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Proteasomal Degrader
(S,R,S)-AHPC-Boc derivative 1 is a selective proteasomal degrader that targets MALT1. By recruiting the E3 ubiquitin ligase CRBN, it forms a ternary complex with MALT1, facilitating its ubiquitination and subsequent proteasomal degradation. This compound inhibits the NF-κB signaling pathway by disrupting the CBM complex, which may induce apoptosis in ABC-DLBCL cells. (S,R,S)-AHPC-Boc derivative 1 is valuable for the investigation of MALT1-dependent cancers, particularly diffuse large B-cell lymphoma (DLBCL). -
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. -
Stable Isotope
D-Ribose (mixture of isomers)-13C5 is a stable isotope-labeled form of D-Ribose, which serves as a crucial sugar moiety in adenosine triphosphate (ATP) production. It functions as an energy enhancer and is commonly employed in metabolic therapy for conditions such as chronic fatigue syndrome and cardiac energy metabolism. Additionally, D-Ribose is involved in protein glycation and can stimulate NF-κB-dependent inflammation through the receptor for advanced glycation end-products (RAGE). This makes it a valuable tool for research in metabolic and inflammatory 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. -
Stable Isotope
Stachydrine-d6 is a deuterated form of Stachydrine, a compound known for its role in promoting blood circulation and alleviating blood stasis, particularly in the traditional Chinese herb Leonurus heterophyllus. This stable isotope can be used in tracing studies and metabolic research due to its labeled nature. Additionally, Stachydrine exhibits inhibitory effects on the NF-κB signaling pathway, highlighting its potential in studies related to inflammation and immunity. -
Secondary Metabolite
Moniliphenone is a secondary metabolite derived from the endophytic fungus Penicillium chrysogenum. This compound exhibits notable anti-inflammatory properties and effectively inhibits TNF-α-stimulated NF-κB activation, making it a valuable tool for exploring pathways involved in inflammation. Its applications in research can aid in understanding the molecular mechanisms of inflammatory diseases and developing potential therapeutic strategies. -
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. -
Chalcone
4'-Hydroxychalcone is a chalcone derivative known for its hepatoprotective properties. It exerts its biological activity by inhibiting TNFα-induced NF-κB activation through the modulation of the proteasome. Additionally, 4'-Hydroxychalcone has been shown to induce rapid potassium release from mitochondrial vesicles, adversely affecting respiratory control and oxidative phosphorylation in isolated rat liver mitochondria. This compound is valuable for research focused on liver protection and mitochondrial function. -
Stable Isotope
Metaxalone-d3 is a deuterium-labeled form of Metaxalone, an FDA-approved muscle relaxant primarily acting on the central nervous system. Its primary mechanism involves inhibition of polysynaptic reflex arcs, promoting muscle relaxation. Additionally, Metaxalone demonstrates inhibitory effects on MAO-A, contributing to its anti-inflammatory and antioxidant properties. This reagent is useful for research applications investigating inflammatory responses, as it modulation of IL-1β-induced phenotypes impacts NF-κB and related signaling pathways in microglia. -
Stable Isotope
Metaxalone-d6 is a deuterium-labeled analog of Metaxalone, an FDA-approved muscle relaxant primarily targeting the central nervous system. It promotes muscle relaxation by inhibiting polysynaptic reflex arcs and also exhibits activity as an inhibitor of MAO-A, contributing to anti-inflammatory and antioxidant effects. Metaxalone effectively reduces the IL-1β-induced inflammatory phenotype, modulates NF-κB signaling pathways, and lowers both expression and activity of MAO-A in IL-1β-treated microglia, making it a valuable tool for research in neurobiology and inflammation. -
Anti-inflammatory Drug
Sanggenon A is an anti-inflammatory compound that modulates the NF-κB and HO-1/Nrf2 signaling pathways, demonstrating significant effects in BV2 and RAW264.7 cells. This reagent effectively inhibits the lipopolysaccharide (LPS)-induced production of nitric oxide, making it a valuable tool for research into inflammatory processes and potential therapeutic applications in inflammation-related diseases. -
