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Catalog No.
Product Name
Application
Product Information
Citations
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NF-κB inhibitor
QNZ inhibits the activation of the transcription factor NF-κB and has been used to investigate NF-κB signaling.- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
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NF-kB inhibitor
Withaferin A is a steroidal lactone present in W. somnifera that at 2-25 μM has been shown to bind to and induce aggregation of vimentin intermediate filaments in cultured endothelial cells and fibroblasts, causing apoptosis.- Chang-Mu Chen, .et al. , Phytomedicine, 2020, Dec;79:153352 PMID: 33007732
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NF-κB inhibitor
JSH 23 is an inhibitor of NF-kB, blocking its translocation into the nucleus (IC50 = 7.1 uM)- Yu N, .et al. , Radiat Res, 2018, Apr;189(4):409-417 PMID: 29420126
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NF-κB inhibitor
SC75741 is a potent NF-kB inhibitor with EC50 of 200 nM.- Yunshang Yang, .et al. , Biomed Pharmacother, 2023, Feb;158:114113 PMID: 36516692
- Yajun Li, .et al. , Cell Prolif, 2022, Oct;55(10) PMID: 35708050
- Crystal A Mendoza, .et al. , Antiviral Res, 2021, Jan;185:104993 PMID: 33296695
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NF-kB inhibitor/Proteasome activator
18α-Glycyrrhetinic acid (18α-GA) is a bioactive triterpenoid found in licorice. It shows selective inhibition of 11-HSD1 (11-hydroxysteroid dehydrogenase 1). -
NF-κB activation inhibitor
Caffeic acid phenethyl ester is a potent and specific inhibitor of NF-κB activation -
ERK/Akt/NF-kB inhibitor
Tomatidine inhibits the phosphorylation of ERK, Akt, and the nuclear content of NF-kB. possess anti-inflammatory properties. -
NF-kB inhibitor
Pyrrolidinedithiocarbamate ammonium is a selective NF-kB inhibitor, inhibits translation of nitric oxide synthase mRNA to prevent induction. -
p53 activator / NF-κB inhibitor
CBL0137 hydrochloride activates p53 and inhibits NF-kB with EC50s of 0.37 μM and 0.47 μM in the cell-based p53 and NF-kB reporter assays, respectively. It also inhibits histone chaperone FACT (facilitates chromatin transcription complex).
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NF-κB inhibitor
Cyclo(his-pro) (Cyclo(histidyl-proline)) is an orally active cyclic dipeptide structurally related to tyreotropin-releasing hormone. Cyclo(his-pro) could inhibit NF-κB nuclear accumulation. -
NF-κB inhibitor
WAY-204688 is an estrogen receptor (ER-α) selective, orally active inhibitor of NF-κB transcriptional activity with an IC50 of 122?±?30 nM for NF-κB-luciferase (NF-κB-luc) in HAECT-1 cells. -
NF-κB inhibitor
Edasalonexent (CAT-1004) is an orally bioavailable NF-κB inhibitor. -
NF-κB inhibitor
DMAPT (Dimethylamino Parthenolide), a water soluble analogue of Parthenolide (PTL), is an oral active NF-κB inhibitor, with a LD50 of 1.7 μM for cell population in AML cells. Has potential anti-cancer and anti-metastatic effect. -
NF-κB inhibitor
DHMEQ racemate is a NF-κB inhibitor. DHMEQ racemate is less active than (-)-DHMEQ. -
Smurf1 inhibitor
Smurf1-IN-A01 (A01) is an ubiquitin ligase Smad ubiquitination regulatory factor-1 (Smurf1) inhibitor with a kd of 3.664 nM, which increases BMP-2 responsiveness by inhibiting Smurf1-mediated Smad1/5 degradation. -
NF-κB inhibitor
CID-2858522 selectively inhibits the NF-κB pathway (IC50 < 0.1 uM for PMA-stimulated IL-8 production) induced by PKC, operating downstream of PKC but upstream of IKKbeta, without inhibiting other NF-kappaB activation pathways. -
NF-κB Inhibitor
