NF-κB

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  1. NLRP3 Inhibitor

    Tabersonine hydrochloride is a selective NLRP3 inhibitor that targets the NACHT domain of the NLRP3 protein, effectively inhibiting its ATPase activity and oligomerization. This action prevents ASC spot formation and caspase-1 activation, leading to a reduction in pro-inflammatory cytokine release, including IL-1β. Additionally, Tabersonine hydrochloride inhibits K63-linked ubiquitination of TRAF6, interfering with NF-κB, PI3K/Akt, and p38 MAPK signaling pathways. Its applications extend to the study of NLRP3-driven inflammatory conditions, such as acute lung injury, sepsis, and peritonitis, as well as in liver cancer research, where it induces apoptosis through mitochondrial and death receptor pathways.
  2. Anti-inflammatory/anti-cancer/anti-viral/anti-tuberculosis Agent

    4-Methoxycinnamic acid ethyl ester is a bioactive natural compound that functions primarily as an anti-inflammatory, anti-cancer, anti-viral, and anti-tuberculosis agent. It demonstrates potent anti-inflammatory activity by inhibiting cyclooxygenases (COX-1 and COX-2) and NF-κB, resulting in reduced cytokine production. Additionally, 4-Methoxycinnamic acid ethyl ester effectively inhibits tumor cell proliferation, migration, and angiogenesis through the downregulation of VEGF expression. It also exhibits significant antiviral properties against dengue virus and antimicrobial activity against Mycobacterium tuberculosis, along with notable analgesic effects in preclinical models.
  3. TNF-α Inhibitor

    TNF-α-IN-11 is a selective inhibitor of tumor necrosis factor alpha (TNF-α) with a dissociation constant (KD) of 12.06 μM. This compound effectively binds to TNF-α, preventing the activation of downstream caspase and NF-κB signaling pathways, as well as inhibiting the phosphorylation of IκBα and the subsequent nuclear translocation of NF-κB p65. TNF-α-IN-11 is suitable for research into TNF-α-mediated autoimmune conditions and the associated inflammatory processes.
  4. TLR4 Agonist

    GlcNAc-MurNAc is a disaccharide that acts as a TLR4 agonist, exhibiting a binding affinity (Kd) of 383 μM for murine TLR4. This compound directly interacts with TLR4, subsequently activating the downstream NF-κB and IRF signaling pathways. Research indicates that GlcNAc-MurNAc ameliorates dextran sulfate sodium salt (DSS)-induced colitis in mice via a TLR4-dependent mechanism, making it a valuable tool for the investigation of inflammatory bowel disease.
  5. COX Inhibitor

    Aspirin lithium is a potent, orally active, irreversible inhibitor of cyclooxygenase COX-1 and COX-2, exhibiting IC50 values of 5 and 210 μg/mL, respectively. This compound promotes apoptosis and inhibits the activation of NF-κB, making it valuable for studies on inflammation and cell death. Additionally, Aspirin lithium effectively inhibits platelet prostaglandin synthetase, providing potential protective effects against coronary artery and cerebrovascular thrombosis.
  6. RIPK2 Inhibitor

    RIPK2-IN-6 is a selective inhibitor of RIPK2, effectively blocking its phosphorylation and subsequently inhibiting the NF-κB and MAPK signaling pathways. This compound exhibits significant anti-inflammatory and anti-fibrotic properties, demonstrated in Dextran sodium sulfate-induced colitis models in mice. RIPK2-IN-6 is valuable in research exploring therapeutic strategies for inflammatory and fibrotic diseases.
  7. Anti-inflammatory Agents

    (±)-Naringenin is an orally bioavailable anti-inflammatory agent that modulates both acute and chronic inflammatory responses. Its biological activities include antioxidant, neuroprotective, hepatoprotective, and potential anti-cancer effects. (±)-Naringenin enhances vasodilation in endothelial cells via the activation of BKCa channels and demonstrates protective effects against experimental colitis by inhibiting the Toll-like receptor 4/NF-κB signaling pathway. This compound is relevant for research applications in sepsis, fulminant hepatitis, fibrosis, and cancer.
  8. Saturated Fatty Acid