Phenylpropanoid Glycoside
Tadehaginoside is a phenylpropanoid glycoside that plays a crucial role in regulating lipogenesis and glucose metabolism. This compound exhibits antioxidant properties and offers hepatoprotective effects by modulating Nrf2 and NF-κB signaling pathways, thereby mitigating oxidative stress and inflammation in liver cells. Tadehaginoside is applicable in research focusing on obesity and diabetes, providing insights into metabolic regulation and associated pathologies. -
E-isomer of Tadehaginoside
(E)-Tadehaginoside is the E-isomer of Tadehaginoside, a phenylpropanoid glycoside known for its role in modulating lipogenesis and glucose metabolism. This compound exhibits antioxidant properties and provides liver protection against oxidative stress and inflammation by influencing the Nrf2 and NF-κB signaling pathways in hepatocytes. (E)-Tadehaginoside is suitable for research applications focused on obesity and diabetes. -
Antioxidant Agent
Santamarine is a sesquiterpene lactone that serves as an effective antioxidant agent. It enhances the expression of heme oxygenase-1 (HO-1) through the translocation of nuclear factor erythroid 2–related factor 2 (Nrf2) while inhibiting the production of nitric oxide (NO), prostaglandin E2 (PGE2), tumor necrosis factor-alpha (TNF-α), and interleukin-1 beta (IL-1β) by blocking NF-κB translocation in LPS-stimulated macrophages. Additionally, Santamarine displays anti-photoaging effects by inhibiting the MAPK/AP-1 pathway and promoting TGF-β/Smad signaling in UVA-irradiated human dermal fibroblasts, highlighting its potential for various biological applications. -
ITK PROTACs Degrader
BSJ-05-037 is an ITK PROTACs degrader that efficiently induces the degradation of ITK in T-cell lymphoma cell lines. This compound inhibits the NF-κB/GATA-3 signaling pathway and decreases PLCγ1 phosphorylation, thereby reducing the proliferation of T-cell lymphoma cells. Additionally, BSJ-05-037 enhances the sensitivity of these cancer cells to chemotherapy. In mouse models, it has shown the ability to diminish GATA-3 expression, lower tumor volume, and counteract chemotherapy resistance, making it a valuable tool for research on T-cell lymphoma. -
Neuroprotective Agent
Hericenone C is a neuroprotective agent derived from the mushroom Hericium erinaceus. It has been shown to inhibit lipopolysaccharide (LPS)-induced NRE::Luc luciferase activity, reduce the phosphorylation of p65, and suppress NF-κB signaling pathways. Due to these effects, Hericenone C is useful for research focused on neuroprotection and the modulation of inflammatory responses in neurological disorders. -
NF-κB Activator
NF-κB activator 1 is a potent activator of the NF-κB signaling pathway, exhibiting an EC50 of 0.9 μM. This compound effectively induces the expression of superoxide dismutase (SOD)2 mRNA, contributing to enhanced cellular antioxidant responses. NF-κB activator 1 is valuable for research applications focusing on inflammation, oxidative stress, and related signaling pathways. -
Anti-inflammatory agent
N,N-Dimethylacetamide (DMAc) is an anti-inflammatory agent that primarily inhibits the NF-κB signaling pathway. Its ability to traverse the blood-brain barrier and function as an FDA-approved drug excipient enhances its utility in various research contexts. DMAc is particularly relevant for investigating the mechanisms of weight gain related to high-fat diets and exploring neuroinflammation associated with Alzheimer's disease. -
Vitamin K2
Geranylgeraniol is an orally active vitamin K2 precursor that functions as an intermediate in the mevalonate pathway. It primarily targets the NF-kB signaling pathway, demonstrating the potential to reduce LPS-induced microglial inflammation in animal models. This compound is valuable for research investigating neuroinflammation and the broader implications of vitamin K2 in cellular signaling and immune responses. -
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. -
Gibberellin
Gibberellin A4 is a bioactive gibberellin that primarily targets gibberellin receptors, promoting flowering in apple trees. Additionally, it demonstrates anti-NF-κB and antioxidant activities, making it valuable in studies investigating inflammatory pathways. Gibberellin A4 is also applicable in research focused on periodontal diseases, contributing to the understanding of plant and human health interactions. -
