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iNOS Inhibitor
Asperuloside is an iridoid compound derived from Hedyotis diffusa, primarily known for its role as an inducible nitric oxide synthase (iNOS) inhibitor. This compound exhibits notable anti-inflammatory properties by suppressing the NF-κB and MAPK signaling pathways. Asperuloside is valuable in studying inflammatory processes and developing therapeutic strategies for related diseases. -
NF-κB Inhibitor
Neocryptotanshinone is a potent NF-κB inhibitor derived from Salvia miltiorrhiza. This compound effectively suppresses lipopolysaccharide-induced inflammation by targeting and inhibiting the NF-κB and iNOS signaling pathways. It shows promise in research applications focused on inflammatory diseases and provides valuable insights into the mechanisms of immune response modulation. -
iNOS/Nf-Κb Inhibitor
Hymenoxin is a dual inhibitor of inducible nitric oxide synthase (iNOS) and nuclear factor kappa B (NF-κB), exhibiting IC50 values of 42.7 μM and 85.5 μM, respectively. This compound demonstrates the capacity to reduce oxidative stress by 16% at a concentration of 125 μg/mL. Hymenoxin is primarily utilized in research focused on inflammatory responses and related signaling pathways. Its inhibitory effects on key regulators make it valuable for studies investigating the roles of iNOS and NF-κB in various disease models. -
NOS Inhibitor
SDMA (p-hydroxyazobenzene-p′-sulfonate) is a potent endogenous inhibitor of nitric oxide synthase (NOS), making it a valuable tool for studying NOS-related pathways. This compound has been shown to activate NF-κB, leading to increased expression of pro-inflammatory cytokines such as IL-6 and TNF-α. Additionally, SDMA demonstrates stability in serum and plasma, allowing its use as a biomarker for assessing hepatic and renal dysfunction in various research applications. -
iNOS/ICAM-1 Inhibitor
Aloenin aglycone is an inhibitor of iNOS and ICAM-1, derived from aloe exudate. It effectively suppresses TNFα-induced NF-κB transcriptional activity with an IC50 of 18.7 μM. Additionally, at a concentration of 10 μM, it significantly reduces the expression of both inducible nitric oxide synthase (iNOS) and intercellular adhesion molecule 1 (ICAM-1) in HepG2 cells following TNFα stimulation. This compound serves as a valuable tool for investigating inflammatory pathways and potential therapeutic interventions in related conditions. -
FOXP3 Inhibitor
Peptide P60 is a potent FOXP3 inhibitor that disrupts the nuclear translocation of FOXP3, thereby decreasing its regulatory effects on NF-κB and NFAT signaling pathways. This action inhibits the immunosuppressive capabilities of regulatory T cells, facilitating the proliferation and activation of effector T cells. Experimental studies have shown that Peptide P60 can induce lymphoproliferative autoimmune syndrome in neonatal ICR mice and diminish the population of CD4+CD25+Foxp3+ T cells in the spleen. Additionally, it enhances the efficacy of peptide vaccines and recombinant adenovirus-based vaccines, making it valuable for research in tumor immunology, viral infections, and autoimmune conditions. -
RANKL Inhibitor
RANKL-IN-1 is a selective and orally bioactive inhibitor of Receptor Activator of Nuclear Factor-κB Ligand (RANKL), displaying a KD value of 7.6 μM. This compound effectively inhibits osteoclastogenesis with an IC50 of 0.07 μM and a selectivity index of 82.57. RANKL-IN-1 directly interacts with RANKL, preventing downstream activation of the NF-κB and MAPK signaling pathways. It is a valuable tool for investigating metabolic disorders, particularly osteoporosis. -
STING Inhibitor
STING-IN-4 is a potent STING inhibitor that effectively reduces the expression and activation of STING and nuclear factor-κB (NF-κB) signaling pathways. This compound exhibits significant anti-inflammatory activity, making it a valuable tool for investigating sepsis and related inflammatory conditions. Researchers can utilize STING-IN-4 to explore the therapeutic potential of modulating STING activity in various biological contexts. -
NF-κB Inhibitor
Eupenicisirenin C is a potent inhibitor of the NF-κB signaling pathway. This compound effectively suppresses the cGAS-STING pathway, demonstrating significant potential in modulating inflammatory responses. Notably, Eupenicisirenin C inhibits RANKL-induced osteoclast differentiation in bone marrow macrophages, making it a valuable tool for research into bone metabolism and inflammatory diseases. -
BACH1 Inhibitor
ASP-8731 is a potent BACH1 inhibitor that enhances NRF2-mediated gene transcription, thereby activating antioxidant and anti-inflammatory pathways. This compound significantly upregulates the expression of key genes such as HMOX1 and FTH1, and increases fetal hemoglobin (HbF) levels, promoting F-cell production in hydroxyurea-unresponsive cells. Additionally, ASP-8731 mitigates inflammatory responses by downregulating VCAM1, ICAM-1, and NF-κB (p65) phosphorylation. Its ability to relieve glutathione depletion and microcirculatory stasis suggests potential applications in the treatment of sickle cell disease and other hematological disorders. -
