20S proteasome, demonstrating potent inhibitory effects on NF-κB activity. This compound induces apoptosis in cancer cells while exhibiting minimal cytotoxicity towards normal hematopoietic cells. It is valuable for research applications in cancer biology, particularly in the study of leukemia and related malignancies. -
Immunoproteasome β5i Subunit Inhibitor
DPLG3 is a selective inhibitor of the immunoproteasome β5i subunit, demonstrating an IC50 of 4.5 nM. It effectively inhibits the mouse i-20S proteasome with an IC50 value of 9.4 nM. DPLG3 is capable of downregulating the protein levels of NF-κB p50 and p65, highlighting its potential in the study of immune-related diseases and therapeutic applications. -
Proteasome Inhibitor
Biotin-(Oaa)3-epoxomicin is a biotinylated proteasome inhibitor derived from Epoxomicin, connected through three hydrophilic oxaacetyl amino acid linkers. This compound is utilized primarily in proteomic research for the capture and identification of proteasome complexes, facilitating target validation and elucidation of intracellular targets. Epoxomicin effectively inhibits proteasome activity through covalent binding to catalytic subunits such as LMP7, X, MECL1, and Z, with a pronounced effect on chymotrypsin-like activity, while sparing non-proteasomal proteases like trypsin and papain. Additionally, it serves as an NF-κB inhibitor, demonstrating potential in studies of inflammatory responses. -
20S Proteasome Inhibitor
5-Amino-8-hydroxyquinoline dihydrochloride is a potent non-competitive inhibitor of the 20S proteasome. This compound effectively inhibits NF-κB activity, leading to apoptosis in cancer cells while exhibiting minimal cytotoxicity towards normal hematopoietic cells. Its unique properties make it a valuable tool for cancer research, particularly in studies related to leukemia and other malignancies. -
Proteasome Inhibitor
Z-LLF-CHO (Z-Leu-Leu-Phe-CHO) is a potent inhibitor of the chymotrypsin-like activity of the proteasome, exhibiting an inhibition constant (Ki) of 460 nM. This compound also functions as an inhibitor of NF-κB nuclear translocation, making it valuable for studies involving immune response and inflammation. Research applications include investigations into proteolytic processes and the role of cytokines in various disease models. -
Proteasome Inhibitor
4-Nitrochalcone serves as a proteasome inhibitor, specifically targeting the proteasomal degradation pathway. It effectively inhibits the activity of NF-κB induced by TNFα, making it a valuable tool for studying inflammatory processes and signaling pathways. This compound is utilized in research focused on cancer, neurodegenerative diseases, and other conditions where proteasome activity plays a critical role. -
Trx/TrxR System Inhibitor
PMX464 is a thiol-reactive quinol that acts as an inhibitor of the thioredoxin-thioredoxin reductase (Trx/TrxR) system. This compound has been shown to inhibit NF-κB-mediated pro-inflammatory activation in human type II alveolar epithelial cells, making it a valuable tool for research focused on inflammation and oxidative stress. PMX464 is particularly useful in studies examining the role of redox signaling in various pathophysiological conditions. -
Tyrosinase Inhibitor
MHY884 is a potent tyrosinase inhibitor that effectively mitigates UVB-induced activation of the NF-κB signaling pathway by downregulating oxidative stress. This compound demonstrates a reduction in oxidative stress within melanoma cells, leading to diminished NF-κB activity in irradiated models. MHY884 holds significant promise for investigations into the mechanisms of UVB-induced skin damage and its potential therapeutic applications. -
Aβ Inhibitor
TML-6 is an orally active curcumin derivative that functions as a β-amyloid (Aβ) inhibitor by impeding the synthesis of β-amyloid precursor protein. It demonstrates key biological activities including the upregulation of Apo E, suppression of NF-κB and mTOR pathways, and enhancement of the anti-oxidative Nrf2 response. TML-6 is positioned as a promising candidate for research in Alzheimer's disease (AD) mechanisms and therapeutic developments. -
NIK Inhibitor