NF- B Activator
NF-κΒ Activator 2 is a potent and orally active NF-κB activator, exhibiting an EC50 of 1.58 μM. This compound enhances the expression and activation of NF-κB, leading to the induction of SOD2. NF-κΒ Activator 2 is useful in researching mechanisms related to amyotrophic lateral sclerosis (ALS) and other conditions associated with 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. -
Anti-Oxidative/Inflammatory Agent
Sulfuretin is a potent anti-oxidative and anti-inflammatory agent that inhibits the NF-κB signaling pathway. It demonstrates efficacy in reducing oxidative stress, platelet aggregation, and mutagenesis, making it relevant for research in allergic airway inflammation. Sulfuretin acts as a competitive inhibitor of monophenolase and diphenolase activities, with an IC50 of 13.64 μM, underscoring its significance in exploring inflammatory responses and oxidative damage in biochemical studies. -
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. -
NF-κB Inhibitor
Myrcene, a natural aromatic compound, functions as an NF-κB inhibitor by suppressing TNFα and NF-κB activity. It exhibits notable anti-invasive properties, induces cell cycle arrest, and promotes apoptosis in cancer cells. Additionally, myrcene demonstrates significant blood protective effects and possesses anti-inflammatory activity, making it valuable for various research applications in cancer and inflammation studies. -
Bcl3 Inhibitor
JS6 is a potent Bcl3 inhibitor that disrupts the interaction between Bcl3 and NF-κB1. This compound demonstrates significant anti-tumor activity by inhibiting tumor cell growth in both in vitro and in vivo models. JS6 is valuable for research focused on cancer biology, specifically regarding NF-κB signaling pathways and their implications in tumorigenesis. -
NF-κB Inhibitor
Deoxyelephantopin is a natural bioactive sesquiterpene lactone that primarily targets NF-κB signaling pathways. It exhibits potent anticancer activity across various cancer types by inhibiting key cellular signaling mechanisms, including MAPK, PI3K/Akt, and β-catenin. This compound serves as a valuable tool for researchers investigating cancer biology and therapeutic interventions. -
NF-κB Inhibitor
Handelin is a guaianolide dimer derived from Chrysanthemum boreale that acts as a potent inhibitor of NF-κB signaling. This compound effectively down-regulates the production of pro-inflammatory cytokines, demonstrating significant anti-inflammatory activity. Handelin is valuable for research applications focused on inflammation, immune response modulation, and related signaling pathways. -
NF-κB Inhibitor
Galloylpaeoniflorin is a potent NF-κB inhibitor that plays a significant role in modulating inflammatory responses. Its mechanism involves the inhibition of NF-κB signaling, which is critical in various pathological conditions. This compound is valuable for research applications focused on inflammation, cancer, and other diseases linked to dysregulated NF-κB activity. Additionally, Galloylpaeoniflorin has been shown to inhibit DNA cleavage, contributing to its potential therapeutic effects in molecular biology studies. -
NF-κB Inhibitor
14-Deoxy-11,12-didehydroandrographolide is a potent inhibitor of NF-κB activation. This natural compound, an analogue of Andrographolide, demonstrates significant anti-inflammatory properties by modulating the NF-κB signaling pathway. It is suitable for research applications investigating inflammation, cancer, and autoimmune disorders. -
NF-κB Inhibitor
Quinoclamine, a naphthoquinone derivative, functions as an NF-κB inhibitor. It has demonstrated anti-cancer properties, making it a valuable tool for cancer research and the investigation of NF-κB signaling pathways. Its ability to modulate NF-κB activity opens avenues for studying inflammatory responses and potential therapeutic approaches in oncology. -
NIK Inhibitor
XT2 is a selective inhibitor of NF-κB-inducing kinase (NIK), demonstrating potent oral activity with an IC50 of 9.1 nM. It effectively suppresses the CCl4-induced upregulation of alanine aminotransferase (ALT), a significant biomarker for acute liver injury, and reduces immune cell infiltration in damaged liver tissue. XT2 is valuable for investigating inflammatory liver diseases and features an alkyne group for click chemistry applications, allowing for copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules.