COX-2 Inhibitor
COX-2-IN-51 is a selective COX-2 inhibitor exhibiting an IC50 of 70.7 nM. It effectively reduces LPS-induced release of nitric oxide (NO) and prostaglandin E2 (PGE2), as well as the expression of COX-2 and inducible nitric oxide synthase (iNOS), and inhibits the NF-κB signaling pathway. This compound demonstrates anti-inflammatory and analgesic properties in various murine models by targeting the NF-κB cascade, while presenting a lower risk of gastrointestinal side effects compared to traditional nonsteroidal anti-inflammatory drugs. -
COX-2/15-LOX Inhibitor
COX-2/15-LOX-IN-5 is a potent dual inhibitor of cyclooxygenase-2 (COX-2) and 15-lipoxygenase (15-LOX). This compound effectively attenuates lipopolysaccharide-induced NF-κB activation in RAW 264.7 macrophages, highlighting its role in modulating inflammatory responses. COX-2/15-LOX-IN-5 exhibits significant anti-inflammatory and antioxidant properties, making it a valuable tool for research into inflammatory diseases and other related biological processes. -
COX-2/TAK1-NF-κB Inhibitor
BPD is a selective inhibitor of COX-2 and TAK1-NF-κB, exhibiting an IC50 of 18.5 μM for COX-2. This compound effectively reduces the transcriptional expression of key pro-inflammatory cytokines, including iNOS, TNF-α, IL-6, and IL-1β, thereby demonstrating notable anti-inflammatory properties. BPD has been shown to inhibit carrageenan-induced paw edema and mitigate LPS-induced septic mortality, making it a valuable tool for research in inflammation and related pathways. -
NF-κB/COX Inhibitor
Methoxycoronarin D is a potent inhibitor of NF-κB, demonstrating an IC50 value of 7.3 μM. Additionally, it selectively inhibits cyclooxygenase-1 (COX-1), with an IC50 value of 0.9 μM. This compound is relevant for research applications focused on inflammation and cancer due to its ability to modulate critical signaling pathways. -
COX-2 Inhibitor
Cavidine is a selective COX-2 inhibitor that exhibits potent anti-inflammatory properties. It is particularly useful in research concerning skin injuries, hepatitis, cholecystitis, and scabies. Additionally, Cavidine has been shown to alleviate LPS-induced acute lung injury through modulation of the NF-κB signaling pathway, making it a valuable compound for studying inflammation-related conditions. -
Sphingomyelinase Inhibitor, K-Ras Inhibitor, H-Ras Inhibitor, NF-κB Inhibitor
Avicin G is a potent inhibitor of sphingomyelinases, specifically targeting neutral sphingomyelinases (SMPD2/3) and acid sphingomyelinase (SMPD1). This compound elevates intracellular sphingomyelin levels and modulates the distribution of sphingomyelin, disrupting signal transduction pathways in oncogenic K-Ras and H-Ras. Avicin G exhibits significant biological activity, including the reduction of ERK and Akt phosphorylation and alterations in lysosomal pH. Its applications extend to research on pancreatic ductal adenocarcinoma and non-small cell lung cancer. -
AP-1/NF-κB Activation Inhibitor
SPC 839 is an orally active inhibitor that targets AP-1 and NF-κB mediated transcriptional activation, demonstrating an IC50 of 0.008 μM. This compound is essential for studying pathways associated with inflammation, cancer progression, and cellular stress responses. Its potent inhibition of key transcription factors makes it a valuable tool for researchers investigating the role of AP-1 and NF-κB in various biological processes. -
NF-κB Inhibitor
Ganoderic acid H is a lanostane-type triterpene that functions as an NF-κB inhibitor. It effectively suppresses the growth and invasive behavior of breast cancer cells by inhibiting the activity of transcription factors AP-1 and NF-κB. This compound holds potential for research applications in cancer biology, particularly for studies focusing on the modulation of signaling pathways involved in tumor progression and metastasis. -
NF-κB/AP-1 Inhibitor
Glucocorticoid receptor modulator 1 is a selective non-steroidal modulator that targets the glucocorticoid receptor, exhibiting potent inhibition of NF-κB and AP-1 with IC50 values of 9 nM and 130 nM, respectively. This compound effectively reduces the expression of key inflammatory cytokines, including IL-6, IL-1β, and TNF-α. Additionally, it demonstrates potential in alleviating dermatitis in preclinical models, making it a valuable tool for research in inflammation and immune response. -
COX Inhibitor
Inulicin (1-O-Acetylbritannilactone) is a potent inhibitor of cyclooxygenase (COX) enzymes, specifically targeting COX-2 activity. This compound demonstrates significant biological activity by inhibiting lipopolysaccharide (LPS)-induced production of prostaglandin E2 (PGE2) as well as the expression of COX-2. Additionally, Inulicin suppresses NF-κB activation and its translocation, making it valuable for research applications related to inflammation and cancer. -