Dendrophenol is a potent NF-κB inhibitor known for its ability to suppress inflammatory responses. This compound exhibits significant cytotoxic effects against tumor cells, promoting cell cycle arrest and apoptosis, thereby demonstrating antitumor activity. Furthermore, Dendrophenol has been shown to inhibit vascular calcification through the suppression of WNT3/β-catenin activation, making it a valuable tool for research in cancer and vascular biology. -
NF-κB Expression Reducer, ERK 1/2 Activator, Beta-Adrenergic Receptor Modulator, Calcium Channel Inhibitor
Eupatorin is a flavonoid that functions primarily as an NF-κB expression reducer and an ERK 1/2 activator, while also modulating beta-adrenergic receptors and inhibiting calcium channels. It demonstrates significant antiproliferative and vasodilatory effects, inducing apoptosis and causing G2/M phase cell cycle arrest, alongside reactive oxygen species (ROS) production. Eupatorin has been shown to impact inflammatory mediators and calcium signaling pathways, making it relevant for research in breast cancer, hypertension, and leukemia. Metabolized by CYP1A1 and other CYP1 enzymes, Eupatorin yields bioactive metabolites that maintain antiproliferative properties. -
MALT1 Inhibitor
SGR-1505 is a small molecule inhibitor targeting MALT1, effectively modulating the NF-κB signaling pathway. This compound demonstrates significant anti-proliferative and antitumor activities by inhibiting MALT1 enzymatic activity, leading to alterations in cell cycle progression, DNA damage response, and apoptosis-related gene expression in in vivo tumor models. SGR-1505 exhibits both tumorostatic and regressive effects in activated B cell-like diffuse large B cell lymphoma (ABC-DLBCL) xenograft models. It is a valuable tool for research into activated B-cell-like diffuse large B-cell lymphoma, non-Hodgkin B-cell lymphomas, chronic lymphocytic leukemia, and mature B cell neoplasms. -
AKR1C1/JAK2/STAT3/NF-κB Inhibitor
Zingiberen Newsaponin is a potent inhibitor of the AKR1C1/JAK2/STAT3 and NF-κB signaling pathways. This steroid saponin compound demonstrates significant anti-hepatocellular carcinoma (HCC) activity by promoting cancer cell apoptosis through the induction of oxidative stress, as evidenced by the upregulation of ROS and MDA levels. Additionally, Zingiberen Newsaponin mitigates cerebral ischemia-reperfusion injury by reducing pro-inflammatory cytokines and enhancing superoxide dismutase (SOD) activity, thereby protecting neuronal cells. Furthermore, it has been shown to induce platelet aggregation, broadening its application in cardiovascular research. -
JAK2/STAT3/NF-κB Inhibitor
Reticuline acts as a JAK2/STAT3 and NF-κB signaling pathway inhibitor, displaying notable anti-inflammatory properties. It effectively downregulates the mRNA expression of pro-inflammatory cytokines such as TNF-α and IL-6 while also reducing the phosphorylation levels of JAK2 and STAT3. Additionally, Reticuline demonstrates potential cardiovascular effects, making it a valuable tool for research in inflammation and cardiovascular studies. -
JAK/STAT and NF-κB Inhibitor
JAK-IN-23 is a potent dual inhibitor of the JAK/STAT and NF-κB signaling pathways, targeting JAK1, JAK2, and JAK3 with IC50 values of 8.9 nM, 15 nM, and 46.2 nM, respectively. This compound effectively modulates the expression of interferon-stimulated genes (ISG) and inhibits NF-κB activation, exhibiting IC50 values of 3.3 nM and 150.7 nM, respectively. JAK-IN-23 demonstrates significant anti-inflammatory properties by reducing the release of various pro-inflammatory cytokines. Its applications include research into inflammatory bowel disease (IBD) and other related inflammatory conditions. -
IRAK4/IRAK1 Inhibitor
IRAK4 modulator-2 is a selective inhibitor of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) and IRAK1, exhibiting IC50 values of 0.005 μM and 0.97 μM, respectively. This compound effectively disrupts IRAK-mediated signaling pathways, including JAK-STAT and NF-κB pathways, leading to a reduction in pro-inflammatory cytokine production, such as IL-1 and TNF. IRAK4 modulator-2 demonstrates potential for use in research focusing on autoimmune and inflammatory diseases, including rheumatoid arthritis, psoriasis, and inflammatory bowel disease. -