    10-Hydroxydecanoic acid (10-HDAA) is a saturated fatty acid that possesses notable anti-inflammatory properties. It exhibits a range of biological activities including anti-malarial, anti-Leishmania, and insecticidal effects, while also enhancing antigen-specific immune responses. Mechanistically, 10-HDAA inhibits NF-κB activation and interferon regulatory factor 1 (IRF-1) translation, leading to reduced levels of interleukin 6 (IL-6) and nitric oxide (NO) in inflammatory cells. Additionally, it plays a role in mitigating neuroinflammatory responses through the p53-autophagy and p53-NLRP3 pathways, making it a valuable reagent for studies in immunology and inflammation research.
  9. Anti-inflammatory/Anti-tumor/Anti-fungal/Neuroprotective Agent

    (+)–Magnoflorine chloride is an aporphine alkaloid that exhibits potent anti-inflammatory, anti-tumor, anti-fungal, and neuroprotective properties. This compound facilitates Parkin/PINK1-mediated mitochondrial autophagy and modulates the NLRP3/Caspase-1 pathway, demonstrating essential immunomodulatory effects. Additionally, it inhibits the JNK and TLR4/NF-κB signaling pathways while activating the Sirt1/AMPK pathway to reduce neuronal oxidative stress and apoptosis. The ability to regulate miR-410-3p and suppress HMGB1/NF-κB signaling further underscores its potential in therapeutic applications across various diseases.
  10. Fatty Acid

    10-Hydroxy-2-decenoic acid (10-HDA) is a bioactive unsaturated medium-chain fatty acid that modulates various physiological processes. It induces reactive oxygen species (ROS)-mediated apoptosis in A549 cells and inhibits VEGF-induced angiogenesis in human venous endothelial cells. Additionally, 10-HDA activates the AMPK-α signaling pathway to alleviate non-alcoholic fatty liver disease (NAFLD) and protects against bone loss by downregulating NF-κB signaling via FFAR4. It also exhibits antimicrobial properties against multiple bacteria and fungi, including Staphylococcus aureus, while demonstrating potential longevity-promoting effects in C. elegans. Furthermore, 10-HDA mitigates osteoarthritis by targeting aspartyl β-hydroxylase to inhibit chondrocyte senescence.
  11. Antibiotic

    Acetoxycycloheximide is an antibiotic with potent antitumor properties, primarily functioning as a protein synthesis inhibitor. It effectively induces procaspase-3 activation, leading to apoptosis through the release of cytochrome c from mitochondria via the JNK signaling pathway. Additionally, acetoxycycloheximide downregulates cell surface TNF-R1 by activating the ERK and p38 MAPK pathways, thereby inhibiting TNF-α-mediated NF-κB signaling. This reagent is valuable for research related to inflammatory and immune diseases as well as cancer.
  12. Cathepsin B Inhibitor

    (Rac)-Z-FA-FMK is a potent inhibitor of cathepsin B, exhibiting a Ki value of 1.5 μM. This compound also inhibits multiple caspases, specifically caspases 2, 3, 6, 7, and 9, with IC50 values ranging from 6.147 to 110.7 μM. Additionally, (Rac)-Z-FA-FMK demonstrates antiviral activity by inhibiting the main protease involved in SARS-CoV-2 replication with an IC50 of 11.39 μM. It further attenuates the increase in IL-1β levels induced by LPS and represses NF-κB transactivation in macrophages, making it useful for research in inflammation and viral pathogenesis.
  13. MDM2 Inhibitor

    LQFM030 is a novel small molecule inhibitor of MDM2, primarily targeting the MDM2-p53 interaction to promote cellular apoptosis. It demonstrates concentration-dependent cytotoxicity in K562 cells with an IC50 value of 0.28 mM, inducing G0/G1 phase cell cycle arrest and enhancing Caspase activity. LQFM030 also downregulates the expression of key oncogenes and proteins, including MDM2, MDMX, p73, MYC, and NF-κB. This compound is particularly valuable in cancer research, especially in the study of leukemia.
  14. Epoxy Diterpene Lactone

