Immunology & Inflammation

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  1. RNA Modifying Substance

    N4-Acetylcytidine is an RNA-modifying nucleoside metabolite produced during tRNA degradation, primarily via N-acetyltransferase 10 and additional enzymes. This compound has been shown to enhance NLRP3 inflammasome activation through the upregulation and release of HMGB1. N4-Acetylcytidine plays a crucial role in modifying the stability and translation efficiency of mRNA, tRNA, and rRNA, particularly in relation to enterovirus 71 RNA. Its applications extend to research in cancer, neuroinflammatory diseases, viral infections, and obesity.
  2. NCD38 Enantiomer

    (1R,2S)-NCD38 TFA is a selective inhibitor of Lysine-specific demethylase 1 (LSD1). This enantiomeric form of NCD38 TFA exhibits potent biological activity, primarily in the modulation of epigenetic regulation through LSD1 inhibition. It is applicable in research focused on cancer biology, developmental studies, and potential therapeutic interventions targeting LSD1-related pathways.
  3. Anti-Inflammatory Agent

    Triamcinolone acetonide is a potent anti-inflammatory agent that primarily targets fibroblast growth factor (bFGF) signaling pathways. It effectively inhibits bFGF-induced proliferation of retinal endothelial cells, promotes macrophage activation with anti-inflammatory properties, and reduces chondrocyte viability, contributing to cartilage degradation. This compound is valuable for research applications related to various inflammatory conditions, including atopic dermatitis.
  4. Nrf2 Activator

    Dimethyl fumarate is an orally bioavailable Nrf2 activator that enhances the expression of antioxidant genes. This compound has been shown to induce necroptosis in colon cancer cells via mechanisms involving glutathione depletion, reactive oxygen species elevation, and activation of MAPK pathways. Additionally, Dimethyl fumarate promotes autophagy and is applicable in studies focused on multiple sclerosis and related neurodegenerative conditions.
  5. Anti-inflammatory Agents

    Balsalazide disodium is a prodrug that releases mesalamine in the colon, primarily targeting anti-inflammatory pathways. It exhibits significant anti-inflammatory activity in conditions such as colitis and demonstrates potential anticancer effects through modulation of the IL-6/STAT3 signaling pathway. This compound is useful in research focused on gastrointestinal disorders and cancer therapy.
  6. Anti-inflammatory Agent

    Luteolin 5-O-glucoside is a potent anti-inflammatory agent derived from Cirsium maackii. This compound effectively inhibits lipopolysaccharide (LPS)-induced nitric oxide production and tert-butyl hydroperoxide (t-BHP)-induced reactive oxygen species generation. Additionally, Luteolin 5-O-glucoside downregulates the expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) in macrophages, making it valuable for research in inflammatory pathways and related conditions.
  7. Anti-inflammatory Agent

    Ajugol is an orally active iridoid glycoside that functions as an anti-inflammatory agent. It activates TFEB-mediated autophagy and lysosomal biogenesis, contributing to its protective effects on cellular homeostasis. Ajugol demonstrates significant potential for research in conditions such as asthma, non-alcoholic fatty liver disease (NAFLD), and osteoarthritis due to its dual role in promoting autophagy and mitigating inflammation.
  8. PDE IV Inhibitor/A1AR Antagonist

    Doxofylline is an orally active phosphodiesterase IV (PDE IV) inhibitor and adenosine A1 receptor (A1AR) antagonist. It exhibits anti-inflammatory properties by reducing mitochondrial reactive oxygen species (ROS) production and modulating various cellular pathways, including the NLRP3-TXNIP inflammasome activation. This compound is valuable for research related to respiratory diseases such as asthma, chronic obstructive pulmonary disease (COPD), and bronchospasm.
  9. Nonsteroidal Anti-inflammatory Agent

    2-Ethoxybenzamide is a nonsteroidal anti-inflammatory agent that exhibits both analgesic and antipyretic activities. Its mechanism involves the induction of melanin synthesis through the phosphorylation of cAMP response element-binding protein (CREB). This compound is valuable for research focused on hypopigmentation and inflammation-related diseases, providing insights into therapeutic applications and biological pathways involved in these conditions.
  10. PD-1/PD-L1 Interaction Inhibitor

