NF-κB/IκB

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  1. GRPR Antagonist

    Aurantiamide is a selective antagonist of the Gastrin-Releasing Peptide Receptor (GRPR), demonstrating significant anti-inflammatory and neuroprotective properties. It effectively mitigates inflammation and oxidative stress in renal tissues by targeting GRPR-mediated pathways, including RIPK3/MLKL signaling and NF-κB activation, thereby providing protection against acute kidney injury and promoting endothelial function. Additionally, Aurantiamide inhibits M1 microglial polarization and NLRP3 activation, showcasing efficacy in improving outcomes in Alzheimer's disease mouse models. Its notable in vivo effectiveness extends to various acute kidney injury contexts, including ischemia/reperfusion, sepsis, and hypertension models.
  2. RIPK1 PROTAC Degrader

    LD4172 is a selective RIPK1 PROTAC degrader that exhibits a Ki of 4.8 nM. It facilitates RIPK1 protein degradation through the formation of a ternary complex with RIPK1 and VHL E3 ligase, leading to ubiquitination and proteasomal degradation. LD4172 effectively inhibits TNF-induced classical NF-κB signaling in TRAF2-deficient cells, significantly reducing IκBα phosphorylation and IL-8 production. Additionally, it promotes apoptosis and immunogenic cell death in tumor cells, enhances tumor-infiltrating lymphocyte responses, and sensitizes tumors to anti-PD1 therapy, making it a valuable chemical probe for studying RIPK1-related functions in melanoma and colon cancer research.
  3. 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.
  4. 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.
  5. 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.
  6. HDAC3 Inhibitor

    HDAC3-IN-2 is a potent inhibitor of histone deacetylase 3 (HDAC3), with an IC50 value of 14 nM. This pyrazinyl hydrazide compound exhibits cytotoxicity against triple-negative breast cancer cell lines, demonstrating an IC50 of 0.55 μM for 4T1 cells and 0.74 μM for MDA-MB-231 cells. In in vivo studies using tumor-bearing mouse models, HDAC3-IN-2 effectively enhances histone acetylation levels at H3K9, H3K27, and H4K12 while promoting apoptosis through increased caspase-3, caspase-7, and cytochrome c levels, alongside a decrease in proliferation markers such as Bcl-2, CD44, EGFR, and Ki-67.
  7. 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.
  8. 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.
  9. PROTAC IKKβ/NR4A1 Degrader

    PROTAC IKKβ/NR4A1 degrader-1 is a novel dual-PROTAC degrader designed to selectively target and degrade IKKβ and NR4A1, utilizing the E3 ligase cereblon. This compound effectively increases the levels of caspase 3 and cleaved caspase 3 proteins, indicating a potential to induce apoptosis without affecting the necroptosis marker RIP kinase. It is a valuable tool for investigating the mechanisms underlying Acute Myeloid Leukemia (AML) and offers insights into therapeutic strategies targeting these pathways.
  10. 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.
  11. 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.
  12. 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.
  13. 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.
  14. 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.
  15. 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.
  16. 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.
  17. 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.
  18. 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).
  19. 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.
  20. 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.
  21. HDAC1/6 Inhibitor

    HDAC1/6-IN-3 is a potent inhibitor of histone deacetylases 1 and 6 (HDAC1 and HDAC6). It demonstrates strong inhibitory activity, with IC50 values of 1.1 nM for HDAC1 and 2.7 nM for HDAC6. This compound effectively induces cell cycle arrest in the G0/G1 phase and promotes both apoptosis and pyroptosis in HepG2 cells. Additionally, HDAC1/6-IN-3 exhibits significant antitumor effects in the HepG2 xenograft model and is valuable for research focused on various types of cancer, including liver, lung, colon, and breast cancers.
  22. 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.
  23. 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.
  24. 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.
  25. 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.
  26. 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.
  27. 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.
  28. 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.
  29. 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.
  30. 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.
  31. 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.
  32. 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.
  33. 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.
  34. TNF Receptor Inducer

    SMU127 is an agonist of the toll-like receptor 1/2 (TLR1/2) heterodimer, primarily targeting NF-κB signaling. It effectively induces TNF-α production in isolated human peripheral blood mononuclear cells (PBMCs) at concentrations of 0.01 to 1 μM and exhibits an EC50 of 0.55 μM in cells expressing human TLR2. In vivo studies demonstrate that SMU127 (0.1 mg/animal) significantly reduces tumor volume in a 4T1 murine mammary carcinoma model, making it a valuable tool for research on immune response and cancer therapy.
  35. PDE Inhibitor