    Triptolidenol is an epoxy diterpene lactone derived from the traditional Chinese medicinal plant Tripterygium wilfordii. It exhibits anti-inflammatory and anticancer properties, significantly inhibiting tumor cell proliferation and migration. Triptolidenol induces S phase cell cycle arrest and apoptosis through the activation of the cytochrome c/caspase cascade signaling pathway, while disrupting the NF-κB/COX-2 pathway via IKKβ inhibition at ATP-binding sites. This compound is pertinent for research in chronic nephritis and various forms of kidney cancer, including clear cell renal cell carcinoma (ccRCC).
  15. Hsp90 Inhibitor

    GUT-70 is a tricyclic coumarin that functions as a potent Hsp90 inhibitor. It activates caspases 2, 3, 8, and 9, leading to apoptosis in leukemic cells. Additionally, GUT-70 effectively inhibits HIV-1 replication in chronically infected cells by targeting the NF-κB signaling pathway. This compound is suitable for research applications involving leukemia, mantle cell lymphoma (MCL), and HIV-1 infection studies.
  16. Proteasome Inhibitor

    TP-110 is a selective proteasome inhibitor that targets the protease-like activity of the 20S proteasome, leaving trypsin-like and peptidyl-glutamyl peptide hydrolysis activities unaffected. This compound effectively disrupts the NF-κB signaling pathway, leading to activation of caspases 3, 8, and 9, and subsequent PARP cleavage, while decreasing levels of anti-apoptotic proteins cIAP-1 and XIAP. TP-110 induces G2/M phase cell cycle arrest and promotes apoptosis in cancer cells, making it a valuable tool for researching various malignancies, including prostate cancer and multiple myeloma.
  17. Stable Isotope

    Aspirin-d3 is a deuterium-labeled derivative of aspirin (acetylsalicylic acid) that serves as a stable isotope for research applications. This compound acts as a potent and irreversible inhibitor of cyclooxygenases COX-1 and COX-2, with IC50 values of 5 and 210 μg/mL, respectively. Aspirin-d3 is utilized to investigate its apoptotic effects and to study the inhibition of NF-κB activation. Additionally, it plays a role in exploring the inhibition of platelet prostaglandin synthetase, contributing to research on coronary artery and cerebrovascular thrombosis.
  18. Anti-inflammatory/Anti-tumor/Anti-fungal/Neuroprotective Agent

    (+)-Magnoflorine is an orally active aporphine alkaloid that serves as an anti-inflammatory, anti-tumor, anti-fungal, and neuroprotective agent. It promotes mitochondrial autophagy through Parkin/PINK1 mechanisms and inhibits the NLRP3/caspase-1 signaling pathway, demonstrating significant immunomodulatory effects. Additionally, (+)-Magnoflorine modulates JNK and TLR4/NF-κB pathways, activates Sirt1/AMPK, and alleviates oxidative stress and apoptosis in neuronal cells. Its capacity to upregulate miR-410-3p and inhibit the HMGB1/NF-κB pathway further supports its anti-tumor activity. Furthermore, (+)-Magnoflorine exhibits marked antifungal properties, making it a versatile reagent in chemical research.
  19. PROTAC

    TD1092 is a PROTAC that functions as a pan-IAP degrader, effectively targeting cIAP1, cIAP2, and XIAP. By promoting the degradation of IAPs, TD1092 activates Caspase 3/7, leading to apoptosis in cancer cells. Additionally, it inhibits the TNFα-mediated NF-κB signaling pathway, reducing the phosphorylation of IKK, IkBα, p65, and p38. This compound is primarily used in cancer research to explore mechanisms of apoptosis and therapeutic resistance.
  20. CD206 Targeting Peptide

    RP-182 is a synthetic immunomodulatory peptide that targets the mannose receptor CD206 on tumor-associated macrophages (TAMs), exhibiting a dissociation constant (Kd) of 8 μM. By inducing a conformational change in the CD206 receptor, RP-182 activates NF-κB signaling, promoting TNFα secretion and phagocytosis in CD206high TAMs, ultimately leading to apoptosis via caspase 8 activation. This compound is valuable for research in pancreatic cancer and melanoma, providing insights into therapeutic strategies that enhance anti-tumor immunity.
  21. NLRP3 Inhibitor