    PD-1/PD-L1-IN 3 is a macrocyclic peptide that acts as a selective inhibitor of the PD-1/PD-L1 and CD80/PD-L1 interactions. By binding to PD-L1, it effectively disrupts the binding of PD-L1 to PD-1 and CD80, exhibiting IC50 values of 5.60 nM and 7.04 nM, respectively. This compound is valuable for research in various fields, particularly in cancer immunotherapy and the study of infectious diseases.
  11. Anti-inflammatory Agent

    Salsalate is an anti-inflammatory agent primarily targeting the modulation of cytokine expression without direct cyclooxygenase inhibition. This compound exhibits significant anti-inflammatory effects and has been shown to lower blood glucose levels, enhance insulin sensitivity, and mitigate the effects of metabolic disorders associated with high-fat diets. Salsalate is utilized in research pertaining to type 2 diabetes, atherosclerosis, and non-alcoholic steatohepatitis, demonstrating its potential in the management of metabolic disorders.
  12. COX-1/cAMP Phosphodiesterase Inhibitor

    Triflusal is a dual inhibitor of Cyclooxygenase-1 (COX-1) and cAMP phosphodiesterase, which penetrates the blood-brain barrier. It effectively inhibits platelet aggregation, nuclear factor kappa B (NF-κB) activation, inducible nitric oxide synthase (iNOS) activity, and prostaglandin synthesis in ischemic tissues. Additionally, Triflusal enhances neutrophil nitric oxide production, endothelial nitric oxide synthase (eNOS) expression, and constitutive nitric oxide synthase (cNOS) activity. This compound is valuable for investigating thromboembolic and ischemic diseases of the cardiovascular and cerebrovascular systems, as well as Alzheimer's disease pathology.
  13. Nrf2 Activator

    Raffinose serves as an Nrf2 activator and is known for its ability to modulate intestinal flora. It inhibits the TLR4-MyD88-NF-κB signaling pathway while promoting Nrf2 signaling, contributing to its anti-inflammatory, antioxidant, and immunomodulatory properties. This compound is orally active and is valuable in research applications focusing on inflammation and oxidative stress.
  14. β/α-1 Blocker

    Carvedilol phosphate hemihydrate is a non-selective β/α-1 adrenergic receptor blocker. It demonstrates significant biological activity by inhibiting lipid peroxidation with an IC50 of 5 μM and acts as a multiple-action antihypertensive agent, with potential applications in treating angina and congestive heart failure. Additionally, carvedilol phosphate hemihydrate has been identified as an autophagy inducer that suppresses the NLRP3 inflammasome, making it valuable for research in inflammation and cardiovascular diseases.
  15. nNOS Inhibitor

    NXN-188 is a selective nNOS inhibitor that also acts as an agonist for the 5HT-1B/1D receptors. This compound exhibits potential in modulating neurogenic inflammation and is particularly relevant in research focused on migraine pathophysiology and treatment strategies. Its dual action supports investigations into the intricate mechanisms underlying headache disorders.
  16. COX Inhibitor

    Pentagamavunon-1 (PGV-1) is a COX-2 inhibitor that modulates multiple molecular pathways to induce apoptosis. This Curcumin analog exhibits notable oral bioactivity and suppresses key angiogenic factors, including vascular endothelial growth factor (VEGF). Additionally, PGV-1 inhibits NF-κB activation, highlighting its potential in cancer research and therapeutic applications targeting inflammation and tumor progression.
  17. E3 Ligase Ligand-Linker Conjugates

    Thalidomide-piperazine-Boc is an E3 ligase ligand-linker conjugate that serves as an intermediate in the synthesis of PROTAC targeting B-cell lymphoma 6 protein (BCL6). This compound plays a significant role in targeted protein degradation, facilitating the selective destruction of BCL6 and aiding in research related to cancer therapeutics. Its application is essential for studies focusing on E3 ligase modulation and PROTAC development in oncology.
  18. CD47-SIRPα axis Inhibitor

