NF-κB

Sul-121 hydrochloride is a potent NF-κB inhibitor that effectively reduces airway inflammation and hyperresponsiveness in models of chronic obstructive pulmonary disease (COPD). This compound demonstrates a dose-dependent inhibition of lipopolysaccharide-induced airway neutrophilia and attenuates oxidative stress markers in human airway smooth muscle cells. By preventing the nuclear translocation of the NF-κB subunit p65, Sul-121 hydrochloride decreases the release of pro-inflammatory cytokines, making it a valuable tool for investigating inflammatory pathways in respiratory diseases.

OT-551 is a selective NF-κB inhibitor that exhibits both antioxidant and anti-inflammatory properties. This compound is utilized in research focused on retinal diseases, providing a valuable tool for exploring the mechanisms of inflammation and oxidative stress in these conditions. Its ability to modulate NF-κB signaling pathways positions OT-551 as a promising candidate for therapeutic development in ocular research.

9,10-Dimethoxycanthin-6-one is an alkaloid compound that functions as an inhibitor of NF-κB. It demonstrates significant inhibitory activity with an IC50 value of 19.5 μM. This compound is primarily utilized in research pertaining to inflammatory responses and cancer pathways, making it relevant for studies investigating NF-κB signaling modulation.

Teuclatriol is an NF-κB inhibitor derived from Salvia mirzayanii, exhibiting notable anti-inflammatory properties. It effectively inhibits TNF-α secretion in a dose-dependent manner, making it valuable for research involving inflammatory pathways and the modulation of NF-κB activity. This compound is essential for studies focused on chronic inflammation, autoimmune diseases, and related therapeutic developments.

NF-κB-IN-13 is a selective inhibitor of the NF-κB signaling pathway. This compound effectively suppresses lipopolysaccharide (LPS)-induced NF-κB activation and nitric oxide (NO) production in RAW264.7 macrophages, demonstrating its potential anti-inflammatory properties. NF-κB-IN-13 is valuable for research applications focusing on inflammation, immune response modulation, and potential therapeutic strategies for related diseases.

APC0576 is an NF-κB inhibitor that effectively disrupts the activation of the NF-κB signaling pathway, demonstrating an IC50 of 1.0 μM for β-galactosidase. This compound significantly inhibits the release of IL-1-induced chemokines, making it a valuable tool for research related to diseases involving pathological endothelial cell activation. Its targeted action allows for the exploration of therapeutic strategies aimed at modulating inflammatory responses.

CAY10657 is a potent NF-κB inhibitor that effectively downregulates the expression of proinflammatory cytokines, including IL-6, and chemokines such as MCP-1. This compound demonstrates significant anti-inflammatory activity, particularly in the context of meningitis induced by Streptococcus suis. CAY10657 is a valuable tool for researchers investigating inflammation and associated signaling pathways.

Icariside F2 is a selective NF-κB inhibitor with an IC50 value of 16.25 μM. This aromatic glycoside, extracted from the leaves of E. ulmoides Oliver, exhibits significant anti-inflammatory activity. It is utilized in biomedical research to explore therapeutic strategies for conditions mediated by NF-κB signaling.

CID 7309015 is a selective inhibitor of retinoic acid-related orphan receptor gamma (ROR-γ). This compound demonstrates significant potential in modulating inflammatory pathways, particularly in the context of NF-κB signaling and inflammatory arthritis research. CID 7309015 serves as a valuable tool for investigating the roles of ROR-γ in immune response and inflammatory diseases.

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-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.

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.

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.

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.

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.

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-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-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.

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.

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.

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.

(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.

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.

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.

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.

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.

Gabexate mesylate is a competitive proteasome inhibitor, primarily targeting serine proteinases such as thrombin and Factor Xa. It exhibits diverse biological activity, including anticoagulant effects by modulating thrombin activity and anti-inflammatory properties through the inhibition of NF-κB and proinflammatory cytokines. Gabexate mesylate is commonly utilized in research focused on pancreatitis and disseminated intravascular coagulation, making it a valuable reagent for studies in hemostasis and inflammation.

Erdosteine functions as a bacterial inhibitor by inhibiting lipopolysaccharide (LPS)-induced activation of NF-κB. This compound exhibits muco-modulatory, anti-bacterial, anti-inflammatory, and antioxidant properties. Erdosteine is primarily utilized in research applications focused on respiratory disorders and inflammation, supporting the study of therapeutic interventions in these areas.

Isoquercitrin is a potent nitric oxide synthase inhibitor with significant antioxidant and anti-inflammatory properties. This naturally occurring polyphenol exerts protective effects against ethanol-induced hepatotoxicity and oxidative stress, primarily through the activation of the Nrf2/ARE signaling pathway. Additionally, Isoquercitrin modulates the expression of nitric oxide synthase 2 (NOS2) via the nuclear factor-κB (NF-κB) regulatory mechanism. Due to its high bioavailability and low toxicity, Isoquercitrin presents potential applications in research on metabolic disorders and the prevention of birth defects in diabetic pregnancies.

Benzoyloxypaeoniflorin is a potent tyrosinase inhibitor derived from the root of Paeonia suffruticosa, exhibiting an IC50 value of 0.453 mM against mushroom tyrosinase. Additionally, it functions as an NF-κB inhibitor, contributing to enhanced blood circulation by inhibiting platelet aggregation and blood coagulation. This compound is of significant interest in research applications focused on skin disorders and inflammation.

Flaconitine is a potent inhibitor of the NF-κB signaling pathway. This compound has been shown to effectively block the activation of NF-κB, thus modulating inflammatory responses. Flaconitine is widely used in research focused on immunology, cancer biology, and studies involving inflammatory diseases. Its ability to regulate gene expression through NF-κB inhibition makes it a valuable tool for investigating cellular signaling and therapeutic pathways.

Tolterodine is an mAChR inhibitor that competitively binds to acetylcholine, leading to a reduction in sympathetic excitation and inhibition of involuntary bladder muscle contractions. It is known to restore the Nrf2/NF-κB signaling pathway, providing protection against inflammatory responses and ferroptosis. Additionally, Tolterodine mitigates LPS-induced reactive oxygen species production and lipid oxidation, making it valuable for research in urinary tract infections and overactive bladder conditions.

RN-0001 is a potent inhibitor of cyclophilins, specifically demonstrating Ki values of 4.1 nM and 12.0 nM against Cyclophilin A (CypA) and Cyclophilin D (CypD), respectively. By directly binding to CypD, RN-0001 effectively inhibits its peptidyl-prolyl cis-trans isomerase activity, preventing mitochondrial permeability transition pore opening. This compound enhances mitochondrial function, diminishes reactive oxygen species (ROS) production, and downregulates lipogenic marker expression. Additionally, RN-0001 inhibits NF-κB p65 nuclear translocation and reduces the release of activated caspase-3 and cytochrome c, making it a valuable tool for investigating alcohol-associated liver disease.

Rhynchophylline is an alkaloid compound characterized as an NF-κB inhibitor. It exhibits significant biological activity with potential applications in anti-inflammatory and neuroprotective research. This compound is derived from Uncaria rhynchophyllum and is of interest for studies investigating the modulation of inflammatory pathways and neuronal protection mechanisms.