Immunology & Inflammation

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  1. COX Inhibitor

    AL-8417 ((2R)-AL-5898) is a potent inhibitor of Cyclooxygenase (COX), exhibiting an IC50 of 120 μM. This compound is significant in modulating inflammatory responses, making it a valuable tool for research into pain relief and inflammation management. Its application in experimental settings can further elucidate the role of COX in various biological processes and disease states.
  2. COX-2 Inhibitor

    N-Caffeoyl serotonin is a selective COX-2 inhibitor, characterized by IC50 and Kᵢ values of 42.5 μM and 65.5 μM, respectively. This compound exhibits minimal inhibitory activity against BACE1, with an IC50 greater than 400 μM, and demonstrates free radical scavenging properties. N-Caffeoyl serotonin is pertinent for research in allergic diseases as well as Alzheimer's disease, providing a valuable tool for investigating inflammatory pathways and neurodegeneration.
  3. COX-2 Inhibitor

    Harmaline analog is a selective inhibitor of cyclooxygenase-2 (COX-2) demonstrating an IC50 of 0.145 μM. This compound is useful for studying the COX-2 enzyme's role in inflammatory processes and pain modulation. Its application includes research on anti-inflammatory therapies and the development of novel analgesics.
  4. COX-2 Inhibitor

    COX-2-IN-36 is a highly selective inhibitor of cyclooxygenase-2 (COX-2), demonstrating an IC50 value of 0.4 μM. This compound effectively inhibits COX-2 enzymatic activity, thereby reducing the synthesis of prostaglandins involved in inflammation and pain. It is suitable for research applications focusing on inflammatory diseases, pain management, and cancer biology, offering a valuable tool for exploring COX-2-related pathways.
  5. COX Inhibitor

    N-(3-Pyridyl)indomethacinamide is a COX-2 inhibitor derived from indomethacin. This compound exhibits potent anti-inflammatory activity by selectively inhibiting cyclooxygenase-2, making it valuable for research in inflammation and pain management. Its unique chemical structure allows for further exploration of its effects in various biological systems and therapeutic applications.
  6. COX-1/2 Inhibitor

    COX-1/2-IN-6 is a potent dual inhibitor of cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2), exhibiting IC50 values of 68 nM and 91 nM, respectively. This compound is valuable for studying inflammatory diseases by effectively modulating the COX enzymatic pathways involved in prostaglandin synthesis. Its inhibition profile makes it suitable for research on pain management and inflammatory-related conditions.
  7. COX-1 Inhibitor

    Tenidap sodium is a selective inhibitor of cyclooxygenase-1 (COX-1), with an IC50 of 0.03 μM for COX-1 and 1.2 μM for COX-2. This non-steroidal anti-inflammatory compound exhibits significant anti-inflammatory and anti-rheumatic properties, making it valuable in research focused on inflammatory diseases. Additionally, Tenidap functions as a specific inhibitor of SLC26A3, further broadening its potential applications in biochemical studies.
  8. COX-2 Inhibitor

    4-Desmethyl-2-methyl celecoxib is a selective cyclooxygenase-2 (COX-2) inhibitor, exhibiting an IC50 value of 0.069 µM. This compound demonstrates significant anti-inflammatory, analgesic, and antipyretic properties by reducing the synthesis of prostaglandins. Its efficacy makes it a valuable tool for the investigation of inflammatory conditions and pain-related disorders, including rheumatoid arthritis and osteoarthritis.
  9. COX-2 Inhibitor

    ABT-963 is a selective inhibitor of cyclooxygenase-2 (COX-2), targeting the COX-2 enzyme involved in the biosynthesis of prostaglandins. This compound exhibits significant anti-inflammatory and analgesic properties, making it a valuable tool for research focused on pain mechanisms and inflammatory diseases. ABT-963 can be utilized to explore the role of COX-2 in various pathophysiological processes, facilitating the development of therapeutic strategies for related conditions.
  10. COX-2 Inhibitor

    Methosulide is a selective COX-2 inhibitor, exhibiting an IC50 value of 2.31 μM. This compound is primarily utilized in the study of inflammatory diseases, providing insights into the role of COX-2 in various pathological conditions. Its selective inhibition profile makes it a valuable tool for researchers investigating potential therapeutic strategies targeting inflammatory pathways.
  11. COX/5-LOX Inhibitor