    DMUP is a potent inhibitor of the CD47-SIRPα axis. This compound promotes apoptosis and enhances macrophage phagocytosis in A549 lung cancer cells, while also reducing the expression of CD47 and SIRPα proteins. DMUP demonstrates significant antitumor activity, making it a valuable tool for research in cancer immunotherapy and macrophage biology.
  19. PD-1/PD-L1 Inhibitor

    PD-1/PD-L1-IN-10 is a potent orally active inhibitor of the PD-1/PD-L1 interaction, with an IC50 value of 2.7 nM. This compound exhibits significant anticancer efficacy by blocking the immune checkpoint pathway, thereby enhancing T-cell activation and promoting anti-tumor responses. PD-1/PD-L1-IN-10 is valuable for research in immunotherapy and cancer treatment studies.
  20. NLRP3-targeting Renalase Peptide

    RP-220 is a renalase peptide that specifically targets the NLRP3 inflammasome. It exhibits significant anti-inflammatory and anti-apoptotic properties, evidenced by its ability to inhibit apoptosis in renal tubular epithelial cells under alkaline stress through activation of the MAPK signaling pathway. Additionally, RP-220 reduces NLRP3 expression, limits macrophage infiltration, and mitigates kidney tissue damage in models of acute kidney injury (AKI). This reagent is particularly relevant for research into systemic lupus erythematosus (SLE) and its associated complication, lupus nephritis (LN).
  21. Nrf2 Activator

    Sarmentosin is a potent activator of the Nrf2 pathway, which plays a crucial role in cellular defense against oxidative stress. This compound has been shown to inhibit mTOR signaling and promote autophagy-dependent apoptosis in human hepatocellular carcinoma (HCC) cells. Its ability to modulate these critical pathways makes Sarmentosin a valuable tool for research into cancer biology and potential therapeutic strategies.
  22. Anti-inflammatory Agent

    Brazilein is an anti-inflammatory agent that targets Na+,K+-ATPase with an IC50 of 500 μM. It exhibits potent neuroprotective activities by reducing iNOS mRNA expression, thereby inhibiting nitric oxide production in immune cells and modulating inflammatory cytokines such as TNF-α and IL-6. Brazilein has been shown to decrease cerebral infarction volume and enhance neurological function in models of cerebral ischemia-reperfusion injury. Additionally, it induces apoptosis in splenic lymphocytes and can affect immune responses and organ weights, making it valuable for research in neurobiology, cardiovascular health, and inflammatory disorders.
  23. Stable Isotope

    Everolimus-d4 is a deuterium-labeled derivative of Everolimus, a potent and selective inhibitor of mTOR1. By binding to FKBP-12, Everolimus-d4 forms an immunosuppressive complex that effectively inhibits tumor cell proliferation, while simultaneously inducing apoptosis and autophagy. This stable isotope is valuable for research applications in oncology and immunology, facilitating studies on the therapeutic mechanisms and metabolic pathways associated with mTOR inhibition.
  24. Nrf2 Activator

    Nrf2 Activator-10 (Compound AI-1) acts as a PI3K-dependent inducer of the antioxidant response element (ARE), with an EC50 value of 2.7 μM, effectively activating Nrf2. By modifying Keap1 and inhibiting the Cul3-Keap1 ubiquitin ligase complex, Nrf2 Activator-10 enhances Nrf2 transcription and promotes cellular defense mechanisms. This compound is particularly valuable for research focused on oxidative stress and cytoprotection, demonstrating protective effects against H2O2-induced apoptosis.
  25. Anti-inflammatory Agent

    (-)-Pinoresinol is a plant-derived tetrahydrofuran lignan that serves as an anti-inflammatory agent through the inhibition of α-glucosidase. This compound exhibits hypoglycemic properties and demonstrates chemopreventive potential by inducing apoptosis and causing G2/M phase cell cycle arrest. Its biological activities make it a valuable tool for research in inflammation and metabolic disorders.
  26. Anti-inflammatory Agent