Cathepsin L/JAK Inhibitor
Dual Cathepsin L/JAK-IN-1 is a dual inhibitor targeting Cathepsin L (CTSL) and Janus kinases (JAK), exhibiting IC50 values of 0.68 μM for CTSL, 337.1 nM for JAK1, 5.251 nM for JAK2, 27.29 nM for JAK3, and 172.6 nM for TYK2. This compound effectively inhibits the activation of key signaling pathways, including MAPK, NF-κB, and JAK/STAT, thereby providing substantial anti-inflammatory effects. Dual Cathepsin L/JAK-IN-1 is useful for investigating mechanisms underlying acute lung injury (ALI) and other inflammatory conditions. -
IKKβ/JAK2 Inhibitor
EC-70124 is an orally active multikinase inhibitor that targets IKKβ and JAK2. By blocking IkB phosphorylation and the activation of STAT3 (Tyr705), EC-70124 inhibits NF-κB nuclear translocation and impedes STAT3 transcriptional activity. This compound has demonstrated the ability to reduce tumor growth and diminish cancer stem cell populations in prostate cancer cells and xenograft models, making it a valuable tool for research in prostate cancer. -
IKKε Inhibitor
IKKε-IN-1 is a selective inhibitor of IKKε, a key enzyme involved in the NF-κB signaling pathway. This compound effectively reduces cell viability, inhibits colony formation, and diminishes cell migration in various cancer cell lines. Additionally, IKKε-IN-1 induces autophagy, illustrating its potential as a research tool in the study of multiple cancer types, including colorectal, hepatocellular, bladder, breast, lung, and cervical cancers. -
Carnitine Palmitoyltransferase I Upregulator, Peroxisome Proliferator-Activated Receptor α Upregulator, Nuclear Factor Erythroid 2-Related Factor 2 Activator, Nuclear Factor-Kappa B Inhibitor, Nuclear Factor Kappa B Kinase Subunit Beta Inhibitor, Sterol Regulatory Element-Binding Protein 1 Downregulator, Acetyl-CoA Carboxylase Downregulator, Acyl-CoA:Cholesterol Acyl Transferase 1 Inhibitor, Acyl-CoA:Cholesterol Acyl Transferase 2 Inhibitor
Esculeogenin A is a potent upregulator of Carnitine Palmitoyltransferase I and Peroxisome Proliferator-Activated Receptor α, while also acting as an activator of Nuclear Factor Erythroid 2-Related Factor 2. This compound exhibits key biological activities, including hepatoprotective, hypolipidemic, and antioxidant effects. Esculeogenin A modulates essential molecular targets such as SREBP1, NF-κB, and ACAT1/ACAT2, leading to enhanced hepatic fatty acid oxidation and diminished inflammation. It is applicable in research focused on nonalcoholic fatty liver disease, atherosclerosis, and hyperlipidemia, showcasing its potential to improve liver function and mitigate the risk of associated metabolic disorders. -
COX-2 Inhibitor/PPAR-γ Activator
Zaltoprofen sulfoxide is a selective COX-2 inhibitor with an IC50 of 45.38 nM, as well as a PPAR-γ activator. This compound effectively inhibits NF-κB and MAPK inflammatory signaling pathways, making it a valuable tool in the study of inflammation and acute lung injury models. It is particularly relevant for research focused on LPS-induced acute lung injury. -
TrxR1 Inhibitor
Aurothioglucose is a potent inhibitor of thioredoxin reductase 1 (TrxR1), exhibiting an IC50 value of 65 nM. This compound effectively inhibits the DNA binding activity of NF-κB in vitro, highlighting its role in modulating key transcriptional pathways. Additionally, Aurothioglucose demonstrates anti-HIV and anti-rheumatic properties, making it a valuable reagent for research in infectious diseases and autoimmune disorders. -
ROS Inhibitor
