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IKK2 Inhibitor
LY2409881 is a selective inhibitor of IκB kinase β (IKK2), demonstrating potent inhibition with an IC50 of 30 nM. This compound is primarily used in research for its ability to modulate the NF-κB signaling pathway, making it relevant for studying inflammation, cancer, and autoimmune diseases. Researchers utilize LY2409881 to explore its therapeutic potential in various disease models and to investigate the role of IKK2 in cellular processes. -
IκB Kinase-2 Inhibitor
PS-1145 dihydrochloride is a selective inhibitor of IκB kinase-2, exhibiting an IC50 value of 88 nM. This compound effectively inhibits the phosphorylation of IκB kinase, thereby suppressing NF-κB activity. PS-1145 dihydrochloride is utilized in research applications targeting inflammatory responses and cancer biology. -
IKK2 Inhibitor
IKK-IN-4 is a selective inhibitor of IkappaB kinase 2 (IKKβ), exhibiting an IC50 of 45 nM for IKKβ and 650 nM for IKKα. This compound is instrumental in research focusing on the NF-κB signaling pathway and its regulation, providing insights into inflammation, cancer, and other diseases linked to IKK activity. IKK-IN-4 serves as a valuable tool for studying IKKβ-mediated signaling mechanisms and potential therapeutic interventions. -
IKK Inhibitor
(E/Z)-HOIPIN-1 is a selective inhibitor of the linear ubiquitin chain assembly complex (LUBAC), targeting the IκB kinase (IKK) pathway. With an IC50 value greater than 2.8 μM, this compound effectively inhibits LUBAC-mediated NF-κB activation. Its potential applications include studies of inflammatory responses, cancer biology, and the modulation of immune signaling pathways. -
IKKβ Inhibitor
MLN-0415 is an inhibitor of IKKβ, a key regulator in the NF-κB signaling pathway. This compound exhibits significant anti-inflammatory activity and is instrumental in researching conditions such as arthritis and other inflammatory diseases. MLN-0415 facilitates the exploration of therapeutic strategies targeting the modulation of inflammatory responses. -
IKKβ Inhibitor
1-Dehydro-[10]-gingerdione functions as a selective inhibitor of IKKβ by targeting its activation loop, leading to the disruption of IKKβ-mediated phosphorylation of IκBα in macrophages stimulated with various agonists. This compound effectively inhibits LPS-induced NF-κB transcriptional activity. 1-Dehydro-[10]-gingerdione holds promise for research into NF-κB-related inflammation and autoimmune disorders. -
IkappaB kinase inhibitor
CGA-JK3 is an ATP-competitive inhibitor of IκB kinase (IKKβ), effectively hindering its kinase activity. This compound inhibits the phosphorylation of IκBα in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells, demonstrating its potential in studying inflammatory signaling pathways. CGA-JK3 is useful for researchers investigating the modulation of NF-κB signaling and related biological processes. -
IKKα/β Inhibitor
GTCpFE is a selective inhibitor of IKKα/β, functioning within the NF-κB signaling pathway. This compound exhibits significant anti-inflammatory properties by preventing the nuclear translocation of the p65 subunit of NF-κB. Additionally, GTCpFE demonstrates targeted anti-cancer stem-like cell activity by impairing mammosphere formation and reducing the CD44+ CD24- immunophenotype associated with aggressive breast cancer. Its dual mechanism positions GTCpFE as a promising agent for both inflammation and cancer research. -
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. -
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. -
NF-κB Inhibitor
Armepavine is a potent NF-κB inhibitor derived from Nelumbo nucifera. It demonstrates significant anti-inflammatory effects on human peripheral blood mononuclear cells and exhibits immunosuppressive activity towards T lymphocytes and in lupus nephritic mice models. Armepavine effectively inhibits TNF-α-induced MAPK and NF-κB signaling pathways, making it a valuable reagent for research into inflammatory and autoimmune disorders. -
NF-κB Inhibitor
NF-κB-IN-4 is a potent inhibitor of the NF-κB signaling pathway, demonstrating significant blood-brain barrier permeability. This compound exhibits anti-neuroinflammatory activity through its ability to block the phosphorylation and activation of IκBα, thereby reducing NLRP3 expression and inhibiting NF-κB activation. NF-κB-IN-4 is suitable for research applications related to neuroinflammatory diseases, providing a valuable tool for therapeutic investigations. -
NF-κB Inhibitor
(R)-(-)-Ibuprofen is a selective inhibitor of NF-κB activation. It demonstrates significant anti-inflammatory and antinociceptive properties, making it a valuable tool in research related to inflammation and pain modulation. This compound is particularly useful for studying pathways associated with NF-κB and its role in inflammatory responses. -