    Taurodeoxycholate-d6 sodium is an anionic detergent derived from bile salts, functioning primarily as an anti-inflammatory agent. This compound promotes the isolation of membrane proteins, particularly in the inner mitochondrial membrane, making it essential for studies in cellular biology. Furthermore, Taurodeoxycholate-d6 demonstrates notable anti-inflammatory and neuroprotective properties, positioning it as a valuable tool for research applications focused on inflammation and neuroprotection pathways.
  27. Anti-inflammatory Agent

    Lactucin is a recognized anti-inflammatory agent that promotes apoptosis in cancer cells. Additionally, it exhibits analgesic, anticancer, and antimalarial properties, making it a versatile compound for various biological research applications. Its multifaceted activity provides valuable insights into potential therapeutic interventions for inflammatory diseases and cancer.
  28. Anticancer/Anti-inflammatory Agent

    Isoangustone A is an effective anticancer and anti-inflammatory agent that promotes apoptosis and autophagic cell death in cancer cells. This compound is of interest for research applications aimed at understanding cancer biology and developing potential therapeutic strategies. Its dual action highlights its relevance in the study of cancer progression and inflammation-mediated diseases.
  29. Stable Isotope

    Lenalidomide-d5 is a stable isotope-labeled derivative of Lenalidomide, an immunomodulatory compound that functions as a molecular glue. By acting as a ligand for the ubiquitin E3 ligase cereblon (CRBN), it facilitates the selective ubiquitination and subsequent degradation of the transcription factors IKZF1 and IKZF3. Lenalidomide-d5 is pivotal for research in cancer biology, particularly for investigating the mechanisms of action in mature B-cell lymphomas, including multiple myeloma, and for studying its effects on cytokine release from T cells.
  30. CypA Inhibitor

    HL001 is an oral small molecule inhibitor targeting Cyclophilin A (CypA) and acting as a receptor antagonist for Lysophosphatidic acid 1 (LPA1). This compound induces cell cycle arrest and apoptosis in tumor cells via p53 stabilization, achieved by down-regulating G3BP1 and promoting reactive oxygen species production and DNA damage. HL001 disrupts the MDM2-p53-72R interaction in a CypA-dependent manner, demonstrating significant antitumor activity. Additionally, HL001 serves as a valuable tool in the investigation of pulmonary fibrosis.
  31. NADPH Oxidase Inhibitor

    VAS 3947 is a selective inhibitor of NADPH oxidase (NOX), demonstrating significant antiplatelet activity. In addition to its role as an NOX inhibitor, VAS 3947 induces apoptosis through the activation of the unfolded protein response (UPR), primarily driven by protein aggregation and misfolding. This compound is valuable for research focused on oxidative stress and its implications in cardiovascular diseases.
  32. TFAP2β Modulator

    TFAP2β modulator-1 is a potent modulator of the transcription factor TFAP2β, promoting its condensation through the induction of conformational changes within its intrinsically disordered region. This compound exhibits significant anti-tumor activity by inducing apoptosis in esophageal squamous cell carcinoma (ESCC) cells, as well as in relevant mouse models and organoids. TFAP2β modulator-1 serves as a valuable tool for investigating the role of TFAP2β in ESCC research and therapeutic development.
  33. NF-κB Inhibitor/Nrf2/AMPK Activator

    Panduratin A is a potent inhibitor of the NF-κB signaling pathway, recognized for its significant anti-inflammatory and antioxidant properties. It demonstrates protective effects against nephrotoxicity induced by Colistin, primarily by mitigating oxidative stress and enhancing mitochondrial function. Additionally, Panduratin A activates autophagy through an AMPK-dependent mechanism and exhibits potential anti-tuberculosis and antiviral activities by inhibiting the methyltransferase of SARS-CoV-2. These diverse biological activities make Panduratin A a valuable tool in various areas of research, including inflammation, cellular stress responses, and infectious diseases.
  34. E3 Ligase Ligand-linker Conjugate

    Thalidomide-4-O-C6-NH2 TFA is a synthetic E3 ligase ligand-linker conjugate designed for use in targeted protein degradation applications. This compound plays a critical role in the PROTAC dTAG-13, facilitating the selective degradation of FKBP12F36V and BET proteins. Its unique structural features allow for efficient recruitment of E3 ligases, making it a valuable tool in cellular studies of protein regulation and degradation pathways.
  35. FLAP Inhibitor