Isodeoxyelephantopin is a sesquiterpene lactone with a primary mechanism as a reactive oxygen species (ROS) inhibitor. It demonstrates significant biological activity by inducing ROS generation and suppressing NF-κB activation, thereby contributing to its anticancer properties. Additionally, Isodeoxyelephantopin modulates long non-coding RNA (LncRNA) expression, making it a valuable reagent for breast cancer research and related fields. -
IKKβ Inhibitor
IKKβ-IN-7 is a selective inhibitor of IKKβ, exhibiting an IC50 value of 9.44 μM. This compound induces DNA damage, S-phase cell cycle arrest, and apoptosis, while also promoting reactive oxygen species accumulation and loss of mitochondrial membrane potential. By inhibiting the phosphorylation of p65 and IκBα, IKKβ-IN-7 effectively restricts p65 nuclear translocation and modulates NF-κB-regulated gene expression. This agent demonstrates significant antitumor activity in xenograft models, particularly in colorectal cancer, while exhibiting low cytotoxicity in normal cells. IKKβ-IN-7 serves as a valuable tool for research in the field of colorectal cancer. -
GADD45β/MKK7 Inhibitor
DTP3 TFA is a highly selective inhibitor of GADD45β/MKK7, targeting a critical pathway involved in cell survival in cancer cells downstream of the NF-κB signaling cascade. This compound exert biological activity by disrupting the function of the GADD45β/MKK7 module, influencing cellular responses to DNA damage and stress. DTP3 TFA serves as a valuable tool in cancer research, particularly in studies investigating the mechanisms of cell survival and the potential for therapeutic interventions in malignancies associated with aberrant NF-κB activity. -
Inflammation Inhibitor
Resolvin D5 is an anti-inflammatory agent primarily targeting the GPR32 receptor, effectively modulating inflammation responses. It alleviates Paclitaxel-induced mechanical allodynia and inflammatory pain in male mice through mechanisms that do not involve TRPV1 or TRPA1 channels. Resolvin D5 reduces LPS-induced ERK phosphorylation and NF-κB nuclear translocation while downregulating pro-inflammatory mediators, inhibiting Th17 differentiation, and promoting regulatory T cell differentiation. This compound is particularly relevant for research on chemotherapy-induced peripheral neuropathy, inflammatory pain, and rheumatoid arthritis. -
NF-κB&ERK1/2 Inhibitor
OP-1118 is a potent dual inhibitor of NF-κB and ERK1/2, targeting critical signaling pathways involved in inflammation and cell survival. This compound demonstrates significant anti-inflammatory, cytoprotective, anti-apoptotic, and antibacterial activities by inhibiting the phosphorylation of NF-κB and ERK1/2, leading to a reduction in pro-inflammatory cytokine expression. In preclinical models of Clostridium difficile infection, OP-1118 effectively mitigates toxin-induced intestinal inflammation, cellular damage, and apoptosis, with its protective effects possibly reversible by PMA. This makes OP-1118 a valuable reagent for research into inflammatory conditions and therapeutic interventions. -
Syk Inhibitor, NF-κB p65 Inhibitor, TGF-β1/Smad Signaling Inhibitor
Flavanomarein is a potent inhibitor of Syk and NF-κB p65, as well as a modulator of TGF-β1/Smad signaling pathways. This compound exhibits cytoprotective, anti-inflammatory, and antioxidant activities, enhancing AKT phosphorylation while regulating key proteins such as PKC-δ, P85α, PKC-β1, Sirt1, Bcl-2, and ICAD. Flavanomarein also inhibits the nuclear translocation of NF-κB p65 and modulates epithelial-mesenchymal transition (EMT) markers, promoting proliferation in HK-2 cells and protecting neuronal cells from 6-OHDA-induced neurotoxicity. This compound is valuable for research on Parkinson's disease and diabetic nephropathy. -
NF-κB Inhibitor/TRP Modulator