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. -
11β-hydroxysteroid dehydrogenase 1 Inhibitor
Lunularin is a selective inhibitor of 11β-hydroxysteroid dehydrogenase 1, exhibiting an IC50 of 45.44 μM for human and 17.39 μM for rat enzymes. This compound has been shown to modulate gene expression by upregulating Sirt1 and Hmox1 in liver tissue, while also reducing food intake, body weight gain, and blood glucose levels in high-fat diet mice. Furthermore, Lunularin displays anti-cancer properties by inhibiting cell proliferation and colony formation in renal and colon cancer cell lines, along with suppression of LPS-induced NF-κB pathway activation. This reagent is valuable for research in obesity, cancer biology, inflammation, and metabolic disorders. -
ACAT Inhibitor
ACAT-IN-8 is a selective inhibitor of acyl-Coenzyme A:cholesterol acyltransferase (ACAT), a key enzyme involved in intracellular cholesterol esterification. By inhibiting ACAT, this compound modulates lipid metabolism and significantly impacts NF-κB mediated transcription. ACAT-IN-8 is useful for research applications related to cardiovascular diseases, metabolic disorders, and inflammation, providing insights into cholesterol-related pathways and their regulation. -
NF-κB Inhibitor, GPx Inhibitor, HIV Replication Inhibitor
α-MSH (11-13) acetate is a selective melanocortin-1 receptor ligand that functions as an inhibitor of NF-κB, GPx activity, and HIV replication. It induces an acute elevation of intracellular calcium levels under certain costimulation or pathway inhibition conditions. This compound effectively suppresses TNF-α-induced NF-κB activation, inhibits colony formation of Staphylococcus aureus and Candida albicans, and demonstrates potential in the study of infections related to these pathogens, as well as in traumatic brain injury, corneal epithelial wounds, and inflammatory bowel disease research. -
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. -
IKKα Inhibitor
BAY32-5915 is a selective inhibitor of IKKα, exhibiting an IC50 value of 60 nM. This compound effectively prevents the activation of NF-κB without interfering with Doxorubicin-induced pathways. It is valuable for research in inflammation and cancer, providing insights into NF-κB signaling modulation. -
IKK/NF-κB Inhibitor
NF-κB-IN-1 is a selective inhibitor of the IκB kinase (IKK) and functions primarily through the inhibition of NF-κB signaling. This compound effectively blocks the activation of NF-κB, demonstrating potent anti-cancer activity by reducing cell viability in lung cancer cells. Additionally, NF-κB-IN-1 significantly diminishes the clonogenic potential of A549 cells, making it a valuable tool for research on cancer therapeutics targeting NF-κB pathways. -
IKK Inhibitor
SU1261 is a potent inhibitor of IKK, displaying Ki values of 10 nM for IKKα and 680 nM for IKKβ. This compound effectively inhibits non-canonical NF-κB signaling pathways, making it a valuable tool for studying the role of IKK in various cellular processes. Its application in research, particularly in osteosarcoma cell models such as U2OS, can provide insights into inflammatory responses and oncogenic signaling mechanisms. -
IKK/NF-κB Inhibitor
SR12343 is an IKK/NF-κB inhibitor that acts as a mimetic of the NF-κB essential modulator (NEMO)-binding domain. It effectively disrupts the interaction between IKKβ and NEMO, leading to inhibition of TNF-α- and LPS-induced NF-κB activation, with an IC50 of 37.02 μM for TNF-α-mediated pathways. SR12343 has been shown to reduce LPS-induced acute pulmonary inflammation in murine models, making it valuable for research into inflammatory and degenerative diseases. -
IKKβ Inhibitor
BOT-64 is a selective IκB kinase β (IKKβ) inhibitor with an IC50 value of 1 µM. This compound effectively inhibits lipopolysaccharide-induced activation of nuclear factor-κB (NF-κB) and the subsequent transcription of NF-κB-regulated inflammatory genes. BOT-64 is valuable for research into inflammatory pathways and NF-κB signaling, providing insights into potential therapeutic strategies for inflammatory diseases. -
ikkβ Inhibitor
IKKβ-IN-4 is a selective inhibitor of IkappaB kinase-β (IKKβ), with an IC50 value of 1.9 μM. IKKβ plays a crucial role in the NF-κB signaling pathway, which is implicated in various diseases, including inflammation and cancer. This compound is utilized in research to study the modulation of NF-κB activity and its potential therapeutic applications in related disease models. -
IKK2 Inhibitor
IKK2-IN-3 is a selective inhibitor of IKK2, demonstrating a potent inhibitory effect with an IC50 value of 0.075 μM. This compound effectively disrupts the NF-κB signaling pathway, impacting various cellular processes such as inflammation and immune response. IKK2-IN-3 is suitable for research applications involving the modulation of IKK2 activity in disease models and studying the role of NF-κB in cellular signaling.