    MK-886 sodium salt is a potent inhibitor of the 5-lipoxygenase-activating protein (FLAP), exhibiting an IC50 of 30 nM. It effectively inhibits leukotriene biosynthesis with IC50 values of 3 nM in intact leukocytes and 1.1 μM in human whole blood. Additionally, MK-886 acts as a non-competitive antagonist of PPARα and can induce apoptosis, making it a valuable tool for research in inflammatory diseases and apoptosis pathways.
  36. COX Inhibitor

    Ketorolac hemicalcium is a non-steroidal anti-inflammatory drug (NSAID) that functions as a nonselective cyclooxygenase (COX) inhibitor, exhibiting IC50 values of 20 nM for COX-1 and 120 nM for COX-2. This compound is utilized in research related to allergic conjunctivitis, cystoid macular edema, intraoperative miosis, and postoperative ocular inflammation and pain, as well as for its potential applications in cancer research due to its role as a DDX3 inhibitor.
  37. Nrf2 activator

    Nrf2 activator-11 is a potent Nrf2 activator that demonstrates blood-brain barrier permeability. This compound exhibits significant biological activities, including antioxidant, anti-inflammatory, anti-ferroptotic, and anti-apoptotic effects. Nrf2 activator-11 is particularly valuable for research involving cerebral ischemia-reperfusion injury models, providing insights into neuroprotective mechanisms and therapeutic interventions.
  38. COX Inhibitor

    Metamizole magnesium is an orally active cyclooxygenase (COX) inhibitor known for its key roles in reducing inflammation and pain. It exhibits significant anti-inflammatory and antioxidant activities, along with the ability to inhibit cell proliferation and promote apoptosis. Due to its antipyretic and analgesic properties, Metamizole magnesium is commonly utilized in various research applications aimed at investigating pain mechanisms and inflammatory responses.
  39. Anti-Inflammatory Agent

    Stephanine ((-)-Stephanine) is an isoquinoline aporphine-type alkaloid known for its anti-inflammatory properties. It induces apoptosis via the reversal of mitotic exit, demonstrating significant antiplasmodial activity. This compound is valuable for research applications related to gastrointestinal disorders, inflammatory conditions such as arthritis, and various cancer types.
  40. Topo I/COX-2 Inhibitor

    Topo I/COX-2-IN-1 is an inhibitor of both Topoisomerase I and Cyclooxygenase-2 (COX-2). It demonstrates significant biological activity, with IC50 values of 0.24 μM for COX-2 and 4.42 μM for Topo I. This compound effectively induces apoptosis and inhibits the migration of cancer cells, showcasing potential applications in cancer research and therapy.
  41. Topo I/COX-2 Inhibitor

    Topo I/COX-2-IN-2 is a potent dual-target inhibitor of Topoisomerase I (Topo I) and Cyclooxygenase-2 (COX-2), exhibiting inhibitory concentrations (IC50) of 0.90 μM and 2.31 μM, respectively. This compound induces apoptosis in cancer cells via the mitochondrial pathway, making it a valuable agent for research in cancer therapeutics and cell death mechanisms. Its dual activity supports investigations into the interplay between topoisomerase inhibition and inflammatory pathways in cancer progression.
  42. STING Activator

    PDIC-NN dimethanesulfonate is a potent STING activator known for its anticancer properties. It enhances the stability and levels of endogenous cyclic dinucleotides (CDNs), triggering a reactive oxygen species (ROS) burst that damages mitochondria, thereby inducing apoptosis and inhibiting DNA replication. By activating the cGAS-STING signaling pathway, PDIC-NN dimethanesulfonate boosts the immunogenicity of tumor cells and stimulates a robust innate immune response, making it a valuable reagent for cancer immunotherapy research.
  43. Celecoxib Analog