    Tabersonine is a selective and orally active inhibitor of the NLRP3 inflammasome, targeting the NACHT domain to modulate its ATPase activity and prevent oligomerization. This mechanism effectively inhibits ASC speck formation and blocks caspase-1 activation, leading to reduced secretion of pro-inflammatory cytokines, including IL-1β. Additionally, Tabersonine interferes with K63-linked ubiquitination of TRAF6, disrupting NF-κB, PI3K/Akt, and p38 MAPK signaling pathways. It is primarily utilized in research on NLRP3-mediated inflammatory diseases, such as acute lung injury, sepsis, and peritonitis, as well as in studies related to liver cancer.
  22. Anti-inflammatory Agent

    Kamebakaurin is an orally active diterpenoid that functions as an anti-inflammatory agent by inhibiting NF-κB activation through direct interference with the DNA-binding activity of p50. This compound exhibits significant biological activity, including the induction of apoptosis and cell cycle arrest in tumor cells. Kamebakaurin is relevant for research applications focused on inflammation and cancer therapeutics.
  23. NF-κB Agonist

    Berubicin is an NF-κB agonist that serves as a doxorubicin analog with the ability to cross the blood-brain barrier. It effectively inhibits P-glycoprotein and MRP1-mediated efflux, demonstrating significant cytotoxicity against glioblastoma multiforme (GBM) and promoting apoptosis in neuroblastoma cells. Berubicin is valuable for investigating tumors of the nervous system and understanding the role of NF-κB in cancer progression.
  24. DpC

    Iron Chelator

    DpC is a selective iron chelator with significant anticancer properties. It targets key signaling pathways, including JNK and NF-κB, inducing oxidative stress in tumor cells through the formation of redox-active iron and copper complexes. DpC promotes apoptosis by activating caspase 3 and 9 and enhances immune responses by increasing TNF-α levels in the tumor microenvironment. Additionally, it effectively overcomes P-glycoprotein-mediated multidrug resistance and demonstrates broad synergistic effects with various chemotherapeutic agents. This compound is relevant for research into multiple malignancies, such as neuroblastoma, pancreatic, prostate, lung, and breast cancers.
  25. Anti-cancer Agent

    Inotodiol is an anti-cancer agent that activates the p53 signaling pathway while inhibiting matrix metalloproteinases MMP-2 and MMP-9, demonstrating significant antitumor activity in HeLa cancer cells. Additionally, Inotodiol exhibits antioxidant and neuroprotective effects by reducing reactive oxygen species (ROS) generation. It also suppresses MAPK and NF-κB signaling pathways, showcasing anti-inflammatory properties. Inotodiol effectively inhibits TLR-4 mediated TNF-α production, with IC50 values of 0.7 μM and 3.0 μM in bone marrow-derived mast cells (BMMC) and macrophages (BMDM) respectively, while also reducing degranulation in mast cells, indicating potential applications in anti-allergic research. This compound is orally active.
  26. Stable Isotope

    Aspirin-d4 is a deuterium-labeled form of Aspirin (Acetylsalicylic acid), functioning as a stable isotope for various biochemical applications. It acts as a potent and irreversible inhibitor of cyclooxygenase enzymes COX-1 and COX-2, demonstrating IC50 values of 5 and 210 μg/mL, respectively. Aspirin-d4 triggers apoptosis and inhibits NF-κB activation, while also affecting platelet function through the inhibition of prostaglandin synthetase. This reagent is suitable for studies involving inflammation, cardiovascular research, and cellular signaling pathways.
  27. TNFα inhibitor