    ZLJ-6 is a dual inhibitor of cyclooxygenase (COX) and 5-lipoxygenase (5-LOX), demonstrating potent oral bioactivity. With IC50 values of 0.73 μM for COX-1, 0.31 μM for COX-2, and 0.99 μM for 5-LOX, ZLJ-6 exhibits significant anti-inflammatory and analgesic properties. This compound is suitable for research applications aimed at investigating inflammatory pathways and potential therapeutic interventions.
  12. COX Inhibitor

    Flosulide is a selective inhibitor of cyclooxygenase-2 (COX-2), demonstrating significant anti-inflammatory properties. It effectively reduces inflammation and alleviates pain associated with various inflammatory diseases. Flosulide is commonly used in research applications focused on the modulation of inflammatory pathways and exploration of COX-2 related biological processes.
  13. COX-2 Inhibitor

    COX-2-IN-39 is a highly effective inhibitor of cyclooxygenase-2 (COX-2), demonstrating an impressive IC50 value of 0.4 nM. This compound plays a critical role in research focused on inflammation and pain pathways, making it a valuable tool for studying COX-2-related diseases and therapeutic interventions. Its potency allows for precise modulation of COX-2 activity in various experimental models, facilitating in-depth analysis of its biological effects.
  14. COX Inhibitor

    Catechin hydrate is a potent inhibitor of cyclooxygenase-1 (COX-1), exhibiting an IC50 value of 1.4 μM. Its anti-inflammatory properties make it valuable in research applications related to pain relief and inflammatory disease models. This compound's capability to modulate COX-1 activity supports studies investigating the biochemical pathways involved in inflammation and related conditions.
  15. 5-LOX/COX Inhibitor

    (-)-Bornyl ferulate serves as a dual inhibitor of 5-lipoxygenase (5-LOX) and cyclooxygenase (COX), displaying IC50 values of 10.4 μM and 12.0 μM, respectively. This compound demonstrates significant anti-inflammatory potential, making it useful for research focused on inflammation-related pathways and conditions. Its ability to modulate leukotriene and prostaglandin synthesis positions it as a valuable tool in the study of various inflammatory diseases and therapeutic interventions.
  16. COX-2 Inhibitor

    Cavidine is a selective COX-2 inhibitor that exhibits potent anti-inflammatory properties. It is particularly useful in research concerning skin injuries, hepatitis, cholecystitis, and scabies. Additionally, Cavidine has been shown to alleviate LPS-induced acute lung injury through modulation of the NF-κB signaling pathway, making it a valuable compound for studying inflammation-related conditions.
  17. COX-2 Inhibitor

    Nimesulide-d5 is a deuterated form of Nimesulide, a selective cyclooxygenase-2 (COX-2) inhibitor. It demonstrates a time-dependent inhibitory effect on COX-2 with IC50 values ranging from 70 nM to 70 μM, while exhibiting negligible activity on COX-1 (IC50 >100 μM). Nimesulide-d5 is utilized in research applications focusing on inflammatory processes, pain management, and antipyretic effects, supporting studies aimed at understanding COX-2 mediated pathways.
  18. COX Inhibitor

    Piroxicam olamine is a non-steroidal anti-inflammatory drug that acts as an inhibitor of cyclooxygenase (COX), targeting both COX-1 and COX-2 isoforms with IC50 values of 47 μM and 25 μM, respectively, in human monocytes. This compound is primarily used in research applications focused on inflammation and analgesia. Its mechanism of action makes it a valuable tool for studying pathways involved in pain and inflammatory responses.
  19. COX Inhibitor

    COX-2-IN-1 is a potent and selective inhibitor of cyclooxygenase-2 (COX-2), exhibiting an IC50 of 3.9 μM. This compound is valuable for studying COX-2-related pathways and has applications in inflammation and pain research. By selectively targeting COX-2, it allows for the investigation of its role in various physiological and pathological processes.
  20. COX Inhibitor

    Tilmacoxib is a highly selective, irreversible inhibitor of human COX-2, demonstrating time-dependent inhibition with an IC50 of 85 nM in enzyme assays. This compound is primarily utilized in studies investigating the role of COX-2 in inflammatory processes and related disease models. Its specificity and potency make it a valuable tool for elucidating the therapeutic potential of COX-2 inhibition in various biological contexts.
  21. COX Inhibitor

    COX/5-LO-IN-1 is a potent inhibitor targeting cyclooxygenase (COX) and 5-lipoxygenase (5-LO), integral enzymes in the arachidonic acid pathway. This compound demonstrates significant anti-inflammatory and anti-allergic properties, making it a valuable tool for investigating the molecular mechanisms underlying inflammatory and allergic diseases. Its dual inhibition profile supports research into therapeutic strategies for various pathological conditions linked to dysregulated eicosanoid signaling.
  22. COX Inhibitor