NF-κB Inhibitor
Ginsenoside Rk3 functions as an NF-κB inhibitor, extracted from the roots of Panax ginseng. It exhibits significant inhibition of TNF-α-induced NF-κB transcriptional activity, with an IC50 value of 14.24±1.30 μM in HepG2 cells. This compound is useful in research focusing on inflammation, cancer, and signaling pathways mediated by NF-κB. -
NF-κB Inhibitor
Rubiadin-1-methyl ether is a natural anthraquinone that acts as an NF-κB inhibitor. It demonstrates significant biological activity by inhibiting osteoclastic bone resorption through the suppression of NF-κB p65 phosphorylation and the degradation of IκBα, resulting in decreased nuclear translocation of p65. This compound is relevant for research applications focusing on bone metabolism and inflammatory responses. -
NF-κB Inhibitor
Aristolochic acid A sodium is a potent NF-κB inhibitor derived from Aristolochia and Asarum species. This compound effectively diminishes the activity of both activator protein 1 (AP-1) and NF-κB, thereby modulating key signaling pathways involved in inflammation and cancer. Additionally, Aristolochic acid A sodium has been shown to reduce BLCAP gene expression in human cell lines, making it valuable for research in cell signaling and gene regulation. -
NF-κB Inhibitor
Suberosin is a potent NF-κB inhibitor derived from Plumbago zeylanica. It demonstrates significant anti-inflammatory and anticoagulant properties by suppressing PHA-induced proliferation of peripheral blood mononuclear cells (PBMC) and inhibiting cell cycle progression from the G1 phase to the S phase. Due to its ability to modulate the transcription factors NF-AT and NF-κB, Suberosin serves as a valuable tool in studies of inflammation and thrombosis. -
NF- B Inhibitor
2,4,6-Trihydroxybenzaldehyde is an orally active inhibitor of NF-κB, a key transcription factor involved in inflammatory and immune responses. This compound exhibits notable anti-tumor activity, inhibits cancer cell proliferation, and demonstrates anti-obesity effects. Its applications in cancer research and metabolic studies make it a valuable reagent for exploring mechanisms of disease and potential therapeutic strategies. -
NF-κB Inhibitor
Lucyoside B is a potent NF-κB inhibitor that effectively modulates inflammatory responses. It inhibits the production of various inflammatory mediators through the NF-κB and activator protein-1 signaling pathways in activated macrophages. This compound is valuable for research applications focused on understanding inflammation and its modulation in various disease states. -
OST-A Inhibitor
NGI-235 is a selective inhibitor of the OST-A enzyme, effectively blocking the glycosylation of Toll-like receptor 4 (TLR4). This compound demonstrates potent inhibition of NF-κB inflammatory signaling, making it a valuable tool for investigating mechanisms of inflammation and immune response regulation. NGI-235 is suitable for research applications focused on inflammatory diseases and TLR4-mediated pathways. -
NIK Inhibitor
NIK-IN-2 is a potent inhibitor of NF-κB-inducing kinase (NIK), exhibiting an impressive pIC50 of 7.4. This compound serves as a valuable tool in cancer research, enabling the investigation of NIK's role in NF-κB signaling pathways and their implications in tumorigenesis. Its selective inhibition of NIK provides insights into therapeutic strategies targeting NF-κB-related diseases. -
NF-κB Inhibitor
9-Hydroxycanthin-6-one is an alkaloid that functions as an NF-κB inhibitor, exhibiting significant biological activity. With an IC50 value of 3.8 μM, this compound effectively modulates the NF-κB signaling pathway. It offers potential applications in research related to inflammation, cancer, and other diseases driven by NF-κB activation. -
NF-κB Inhibitor
NBD peptide is a selective inhibitor of the NF-κB signaling pathway, acting by disrupting the interaction between NEMO and the IKK complex. This inhibition leads to reduced production of pro-inflammatory cytokines, showcasing its anti-inflammatory properties. Additionally, NBD peptide demonstrates immunosuppressive effects through modulation of immune cell activity. The incorporation of the cell-penetrating HIV-TAT peptide enhances its cellular uptake, facilitating its application in various research contexts. -
BRD4 BD2 Inhibitor
BRD4-BD1/2-IN-3 is a selective inhibitor of the BRD4 bromodomain 2 (BD2), exhibiting an IC50 of 0.41 nM for BRD4 BD2 compared to BRD4 BD1. This compound effectively inhibits LPS-induced expression of IL-6, demonstrating significant anti-inflammatory properties through modulation of the TNF and NF-κB signaling pathways. BRD4-BD1/2-IN-3 is valuable for research focused on inflammatory diseases. -