    Aloeresin G is a chromone glycoside derived from Aloe, demonstrating inhibitory activity against TNFα. It attenuates TNFα-induced NF-κB transcriptional activity, exhibiting an IC50 value of 40.02 μM. This compound is valuable for research focused on inflammatory pathways and the modulation of immune responses.
  28. CMC2.24 (TRB-N0224) is an orally active tricarbonylmethane compound that exhibits antitumor activity in pancreatic cancer models by inhibiting Ras activation and downstream ERK1/2 signaling. It is also a potent inhibitor of zinc-dependent matrix metalloproteinases (MMPs), with IC₅₀ values ranging from 2.0 to 69 μM. Additionally, CMC2.24 has therapeutic potential in osteoarthritis, where it restores cartilage homeostasis and reduces chondrocyte apoptosis through modulation of the NF-κB/HIF-2α pathway.
  29. NF-kB inhibitor

    SM-7368 is a potent NF-κB inhibitor that acts downstream of MAPK p38 activation. It suppresses TNF-α-induced upregulation of MMP-9 and is suitable for research on chemotherapeutic strategies targeting TNF-α-mediated tumor invasion and metastasis.
  30. TLR1/2 agonist

    CU-T12-9 is a specific and potent agonist of the Toll-like receptor 1/2 (TLR1/2) heterodimer, with an EC₅₀ of 52.9 nM in the HEK-Blue hTLR2 SEAP assay. It selectively activates TLR1/2 without affecting TLR2/6 and stimulates both innate and adaptive immune responses. CU-T12-9 signals through the NF-κB pathway, leading to elevated expression of downstream effectors such as TNF-α, IL-10, and iNOS, making it a valuable tool for immunological and inflammatory research.
  31. DK/PI3K/BRD4 Inhibitor

    SRX3177 is a potent triple inhibitor targeting CDK4/6, PI3K, and BRD4, with IC50 values of <2.5 nM for CDK4, 3.3 nM for CDK6, 79 nM for PI3Kα, 83 nM for PI3Kδ, 3.18 μM for PI3Kγ, and 33 nM and 89 nM for BRD4 BD1 and BD2, respectively. It exhibits broad cytotoxic activity against cancer cells while sparing normal epithelial cells, highlighting its potential as a targeted cancer therapeutic with reduced toxicity.
  32. RelB inhibitor

    RS47 is a potent and specific inhibitor of the non-canonical NF-κB signaling pathway, acting by disrupting the binding of RelB to its target DNA with a Kd of 1.1 μM. It effectively inhibits the growth of colorectal cancer (CRC) cells and B lymphomas, making it a valuable research tool for studying and potentially targeting cancers driven by hyperactive non-canonical NF-κB signaling.
  33. SOD mimetic

    MnTBAP chloride is a superoxide dismutase (SOD) mimetic and peroxynitrite scavenger, classified as a manganic porphyrin complex with potent antioxidant properties. It exerts anti-inflammatory effects by upregulating BMPR-II expression and inhibiting NFκB signaling. MnTBAP chloride holds therapeutic potential for research into fibrotic responses in chronic kidney diseases (CKDs).
  34. Osteoclast formation inhibitor

    ABD56 is a bioactive compound that inhibits osteoclast formation and induces osteoclast apoptosis. Its mechanism of action involves suppression of the NFκB and ERK signaling pathways, making it a promising candidate for research in bone metabolism and osteolytic diseases.
  35. PPAR agonist

    Lobeglitazone sulfate is a novel thiazolidinedione and an orally active agonist of peroxisome proliferator-activated receptors (PPARs), with EC50 values of 137.4 nM for PPARγ and 546.3 nM for PPARα. It also acts as an inhibitor of the ERK/JNK/Smad/NF-κB signaling pathways. Lobeglitazone sulfate exhibits anti-inflammatory, anti-diabetic, anti-fibrotic, and anti-atherosclerotic activities, supporting its potential in the treatment of metabolic and inflammatory diseases.
  36. Endoplasmic Reticulum Stress Inhibitor

    Tauroursodeoxycholate (Tauroursodeoxycholic acid; TDUCA) dihydrate is an inhibitor of endoplasmic reticulum (ER) stress that significantly downregulates pro-apoptotic molecules, including caspase-3 and caspase-12. Additionally, it suppresses ERK signaling, contributing to its cytoprotective and anti-apoptotic effects.
  37. NF-κB inhibitor

