Catalog No.
Product Name
Application
Product Information
Citations
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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. -
P2Y12 Receptor Activator
ADP-β-S trilithium is the trilithium salt form of ADP-β-S, serving as a potent activator of the P2Y12 receptor. It facilitates the upregulation of IL-1β and IL-6 production in microglial cells, promotes NF-κB phosphorylation and nuclear translocation, and enhances NLRP3 inflammasome activation. This reagent is valuable for research into inflammatory responses and signaling pathways involving P2Y12 receptor activation. -
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. -
Active Compound
(-)-Camphoric acid is an active compound known to modulate glutamate receptor expression. It significantly stimulates the activation of key transcription factors NF-κB and AP-1. This compound has been shown to promote the differentiation of mouse osteoblastic MC3T3-E1 cells, highlighting its potential in osteogenesis research. Additionally, (-)-Camphoric acid can induce the mRNA expression of glutamate signaling molecules, further supporting its role in osteoblast differentiation and related biological pathways. -
Anti-inflammatory Agent
11-Keto-beta-boswellic acid is a pentacyclic triterpenic acid derived from the oleogum resin of the Boswellia serrata tree, commonly known as Indian Frankincense. This compound exhibits significant anti-inflammatory activity through the inhibition of 5-lipoxygenase (5-LOX), which subsequently reduces leukotriene synthesis and attenuates nuclear factor-kappa B (NF-κB) activation, along with the production of tumor necrosis factor alpha. Due to its mechanism of action, 11-Keto-beta-boswellic acid is of interest in studies focused on inflammation-related conditions. -
CysLt1 Antagonist
Q8 is a potent CysLt1 antagonist with an IC50 of 4.9 μM. This compound effectively inhibits angiogenesis by reducing cellular levels of NF-κB and calpain-2. Additionally, Q8 decreases the secretion of proangiogenic proteins such as intercellular adhesion molecule-1, vascular cell adhesion protein-1, and VEGF, making it valuable for research in cancer and vascular biology. -
Stable Isotope
Tolterodine-d14 hydrochloride is a deuterium-labeled version of Tolterodine hydrochloride, a potent muscarinic acetylcholine receptor (mAChR) inhibitor. This compound competitively binds to acetylcholine, thereby reducing involuntary bladder muscle contractions and modulating sympathetic nervous activity. In addition to its role in managing overactive bladder and urinary tract infections, Tolterodine has been shown to restore the Nrf2/NF-κB signaling pathway, offering protective effects against inflammation and ferroptosis. Its applications extend to studies involving reactive oxygen species and lipid oxidation. -
NF-κB Inhibitor
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. -
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. -
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. -
Sigma-2 ligand/Agonist
SW43 is a selective Sigma-2 ligand and agonist that plays a pivotal role in cancer research. This compound enhances the development of targeted therapeutic agents, showing significant antitumor activity when conjugated with DOX-L-NETA (89Y) in a VX2 liver tumor allograft rabbit model. Additionally, when combined with SW IV-52s to create SW III-123, SW43 activates the NF-κB pathway, demonstrating potent cytotoxic effects against ovarian cancer cell lines and promoting apoptosis. This dual functionality underscores its utility in cancer therapeutic development. -
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. -
Negative control of IKK
6-Chloro-7-deazaguanine serves as a negative control for IκB kinase (IKK), specifically lacking the essential 5-cyano group that defines its activity. As an inactive analog, it provides a useful reference for studying the IKKβ and IKKα pathways, which are crucial components of the canonical and non-canonical NF-κB signaling pathways. Researchers can utilize this compound to delineate the role of IKK in various cellular processes and disease models, particularly in inflammation and immune responses. -
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. -
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. -
Vasodilator
(Z)-11,12-Epoxyeicosatrienoic acid acts as a potent vasodilator, primarily targeting small renal arteries. This compound exhibits anti-inflammatory properties by inhibiting leukocyte adhesion to the vascular wall through modulation of the NF-κB signaling pathway and IκB kinase (IKK) activity. It is suitable for research applications focused on vascular inflammation and related cardiovascular studies. -
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. -
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.