    Theophylline sodium acetate functions as a potent phosphodiesterase (PDE) inhibitor, specifically targeting PDE3 to promote the relaxation of airway smooth muscle. It also acts as an adenosine receptor antagonist and histone deacetylase (HDAC) activator, contributing to its anti-inflammatory properties by elevating IL-10 levels and inhibiting NF-κB translocation to the nucleus. Additionally, Theophylline sodium acetate is known to induce apoptosis, making it a valuable reagent for research on asthma and chronic obstructive pulmonary disease (COPD).
  36. NF-κB Inhibitor

    CAY10512 is a potent NF-κB inhibitor that effectively suppresses the upregulation of NF-κB-sensitive proinflammatory microRNAs, including miRNA-9, miRNA-125b, miRNA-146a, and miRNA-155, in cerebrospinal fluid and extracellular environments. This compound significantly reduces the release of pro-inflammatory cytokines such as TNF-α, MCP-1, IL-8, and IL-6. CAY10512 is valuable for research applications focused on neuroinflammation, islet transplantation, and the regulation of microRNA.
  37. TLR7 Agonist

    SMU-L11-R is a selective TLR7 agonist that demonstrates an EC50 of 0.012 μM for human TLR7. This compound specifically activates TLR7, recruits MyD88, and initiates the MAPK/NF-κB signaling pathways, resulting in the secretion of pro-inflammatory cytokines such as TNF-α, IL-1β, and IL-6 in both mouse and human peripheral blood mononuclear cells. Additionally, SMU-L11-R promotes M1-like macrophage polarization and exhibits synergistic anti-tumor effects in combination with PD-L1 inhibitors through the upregulation of CD8+ T cells, making it a valuable tool for research in colorectal cancer.
  38. Anti-inflammatory Agent

    Kaempferol 3-O-(2G-glucosylrutinoside)-7-O-glucoside is a potent anti-inflammatory agent that targets key signaling pathways, including NF-κB, MAPK, and Akt. This compound significantly reduces the production of inflammatory mediators such as nitric oxide (NO) and prostaglandin E2 (PGE2) in LPS-induced RAW 264.7 macrophages. Additionally, it suppresses the secretion of pro-inflammatory cytokines, including TNF-α, IL-1β, and IL-6, making it valuable for research into inflammation and related disorders.
  39. COX-1/2 Inhibitor

    Cudraflavone B is a prenylated flavonoid that functions as a dual inhibitor of COX-1 and COX-2, demonstrating significant anti-inflammatory and anti-tumor activity. This compound inhibits the translocation of nuclear factor κB (NF-κB) in macrophages, leading to decreased tumor necrosis factor α (TNFα) gene expression and secretion. Additionally, Cudraflavone B induces the mitochondrial apoptotic pathway while activating MAPK signaling pathways, including p38 and ERK, and upregulating SIRT1 expression. These mechanisms contribute to its efficacy in attenuating the growth of human oral squamous cell carcinoma cells, making it a valuable tool for cancer research.
  40. Anti-inflammatory Agent

    rel-Cleroindicin F is an anti-inflammatory agent that targets the NF-κB signaling pathway. It effectively inhibits the production of nitric oxide (NO) and tumor necrosis factor-alpha (TNF-α) by downregulating NF-κB and its kinases in LPS-stimulated RAW 264.7 cells. This mechanism contributes to the suppression of inducible nitric oxide synthase expression, leading to decreased NO production. Rel-Cleroindicin F is valuable for research into inflammatory processes and potential therapeutic applications.
  41. sEH Inhibitor

    sEH-IN-21 is a potent inhibitor of soluble epoxide hydrolase (sEH), displaying IC50 values of 0.1 nM for both human and mouse sEH isoforms. This compound effectively inhibits NF-κB signaling pathways and demonstrates significant anti-inflammatory activity by reducing the release of pro-inflammatory cytokines IL-6 and TNF-α. Additionally, sEH-IN-21 helps maintain intestinal barrier integrity, making it a valuable tool for research on inflammatory bowel disease (IBD) and related inflammatory conditions.
  42. Antitumor Agent

    CDN-3 is a cyclic dideoxy nucleotide derivative that functions as an antitumor agent. It stimulates the production of IFN-β and activates the IRF-3 and NF-κB signaling pathways, leading to the induction of type I interferons and pro-inflammatory cytokines such as IL-6 and TNF-α. CDN-3 effectively inhibits the proliferation of cancer cells, making it a valuable tool for investigating mechanisms of colon cancer progression and therapeutic strategies.
  43. NF-κB Inhibitor

    Panaxytriol is a potent NF-κB inhibitor that effectively reduces the nuclear translocation of NF-κB. This mechanism leads to decreased production of pro-inflammatory cytokines, including TNF-α, IL-1β, and IL-6, as well as nitric oxide in response to LPS stimulation. Additionally, Panaxytriol promotes the upregulation of CYP3A4 through activation of the nuclear receptors PXR and CAR. Its ability to improve motor dysfunction in mouse models of brain inflammation makes Panaxytriol valuable for research into neurodegenerative diseases, such as Alzheimer's disease.
  44. Anti-inflammatory Agent