    Asperulosidic Acid (ASPA) is a bioactive iridoid glycoside isolated from the herb Hedyotis diffusa Willd., exhibiting anti-tumor, antioxidant, and anti-inflammatory properties. Its anti-inflammatory effects are associated with the downregulation of proinflammatory cytokines such as TNF-α and IL-6, mediated through inhibition of the NF-κB and MAPK signaling pathways.
  38. Apoptosis activator

    Sulforaphene, a natural compound isolated from radish seeds, exhibits an ED₅₀ of approximately 2 × 10⁻⁴ M against velvetleaf seedlings. It promotes apoptosis and inhibits migration in cancer cells by suppressing signaling pathways including EGFR, phosphorylated ERK1/2 (p-ERK1/2), and NF-κB.
  39. NF-κB/FAK/MAPK inhibitor

    Keracyanin chloride is an orally active anthocyanin compound with potent antioxidant, anti-inflammatory, and hypoglycemic properties. It exerts its biological effects by inhibiting the NF-κB/FAK/MAPK signaling pathways, which are central to inflammation, cell adhesion, and metabolic regulation.
  40. Anticholinergic agent

    Penehyclidine hydrochloride (also known as Penequinine hydrochloride) is a selective anticholinergic agent that acts as an antagonist of muscarinic M1 and M3 receptors. It exerts anti-inflammatory effects by modulating immune signaling in lung tissue, notably through activation of the NF-κB pathway and inhibition of pro-inflammatory cytokine release. In preclinical studies, Penehyclidine hydrochloride has been shown to alleviate pulmonary inflammation in rat models of chronic obstructive pulmonary disease (COPD), particularly under conditions of mechanical ventilation. These properties suggest its potential utility in managing respiratory inflammatory conditions and improving outcomes in mechanically ventilated patients with COPD.
  41. PPAR agonist

    Lobeglitazone is a novel thiazolidinedione-class compound and an orally active dual agonist of peroxisome proliferator-activated receptors (PPARs), with EC₅₀ values of 137.4 nM for PPARγ and 546.3 nM for PPARα. In addition to its metabolic effects, Lobeglitazone functions as an inhibitor of multiple pro-inflammatory and pro-fibrotic signaling pathways, including ERK, JNK, Smad, and NF-κB. Lobeglitazone exhibits a broad range of pharmacological activities, including anti-inflammatory, anti-diabetic, anti-fibrotic, and anti-atherosclerotic effects. These properties make it a promising candidate for therapeutic research in metabolic syndrome, type 2 diabetes, cardiovascular disease, and fibrosis-related conditions.
  42. ACAT inhibitor

    Enniatin B1 is a mycotoxin produced by Fusarium species, known for its diverse bioactivities. It functions as a moderate inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT), with an IC₅₀ of 73 μM in assays using rat liver microsomes, implicating a role in lipid metabolism modulation. Enniatin B1 is capable of crossing the blood-brain barrier, suggesting potential effects on central nervous system function. It also decreases the activation of ERK1/2 (p44/p42 MAPK) and moderately inhibits TNF-α-induced NF-κB activation, indicating anti-inflammatory and cell signaling modulatory properties.
  43. Anti-inflammatory agent 35 (compound 5a27) is an orally active curcumin analogue that exhibits potent anti-inflammatory activity. It exerts its effects by blocking mitogen-activated protein kinase (MAPK) signaling and inhibiting the nuclear translocation of the NF-κB subunit p65, thereby suppressing key inflammatory pathways. Additionally, compound 5a27 reduces neutrophil infiltration and the production of pro-inflammatory cytokines. In vivo, it significantly attenuates lipopolysaccharide (LPS)-induced acute lung injury (ALI), highlighting its potential as a therapeutic candidate for inflammatory and respiratory disorders.
  44. Endogenous Metabolite