    SC58451 is a selective inhibitor of cyclooxygenase-2 (COX-2), known for its potency in downregulating inflammatory pathways. By specifically targeting COX-2, this compound is effective in reducing prostaglandin synthesis, making it valuable for studies related to inflammation and pain management. SC58451 is suitable for research applications in understanding diseases where COX-2 plays a critical role, such as cancer and inflammatory disorders.
  23. CTLA-4/PD-L1 Inhibitor

    Davoceticept is a fusion protein consisting of the CD80 (1-107) fragment linked to IGHG1 Fc via a peptidyl linker, targeting CTLA-4 and PD-L1. This variant CD80 vIgD-Fc acts as an immune checkpoint inhibitor, enhancing T cell activation and promoting anti-tumor responses. Its applications include cancer immunotherapy and studying immune modulation in various malignancies, making it a valuable tool for researchers investigating therapeutic strategies in cancer treatment.
  24. Calcineurin Inhibitor

    Cyclosporin A-Derivative 1 (Free base) acts as a potent calcineurin inhibitor through its interaction with cyclophilin. This compound is derived from cyclosporin A and plays a critical role in immunosuppression by inhibiting T-lymphocyte activation. It is primarily utilized in research applications focused on transplant immunology and autoimmune disease modeling.
  25. CypD Inhibitor

    CypD-IN-4 is a potent and selective inhibitor of cyclophilin D (CypD), exhibiting high affinity with an IC50 of 0.057 μM. This compound is valuable in researching various conditions related to oxidative stress, neurodegenerative diseases, liver dysfunction, aging processes, autophagy, and diabetes. CypD-IN-4 facilitates the exploration of CypD's role in these pathologies, providing insights into potential therapeutic strategies.
  26. CypD Inhibitor

    CypD-IN-3 is a potent and selective inhibitor of cyclophilin D (CypD), demonstrating high affinity with an IC50 value of 0.01 μM. This compound is valuable for studying a range of biological processes and diseases, including oxidative stress, neurodegenerative disorders, liver diseases, aging, autophagy, and diabetes. Its specificity towards CypD makes it an important tool for elucidating the role of this target in various cellular functions and pathological conditions.
  27. CypE Inhibitor

    CypE-IN-1 is a highly potent and selective inhibitor of cyclophilin E (CypE), exhibiting an IC50 of 0.013 μM and a Ki value of 0.072 μM. This compound is valuable for investigating the role of CypE in various pathological conditions, including oxidative stress, neurodegenerative diseases, liver disorders, aging processes, autophagy, and diabetes. Researchers can utilize CypE-IN-1 to explore therapeutic strategies targeting CypE-related pathways.
  28. Cyclophilin Inhibitor

    CypD-IN-29 is a selective inhibitor of Cyclophilin D (CypD), with a key dissociation constant (KD) of 88.2 nM. By targeting CypD, this compound interferes with its interaction with β-amyloid protein in mitochondrial environments, thereby mitigating the formation of mitochondrial permeability transition pores (mPTP). CypD-IN-29 is suited for research focused on Alzheimer's disease mechanisms and mitochondrial dysfunction in neuronal cells.
  29. Cyclophilin J Inhibitor

    ZX-J-19j is a selective inhibitor of cyclophilin J, a crucial target involved in various cellular processes. This compound exhibits potent antitumor activity, making it a valuable tool for cancer research. Its ability to modulate cyclophilin J function provides insights into tumor biology and potential therapeutic pathways.
  30. FAP Inhibitor

    UAMC-1110 is a highly potent and selective inhibitor of fibroblast activation protein (FAP), exhibiting an IC50 of 3.2 nM. In addition to FAP inhibition, UAMC-1110 also affects prolyl oligopeptidase (PREP) with an IC50 of 1.8 μM. This compound is primarily utilized in research applications targeting tumor microenvironment modulation and fibroblast-related pathologies.
  31. FAP Inhibitor

    AZD2389 is a potent and orally active inhibitor of fibroblast activation protein (FAP). It has demonstrated significant efficacy in research related to metabolic dysfunction-associated steatohepatitis. This compound serves as a valuable tool for studying the role of FAP in metabolic diseases and may aid in the development of therapeutic strategies aimed at targeting metabolic liver disorders.
  32. FAP Inhibitor