Cannabitwinol is a selective NF-κB inhibitor and thermosensitive TRP modulator. It effectively inhibits TNFα-induced NF-κB-driven transcription and IL-8 release, exhibiting notable anti-inflammatory and antioxidant properties. Cannabitwinol selectively activates cold-activated TRP channels, such as TRPA1 (EC50 = 3.0 μM), while antagonizing TRPM8 (IC50 = 3.9 μM), with minimal interaction with heat-activated TRP channels like TRPV1 and TRPV2. This compound is applicable in research focused on inflammatory skin diseases, cold allodynia, and hyperalgesia. -
NF-κB Inhibitor
Bengamide B is a potent inhibitor of NF-κB with an IC50 of 85 nM. This compound effectively reduces LPS-induced expression of pro-inflammatory cytokines, including TNF-α, IL-6, and MCP-1, demonstrating significant anti-inflammatory activity. Additionally, Bengamide B displays antitumor efficacy, with an IC50 of 2 nM against HCT-116 colorectal cancer cells, making it a valuable reagent for research in inflammation and oncology. -
SEAP Inhibitor
Cycloepoxydon is a potent inhibitor of secreted alkaline phosphatase (SEAP) expression, targeting both NF-κB and AP-1 signaling pathways. It effectively reduces PMA-induced SEAP expression with IC50 values ranging from 1-2 μg/mL (4.2-8.4 μM) for NF-κB and 3-5 μg/mL (12.6-21 μM) for AP-1. This compound is valuable for research applications involving inflammation, cancer biology, and signal transduction studies. -
NF-κB Inhibitor
2,4,5-Trimethoxybenzoic acid is an NF-κB inhibitor with notable anti-inflammatory properties. This compound, derived from purple perilla extracts, effectively inhibits LPS-induced inflammatory responses by blocking the activation of NF-κB and STAT signaling pathways. It has been shown to suppress M1 macrophage phenotype-mediated inflammation, making it a valuable tool for research into diabetes and related inflammatory conditions. -
S100P Inhibitor
5-Methyl cromolyn disodium is a selective inhibitor of the S100P protein, targeting its interaction with the receptor for advanced glycation end-products (RAGE). It effectively suppresses NF-κB activity and cell proliferation while enhancing Gemcitabine-induced apoptosis. In preclinical mouse models, 5-Methyl cromolyn disodium demonstrates significant anti-tumor effects by reducing growth and metastasis of pancreatic ductal adenocarcinoma (PDAC), ultimately extending survival. This compound serves as a valuable tool for investigating pancreatic cancer mechanisms and potential therapeutic approaches. -
NF-κB Inhibitor
NF-κB-IN-5 is a potent inhibitor of nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) that acts by directly interacting with the NF-κB complex. This compound demonstrates significant antitumor activity across multiple human cancer cell lines, including HCT116, U87-MG, HepG2, BGC823, and PC9, with IC50 values ranging from 2.02 to 5.35 μM. NF-κB-IN-5 also promotes apoptosis in U87-MG cells and induces cell cycle arrest in the G0/G1 phase, positioning it as a valuable tool for cancer research and therapeutic development. -
c-Myc Inhibitor
EP12 is a selective c-Myc inhibitor that stabilizes c-Myc G-quadruplexes. This compound induces apoptosis and causes DNA damage in multiple myeloma cells, effectively inhibiting their growth. Additionally, EP12 disrupts the nuclear translocation of P65/P50 by interfering with the NF-κB signaling pathway, highlighting its potential in cancer research and therapeutic applications. -
IRAK4 Inhibitor
Emavusertib phosphate is a potent inhibitor of IRAK4, exhibiting an IC50 of 57 nM. This compound effectively disrupts NF-κB and MyD88 signaling pathways, leading to a significant reduction in pro-inflammatory cytokines such as IL-6 and IL-10. Emavusertib phosphate demonstrates both anti-inflammatory and anti-proliferative effects on cancer cells, promoting apoptosis and showcasing antitumor activity in preclinical mouse models. Its applications extend to investigating inflammatory diseases and cancer therapies.