    OSU-03013 is a Celecoxib analog that targets multiple pathways involved in cancer progression. It promotes apoptosis while enhancing E-cadherin expression and reduces β-catenin, c-myc, Wnt1, and N-cadherin levels. By inhibiting cell migration and invasion, OSU-03013 effectively regulates Wnt and mTOR signaling, leading to decreased proliferation of colon cancer cells. This compound is suitable for research focused on colon cancer and its underlying mechanisms.
  44. TLR3 Agonist

    Polyinosinic-polycytidylic acid sodium is a synthetic analogue of double-stranded RNA and acts as an agonist for toll-like receptor 3 (TLR3) and RIG-I-like receptors. It serves as a potent immunomodulator, enhancing both innate and adaptive immune responses, making it valuable for vaccine development. Additionally, Poly(I:C) sodium can influence the tumor microenvironment and directly induce apoptosis in cancer cells, thus providing significant potential in cancer research and therapy.
  45. Complement Inhibitor

    Dextran sulfate sodium salt (DSS, MW 5000) primarily functions as a complement inhibitor, derived from a polymer of dehydrated glucose. This compound exhibits significant biological activities, including anticoagulation, antiviral properties, and anti-lipemic effects. Its mechanisms involve blocking HIV-1 adsorption to host cells, preventing natural killer (NK) cell-mediated cytotoxicity, and inhibiting instant blood-mediated inflammatory reactions (IBMIR). Dextran sulfate sodium salt (MW 5000) is valuable in research related to immunology, virology, and cardiovascular studies.
  46. TLR9 Agonist

    ODN 1826 is a class B CpG oligodeoxynucleotide that acts as an agonist for Toll-like receptor 9 (TLR9). It stimulates the production of nitric oxide (NO) and inducible nitric oxide synthase (iNOS), promoting apoptosis and enhancing immune surveillance. This compound is also associated with increased aortic atherosclerotic plaque size and exhibits antitumor activity against various cancer types, including lung cancer, glioma, and melanoma. ODN 1826 is valuable for researching immune response mechanisms and potential cancer therapies.
  47. TLR7/8 Antagonist

    Afimetoran is a selective and highly bioavailable antagonist of Toll-like receptors 7 and 8 (TLR7/8). It effectively inhibits TLR7/8-mediated activation of the NF-κB signaling pathway and can reverse TLR7-induced resistance to steroid-driven apoptosis in plasmacytoid dendritic cells. This compound is particularly relevant for research into inflammation and autoimmune diseases, including systemic lupus erythematosus.
  48. TLR9 Agonist

    Agatolimod is a Toll-like receptor 9 (TLR9) agonist and immunomodulator with an EC50 of 180 nM. It activates TLR9 and upregulates TLR6 expression, initiating downstream signaling through IRAK4, IRF5, and IRF7. Agatolimod enhances Th1-type immune responses and promotes the activation of various immune cells, leading to increased antigen presentation, antibody regulation, cytokine secretion, apoptosis, and enhanced cytotoxicity. This compound is relevant for research into COVID-19, breast cancer, lung adenocarcinoma, HPV-related tumors, melanoma, and salmonellosis.
  49. Autophagy Inducer, NLRP3 Inhibitor

    Britannin is an autophagy inducer and NLRP3 inflammasome inhibitor with an IC50 of 3.630 μM. It exhibits significant anti-inflammatory effects by disrupting the interaction between NLRP3 and NEK7, effectively preventing NLRP3 activation and assembly. Additionally, Britannin shows antitumor properties by inhibiting tumor cell proliferation through interference with the interaction of HIF-1α and Myc, leading to reduced PD-L1 expression and enhanced activity of cytotoxic T lymphocytes. This compound also promotes apoptosis and autophagy in liver cancer cells via activation of ROS-regulated AMPK, making it a valuable tool for research in anti-inflammatory and oncology studies.
  50. COX-1 Inhibitor

    Ibuprofen sodium is a selective inhibitor of cyclooxygenase-1 (COX-1), exhibiting an IC50 value of 13 μM. This compound demonstrates significant biological activities, including inhibition of cell proliferation, angiogenesis, and induction of apoptosis. As a nonsteroidal anti-inflammatory agent and nitric oxide (NO) donor, ibuprofen sodium is valuable in research areas such as pain, inflammation, infection, immunology, and oncology.

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