    FAP-IN-2 is a selective inhibitor of fibroblast activation protein (FAP), characterized by its isonitrile structure. This compound exhibits significant potential for therapeutic applications aimed at cancer treatment as well as for imaging purposes. When labeled with technetium-99m (99mTc), FAP-IN-2 can be utilized for targeted tumor single-photon emission computed tomography (SPECT) imaging, enhancing the visualization of FAP-expressing tumors.
  33. FAP Inhibitor

    ARI-3099 is a selective fibroblast activation protein (FAP) inhibitor that targets the proteolytic activity of FAP, preventing the cleavage of human FGF-21 between residues P171 and S172. By inhibiting this activity, ARI-3099 extends the half-life of circulating human FGF-21 in murine models. This compound is relevant for research focused on type 2 diabetes and various metabolic disorders, making it a valuable tool for investigating therapeutic strategies in these areas.
  34. FAP Inhibitor

    PNT6555 is a selective inhibitor of fibroblast activation protein-α (FAP), with notable antitumor activity. This compound is particularly valuable in the study of FAP-positive tumors, facilitating imaging applications that aid in tumor characterization and monitoring. Its specificity for FAP makes it a significant tool for cancer research, advancing the understanding of tumor microenvironments and potential therapeutic strategies.
  35. FAP Inhibitor

    DOTAGA-FAP-2286-ALB is a selective inhibitor of fibroblast activation protein (FAP) with an IC50 value of 67.5 nM. This compound enhances tumor retention through its interaction with albumin, thereby prolonging blood circulation and increasing the stability of radiometal complexes such as 111In and 225Ac. DOTAGA-FAP-2286-ALB is of particular interest for research applications in radionuclide therapy (TRT) targeting FAP-positive solid tumors.
  36. FAP Inhibitor

    FAPI-2 is a quinoline-based inhibitor targeting fibroblast activation protein (FAP). It exhibits rapid tracer kinetics and is suitable for use as a PET tracer in cancer diagnosis, labeled with 68Ga. Notably, FAPI-2 does not require fasting preparation and remains effective regardless of blood glucose levels, making it a valuable tool for oncological research and imaging applications.
  37. FAP Inhibitor

    FAP-IN-4 is a fibroblast activation protein (FAP) inhibitor that serves as an 18F-labeled PET tracer targeting FAP. This compound demonstrates significant potential in cancer research by facilitating the visualization of FAP-expressing tumors, thereby aiding in the understanding of tumor biology and treatment responses. It can be utilized in studies focused on tumor microenvironments and therapeutic interventions targeting FAP.
  38. FAP Inhibitor

    SB03178 is a selective inhibitor of fibroblast activation protein-alpha (FAP). This compound demonstrates significant potential in cancer research, particularly in modulating tumor microenvironments and enhancing the efficacy of cancer therapies. Additionally, SB03178 can be conjugated with DOTA for further applications in targeted imaging and therapeutic strategies.
  39. FAP Inhibitor

    FAP-IN-1 is a selective fibroblast activation protein (FAP) inhibitor that demonstrates potent activity with an IC50 value of 3.3 nM. This compound is valuable for investigating the role of FAP in the tumor microenvironment and its implications in cancer biology. FAP-IN-1 can be utilized in various research applications aimed at elucidating the mechanisms of tumor progression and the development of targeted therapeutic strategies.
  40. FAP Inhibitor

    QI-18 is a potent inhibitor of fibroblast activation protein (FAP) with an IC50 of 0.50 nM, exhibiting 6.5-fold increased potency compared to UAMC-1110. Its high affinity makes QI-18 suitable for the development of radiotracers with enhanced tumor selectivity and dosage for tumor diagnosis and research applications. This compound plays a significant role in studies focusing on tumor microenvironments and potential therapeutic interventions targeting FAP.
  41. FAP Inhibitor

    FAPI-P8PN is a selective inhibitor of fibroblast activation protein (FAP), exhibiting an IC50 value of 3.6 nM. This compound is particularly useful for investigating FAP-overexpressing solid tumors, providing insights into tumor microenvironments and potential therapeutic approaches. Its targeted activity makes it a valuable tool in cancer research aimed at developing FAP-focused therapies.
  42. FAP Inhibitor

    FAP-IN-8 is a selective inhibitor of fibroblast activation protein (FAP) and prolyl endopeptidase (PREP), exhibiting pIC50 values of 10.08 and 8.99 for these targets respectively. With IC50 values of 1 nM for FAP and 0.08 nM for PREP, FAP-IN-8 demonstrates potent inhibition that supports its utility in cancer research. This compound is valuable for studying tumor microenvironment interactions and the therapeutic targeting of cancer-associated fibroblasts.
  43. FAP Inhibitor