NF-κB Inhibitor
HSR1304 is a potent NF-κB inhibitor that targets the multifunctional transcription factor involved in various human diseases, including cancer and chronic inflammation. This compound demonstrates significant biological activity in modulating NF-κB signaling pathways. HSR1304 is intended for research applications focused on cancer biology and the development of anti-inflammatory strategies. -
NF-κB Inhibitor
Rubioncolin C is a potent NF-κB inhibitor that demonstrates significant anti-tumor activity. It promotes apoptotic and autophagic cell death in human cancer cells while effectively suppressing the NF-κB and Akt/mTOR/P70S6K signaling pathways. This compound is valuable for research focused on cancer biology and therapeutic development. -
NF-κB Inhibitor
(−)-N-Hydroxyapiosporamide is a potent NF-κB inhibitor known for its significant antitumor activity both in vitro and in vivo. Its biological properties make it particularly relevant for research applications targeting colorectal cancer (CRC). This alkaloid serves as a valuable tool for studying the mechanisms of NF-κB signaling and its role in tumor progression. -
NF-κB Inhibitor
NF-κB-IN-3 is a potent NF-κB inhibitor with an IC50 of 0.70 µM. It exhibits significant biological activity by disrupting the NF-κB signaling pathway, which is crucial in various cellular processes including inflammation and cancer progression. This compound is utilized in research applications focused on cancer biology and therapeutic interventions targeting NF-κB-related pathways. -
NF-κB Inhibitor
Stipuleanoside R2 is a potent inhibitor of NF-κB activation, specifically blocking the pathway triggered by TNFα. This compound demonstrates dose-dependent inhibitory activity, with an IC50 value of 4.1 μM. Stipuleanoside R2 can be utilized in research focused on inflammatory response, cancer biology, and other diseases associated with NF-κB signaling. -
NF-κB Inhibitor
Andrographolide-lipoic acid is an NF-κB inhibitor that combines Andrographolide and Lipoic acid. This compound exhibits significant anti-diabetic properties and provides protective effects on pancreatic β-cells. Its ability to modulate inflammatory pathways makes it a valuable tool for research in diabetes and related metabolic disorders. -
NF-κB Inhibitor
6-O-p-Hydroxybenzoylglutinoside is a selective NF-κB inhibitor that effectively suppresses TNF-α-activated NF-κB transcriptional activity, with an IC50 of 52.78 μM. This compound demonstrates targeted biological activity without significantly inhibiting soluble epoxide hydrolase (sEH), acetylcholinesterase (AChE), or butyrylcholinesterase (BChE). Isolated from the seeds of Catalpa bungei (Manchurian catalpa), 6-O-p-Hydroxybenzoylglutinoside is valuable for research applications focused on inflammation and signal transduction pathways. -
NF-κB Inhibitor
NF-κB-IN-10 is a potent inhibitor of the NF-κB signaling pathway, primarily targeting NF-κB activation. This compound has demonstrated the ability to alleviate heart failure by mitigating oxidative stress and inflammation through the modulation of the Nrf2/NF-κB axis. In RAW264.7 cells, NF-κB-IN-10 effectively inhibits lipopolysaccharide-induced nitric oxide production, as well as the expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2). This reagent is invaluable for research into cardiovascular diseases and related inflammatory processes. -
NF-κB Inhibitor
IKKγ NBD Inhibitory Peptide is a selective inhibitor of NF-κB signaling. It functions by disrupting the interaction between the IKKγ/NEMO-binding domain and IKKα/IKKβ, effectively blocking TNF-α-induced NF-κB activation. This peptide exhibits significant anti-inflammatory properties and has potential applications in studying cerebral ischemia and its associated neurological deficits. -
NF-κB Inhibitor
(Rac)-Myrislignan is a potent NF-κB inhibitor derived from Myristica fragrans Houtt. This compound demonstrates significant anti-inflammatory properties by effectively reducing LPS-induced inflammatory responses in murine macrophage cells. Its ability to inhibit the NF-κB signaling pathway makes (Rac)-Myrislignan a valuable tool for research into inflammation and related diseases. -
NF-κB Inhibitor
Helenalin isobutyrate is an NF-κB (p65 subunit) inhibitor known for its anti-inflammatory properties. It functions by irreversibly alkylating cysteine sulfhydryl groups within the p65 subunit, effectively diminishing the DNA binding activity of the NF-κB complex. This compound is valuable in research focused on understanding inflammation pathways and potential therapeutic interventions in related diseases.