    Anti-inflammatory agent 41 is an effective inhibitor of lipopolysaccharide (LPS)-induced expression of pro-inflammatory cytokines IL-6 and TNF-α in J774A.1, THP-1, and LX-2 cells. This compound also inhibits the activation of the NF-κB signaling pathway. Its primary applications include investigating the mechanisms of inflammation and assessing potential therapeutic strategies in inflammation-related diseases.
  45. NO Release Inhibitor

    Sabialimon P is a nitric oxide (NO) release inhibitor with an IC50 of 18.12 μM. This compound exhibits potent anti-inflammatory effects by significantly reducing the secretion of pro-inflammatory cytokines such as TNF-α, IL-6, and the enzyme iNOS in LPS-stimulated RAW264.7 macrophage cells. Additionally, Sabialimon P inhibits the expression of COX-2 and the NF-κB/p65 pathway, making it a valuable tool for research into inflammation-related pathways and potential therapeutic applications.
  46. Anti-inflammatory Agent

    Anti-inflammatory agent 20 is a potent inhibitor of nitric oxide (NO) activity, demonstrating significant anti-inflammatory properties. This compound effectively suppresses lipopolysaccharide (LPS)-induced inflammation by inhibiting the activation of NF-κB and MAPK signaling pathways, leading to a reduction in pro-inflammatory cytokines such as IL-6, TNF-α, as well as the enzymes iNOS and COX-2. It serves as a valuable tool for research applications focused on inflammation and related signaling mechanisms.
  47. Furoquinoline Alkaloid

    Skimmianine is an orally active furoquiniline alkaloid present mainly in the Rutaceae family. Skimmianine has analgesic, antispastic, sedative, and anti-inflammatory properties. Skimmianine inhibits acetylcholinesterase (AChE) (IC50 = 8.6 μg/mL). Skimmianine exhibits cytotoxicity against a variety of cancer cell lines and genotoxicity. Skimmianine has antioxidant and anti-inflammatory effects on ischemia-reperfusion (IR) injury. Skimmianine exerts anti-inflammatory effects through activation of the phosphatidylinositol-3-kinase (PI3K)-protein kinase B (AKT) pathway. Skimmianine is neuroprotective by targeting the NF-κB activation pathway to prevent neuroinflammation. Skimmianine inhibits the release of histamine, intracellular Ca2+ signaling and protein kinase C signaling.
  48. Diterpenoid

    Kirenol is a diterpenoid compound, an orally active apoptosis inducer and signaling pathway regulator, with a Kd value of 5.47 μM against the target CK2. Kirenol promotes the cleavage of Bid into tBid, regulates the protein levels/phosphorylation of Bax, Bcl-2, p53 and p21, and induces caspase-independent apoptosis, S-phase cell cycle arrest, ROS accumulation and cytotoxicity in cancer cells. Kirenol activates the CK2/AKT and AMPK-mTOR-ULK1 pathways, inhibits the signaling of NF-κB, TGF-β/Smads and NLRP3 inflammasome, and regulates the GSK3β, BMP and Wnt/β-catenin pathways. Kirenol induces autophagy, mitophagy and osteoblast differentiation, promotes mitochondrial fusion, and exerts antioxidant, anti-inflammatory, antifibrotic, renoprotective, cardioprotective, neuroprotective and analgesic effects. Kirenol is applicable to research related to chronic myeloid leukemia, ischemic stroke, diabetic nephropathy, heart failure, acute lung injury and osteoporosis.
  49. pre-mRNA Splicing Inhibitor

    Isoginkgetin is a pre-mRNA splicing inhibitor that modulates splicing processes critical for gene expression. In addition to its primary function, Isoginkgetin inhibits the activities of the signaling proteins Akt and NF-κB, as well as matrix metalloproteinase-9 (MMP-9). This compound is known to inhibit the 20S proteasome, inducing apoptosis and activating autophagy, making it a valuable tool in cancer research and studies focused on cellular stress responses.
  50. COX Inhibitor

    Oxaprozin is a potent, orally active cyclooxygenase (COX) inhibitor, demonstrating IC50 values of 2.2 μM for human platelet COX-1 and 36 μM for IL-1-stimulated human synovial cell COX-2. This compound exhibits significant anti-inflammatory activity and is known to inhibit the activation of NF-κB, promoting cell apoptosis. The inhibition of the Akt/IKK/NF-κB signaling pathway is a key mechanism underlying its anti-inflammatory properties, making Oxaprozin valuable for research in inflammation and related disorders.

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