    FAP-IN-7 is a selective inhibitor of fibroblast activation protein (FAP), a serine protease implicated in tumor progression and immune modulation. This compound effectively hinders FAP activity, contributing to the investigation of cancer-associated fibroblasts in the tumor microenvironment. FAP-IN-7 is valuable for research applications focused on understanding cancer biology, developing therapeutic strategies, and exploring the role of FAP in various disease states.
  44. FAP Inhibitor

    DOTA-NI-FAPI-04 is a fibroblast activation protein (FAP) inhibitor with an IC50 of 7.44 nM, designed to enhance tumor uptake and retention using hypoxia-sensitive nitroimidazole groups. This compound forms stable complexes with metallic isotopes such as 68Ga and 177Lu through its DOTA moiety, serving as a foundation for the creation of radioactive probes ([68Ga]Ga/DOTA-NI-FAPI-04 and [177Lu]Lu/DOTA-NI-FAPI-04). DOTA-NI-FAPI-04 is valuable for research in cancer diagnostics, exploring the tumor microenvironment, and radionuclide therapy, particularly in the context of tumor stroma and hypoxic regions.
  45. FAP Inhibitor

    3BP-3580 is a potent inhibitor of fibroblast activation protein (FAP), exhibiting a pIC50 of 8.6. This compound is relevant for cancer research, specifically in studies investigating tumor microenvironments and the role of FAP in cancer progression. Its ability to modulate FAP activity makes it a valuable tool for exploring therapeutic strategies in oncology.
  46. FAP Inhibitor

    FAPI-X5 is a selective inhibitor of fibroblast activation protein (FAP) that binds to the catalytic domain, effectively disrupting its enzymatic activity through hydrogen bonding and π-π interactions. This compound exhibits significant cytostatic effects on glioblastoma tumors, resulting in reduced tumor growth without inducing regression. When radiolabeled with 68Ga, FAPI-X5 serves as a highly effective PET tracer, facilitating rapid tumor localization and high-contrast imaging in glioblastoma models. Additionally, FAPI-X5 can be labeled with 177Lu or 47Sc, functioning as a targeted radionuclide agent with extended tumor retention, making it valuable for glioblastoma research applications.
  47. FEN1 Inhibitor

    FEN1-IN-4 is a selective inhibitor of human flap endonuclease-1 (hFEN1), targeting the enzyme's crucial role in DNA replication and repair. This compound demonstrates significant biological activity by obstructing hFEN1's enzymatic function, which is essential for maintaining genomic stability. FEN1-IN-4 is valuable for research applications in cancer biology and the study of DNA repair mechanisms, providing insights into potential therapeutic strategies for related diseases.
  48. FLAP Inhibitor

    BRP-7 is a highly selective FLAP inhibitor with an IC50 of 0.31 μM. By targeting the 5-lipoxygenase activating protein (FLAP), BRP-7 effectively interrupts the co-localization of FLAP and 5-lipoxygenase, inhibiting the transfer of arachidonic acid and consequently reducing leukotriene production (IC₅₀ = 0.15 μM). It does not inhibit cyclooxygenase (COX-1/COX-2) or microsomal prostaglandin E₂ synthase-1 (mPGES-1), and maintains cell viability. BRP-7 has demonstrated significant anti-inflammatory properties in rodent models of pleurisy and peritonitis, making it a valuable tool for investigating inflammatory diseases.
  49. FEN1 Inhibitor

    FEN1-IN-2 is a selective inhibitor of flap endonuclease 1 (FEN1), demonstrating an IC50 of 3 nM. It exhibits significantly lower activity against XPG, with an IC50 of 226 nM. This compound is valuable for investigating FEN1's role in DNA repair processes and its potential implications in cancer research. Researchers can utilize FEN1-IN-2 to study mechanisms of cellular response to DNA damage and identify therapeutic strategies targeting FEN1-related pathways.
  50. FLAP Inhibitor

    Atuliflapon (AZD5718) is a potent, orally active inhibitor of FLAP (5-Lipoxygenase Activating Protein), exhibiting an IC50 of 2 nM. This compound is primarily utilized in research related to inflammatory processes, particularly in the context of coronary artery disease. Its selective inhibition of FLAP contributes to the regulation of leukotriene biosynthesis, making it a valuable tool for investigating therapeutic strategies for cardiovascular conditions.

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