B022 is a selective inhibitor of NF-κB-inducing kinase (NIK) with a Ki of 4.2 nM and an IC50 of 15.1 nM. This compound exhibits protective effects against liver inflammation, oxidative stress, and injury caused by toxins. Additionally, B022 features an alkyne group, enabling its use in click chemistry applications, specifically for copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules. -
NF-κB Inhibitor
Helenalin is a sesquiterpene lactone that acts as an inhibitor of the transcription factor NF-κB. By directly targeting the p65 subunit, Helenalin exhibits alkylating activity through its interaction with cysteine sulfhydryl groups, effectively hindering NF-κB's ability to bind DNA. This compound is primarily utilized in research focused on anti-inflammatory pathways and mechanisms involving NF-κB signaling. -
NF-κB Inhibitor
NF-κB-IN-11 is a selective NF-κB inhibitor that targets the NF-κB signaling pathway. It effectively inhibits TNF-α induced activation of NF-κB and prevents its nuclear translocation, leading to down-regulation of phospho-IKK, IκBα, and NF-κB p65 expression levels. This compound demonstrates significant anti-inflammatory properties, as evidenced by its ability to alleviate dextran sulfate sodium-induced colitis in murine models. NF-κB-IN-11 also exhibits a maximum tolerated dose (MTD) exceeding 1852 mg/kg in acute toxicity assessments in mice, highlighting its safety profile for research applications. -
NF-κB Inhibitor
Bezisterim is a synthetic derivative of the natural anti-inflammatory steroid β-AET, functioning as a partial inhibitor of NF-κB. This compound effectively reduces pro-inflammatory signals, such as IL-6 and matrix metallopeptidase 3, and demonstrates the ability to penetrate the blood-brain barrier in murine models. Bezisterim is valuable in research applications related to ulcerative colitis, arthritis, and experimental autoimmune encephalomyelitis. Additionally, its alkyne group allows it to participate in copper-catalyzed azide-alkyne cycloaddition, making it a versatile tool in click chemistry. -
NF-κB Inhibitor
AP-1/NF-κB activation inhibitor 1 is a potent inhibitor of AP-1 and NF-κB-mediated transcriptional activation, with an IC50 of 1 μM. This compound does not interfere with basal transcription driven by the β-actin promoter, making it suitable for study in various cellular contexts. Additionally, AP-1/NF-κB activation inhibitor 1 effectively reduces IL-2 and IL-8 production in stimulated cells, supporting its utility in inflammatory and immunological research applications. -
NF-κB/AP-1 Inhibitor
SP-100030 is a potent inhibitor of NF-κB and activator protein-1 (AP-1), exhibiting IC50 values of 50 nM for both targets. This compound effectively suppresses the production of pro-inflammatory cytokines, including IL-2, IL-8, and TNF-alpha, in Jurkat and other T cell lines. Additionally, SP-100030 has demonstrated efficacy in reducing symptoms in murine models of collagen-induced arthritis (CIA). -
c-Rel Inhibitor
IT-901 is a potent and orally active inhibitor of the NF-κB subunit c-Rel, exhibiting an IC50 of 0.1 μM for NF-κB DNA binding and 3 μM for c-Rel DNA binding. As a bioactive derivative of naphthalenethiobarbiturate, IT-901 holds promise for therapeutic applications in human lymphoid tumors and may provide benefits in mitigating graft-versus-host disease (GVHD). This compound is valuable for research in cancer and immunological responses, facilitating the exploration of NF-κB-related pathways. -
NF-κB Inhibitor
DMAPT (Dimethylamino Parthenolide) is a potent inhibitor of NF-κB signaling, characterized by an LD50 of 1.7 μM in acute myeloid leukemia (AML) cells. This compound exhibits significant anti-cancer and anti-metastatic properties, making it a valuable tool for research in cancer therapeutics. DMAPT can be used to investigate the role of NF-κB in cancer progression and to explore new treatment strategies. -
NF-κB Inhibitor
Hesperidin methylchalcone is a potent NF-κB inhibitor, functioning as an orally bioavailable flavonoid with notable analgesic, anti-inflammatory, and antioxidant properties. Its ability to inhibit oxidative stress, cytokine production, and NF-κB activation highlights its potential in managing inflammatory conditions. This compound is particularly relevant for research into gout disease and related inflammatory disorders.