    Gamma-linolenic acid (γ-linolenic acid, GLA) is an orally active omega-6 unsaturated fatty acid with broad pharmacological activities. It exhibits anti-inflammatory effects by inhibiting the NF-κB signaling pathway and suppressing the phosphorylation of ERK1/2 and JNK, key mediators of inflammatory responses. GLA also induces apoptosis in cancer cells, contributing to its anticancer potential. Additionally, it possesses antioxidant properties and has been shown to improve memory function, suggesting neuroprotective benefits. These multifunctional effects position gamma-linolenic acid as a promising compound for research in inflammation, oncology, and neurological disorders.
  45. PDE4/NF-κB inhibitor

    Sappanone A is an orally active homoisoflavone isolated from Caesalpinia sappan L., exhibiting notable anti-inflammatory and antioxidant properties. It functions as an inhibitor of phosphodiesterase 4 (PDE4) and NF-κB, key regulators of inflammatory signaling. Additionally, Sappanone A activates the Nrf2 pathway, leading to increased expression of the cytoprotective enzyme heme oxygenase-1 (HO-1). Sappanone A also inhibits RANKL-induced osteoclastogenesis, suggesting potential benefits in bone metabolism disorders. With its multifaceted bioactivity, Sappanone A holds significant promise for research in inflammation-related diseases, cardiovascular conditions, and bone health.
  46. NF-kB inhibitor

    EF24 is a synthetic curcumin analogue and a potent NF-κB inhibitor with demonstrated oral bioavailability and strong antitumor activity. It exerts its anticancer effects, particularly in oral squamous cell carcinoma (OSCC), through deactivation of the MAPK/ERK signaling pathway. EF24 is effective against various cancer cell lines, with GI₅₀ values of 0.7 μM in melanoma and 0.8 μM in breast cancer cells. In MDA-MB-231 (breast cancer) and DU-145 (prostate cancer) cells, EF24 induces cell cycle arrest and apoptosis, accompanied by increased activation of caspase-3 and caspase-9. It also reduces the phosphorylation of MEK1 and ERK, further contributing to its pro-apoptotic and anti-proliferative effects. These properties make EF24 a promising compound for cancer therapy research.
  47. Microglial inhibitor

    Inflachromene is a microglial inhibitor that exerts anti-inflammatory effects by directly binding to high mobility group box proteins HMGB1 and HMGB2. Through this interaction, it effectively downregulates the proinflammatory activities of HMGB proteins, leading to reduced microglial activation and neuronal damage. Inflachromene holds promise as a therapeutic candidate for the treatment of neuroinflammatory disorders, including neurodegenerative diseases and central nervous system injuries.
  48. Gypenoside L is a bioactive saponin isolated from *Gynostemma pentaphyllum*, known for its diverse pharmacological properties. It induces cellular senescence by increasing senescence-associated β-galactosidase (SA-β-gal) activity and promoting the secretion of senescence-associated secretory phenotype (SASP) cytokines. Mechanistically, Gypenoside L activates the p38 and ERK MAPK pathways as well as the NF-κB signaling pathway to trigger senescence. In addition to its pro-senescent effects, Gypenoside L exhibits notable anti-tumor and anti-inflammatory activities, making it a promising compound for research in cancer biology and inflammation-related diseases.
  49. NF-κB p65 Inhibitor

    Licochalcone D is a naturally occurring flavonoid primarily found in the root of *Glycyrrhiza uralensis* (Chinese licorice). It functions as a potent and orally active inhibitor of the NF-κB p65 subunit, a key regulator of inflammation and cancer-related signaling pathways. Licochalcone D exhibits broad pharmacological properties, including antioxidant, anti-inflammatory, and anticancer activities, making it a promising candidate for research in inflammation-related diseases and oncology.
  50. Anti-inflammatory Agent

    Berkeleyacetal C is a meroterpenoid compound that acts as an anti-inflammatory agent by inhibiting the NF-κB, ERK1/2, and IRF3 signaling pathways. It effectively reduces the expression of inducible nitric oxide synthase (iNOS) and subsequent nitric oxide production in macrophages. Additionally, Berkeleyacetal C suppresses the expression and secretion of key pro-inflammatory cytokines and chemokines, including TNF-α, IL-6, IL-1β, MIP-1α, and MCP-1, while also inhibiting neutrophil activation and reactive oxygen species (ROS) production. This compound is valuable for research into inflammatory disorders.

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