Phospholipases

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  1. Phospholipase A2 Inhibitor

    PACOCF3 (Palmityltrifluoromethylketone) is a selective inhibitor of phospholipase A2, demonstrating an IC50 of 3.8 μM. This compound effectively modulates Ca2+ signaling within renal tubular cells, making it a valuable tool for studying phospholipase A2-related pathways and their implications in renal physiology and pathology. Researchers can utilize PACOCF3 to explore therapeutic interventions in conditions mediated by altered phospholipid metabolism.
  2. Lp-PLA2 Inhibitor

    GSK2647544 is an orally available, selective inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2). This enzyme is a calcium-independent phospholipase A2 involved in proinflammatory processes, primarily secreted by monocyte-derived macrophages. GSK2647544 demonstrates potential for modulation of inflammatory pathways and is applicable in research focusing on cardiovascular diseases and inflammatory disorders.
  3. Serine Hydrolases Inhibitor

    ABC47 is a potent inhibitor of serine hydrolases, specifically targeting ABHD4 and ABHD3, with IC50 values of 0.03 μM and 0.1 μM, respectively. This compound plays a significant role in research related to infantile neuronal ceroid lipofuscinosis, making it a valuable tool for studying the mechanisms and treatment of this neurodegenerative disorder. Its specificity and potency facilitate investigations into serine hydrolase functions and their implications in various biological processes.
  4. cPLA2 Inhibitor

    Giripladib is an indole-based inhibitor of cytosolic phospholipase A2 (cPLA2). It demonstrates potent inhibitory activity against cPLA2, making it a valuable tool for investigating inflammatory processes. Giripladib is applicable in research focused on osteoarthritis and breast cancer, facilitating studies on the role of phospholipase A2 in these conditions.
  5. cPLA2α Inhibitor

    CAY10502 is a potent inhibitor of calcium-dependent cytosolic phospholipase A2 α (cPLA2α), exhibiting an IC50 of 4.3 nM in isolated enzyme assays. This compound is valuable for research into retinopathy and inflammatory diseases, highlighting its potential role in modulating lipid metabolism and inflammation pathways. Its specificity and efficacy provide a useful tool for elucidating cPLA2α's involvement in various pathological processes.
  6. Lp-PLA2 Inhibitor

    SB-435495 is a potent and selective inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2), exhibiting reversible and non-covalent binding with an IC50 of 0.06 nM. This compound demonstrates significant anti-inflammatory properties and is utilized in research related to cardiovascular diseases and atherosclerosis. Its oral bioavailability makes it a valuable tool for studying Lp-PLA2's role in various disease models.
  7. Phospholipase Inhibitor

    1-Naphthaleneacetic acid potassium salt is a synthetic auxin that primarily inhibits phospholipase A2 (PLA2) with an IC50 of 13.16 μM. This compound is utilized in plant biology to promote growth and development, as well as in biochemical studies to explore the role of PLA2 in cellular processes. Its ability to modulate enzymatic activity makes it a valuable tool in both agricultural research and molecular biology investigations.
  8. sPLA2 Inhibitor

    Varespladib sodium is a highly selective inhibitor of group IIA secretory phospholipase A2 (sPLA2), exhibiting an IC50 of 9 nM. This compound demonstrates significant inhibition of sPLA2 activity in serum from multiple species, including rat, rabbit, guinea pig, and human, with reported IC50 values of 8.1 nM, 5.0 nM, 3.2 nM, and 6.2 nM, respectively. Varespladib sodium is instrumental in studying inflammatory processes and lipid metabolism, making it valuable for research applications related to cardiovascular diseases and other sPLA2-mediated conditions.
  9. nSMase2 Inhibitor

    nSMase2-IN-1 is an orally active inhibitor of Neutral sphingomyelinase 2 (nSMase2), exhibiting an IC50 value of 0.13 ± 0.06 μM. This compound demonstrates metabolic stability in liver microsomes and possesses a favorable brain-to-plasma ratio, making it suitable for studies involving central nervous system diseases. nSMase2-IN-1 is a valuable reagent for research applications focused on elucidating the role of sphingolipid metabolism in neurological disorders.
  10. Phospholipase Inhibitor

    Aristolochic acid C is a potent inhibitor of phospholipase A2 (PLA2), a key enzyme involved in various inflammatory processes. This compound has demonstrated the ability to disrupt cortical microtubule arrays, thereby influencing cellular structure and root growth in Arabidopsis. Its applications extend to studies in plant biology and the investigation of signaling pathways mediated by phospholipase activity.
  11. sPLA2 Inhibitor

    LY-311727 is a potent inhibitor of secretory non-pancreatic phospholipase A2 (sPLA2), demonstrating an IC50 of less than 1 μM for group IIA sPLA2. This compound functions by blocking the enzymatic activity of sPLA2, which plays a critical role in proinflammatory processes. LY-311727 is valuable for research focused on the modulation of inflammation and the investigation of sPLA2-related biological pathways.
  12. Phospholipase Inhibitor

    (S)-Bromoenol lactone is an irreversible inhibitor targeting calcium-independent phospholipase A2β (iPLA2β). It effectively reduces the vasopressin-induced release of arachidonate from cultured rat aortic smooth muscle (A10) cells, demonstrating an IC50 of 2 µM. This compound serves as a valuable tool for studying phospholipase activity and its role in various cellular processes.
  13. Secreted Phospholipases A2 Inhibitor

    N-Palmitoyl-l-leucine is an inhibitor of secreted phospholipases A2, targeting the hydrolysis of membrane phospholipids. This compound exhibits significant anti-inflammatory properties and is valuable in research applications related to inflammatory diseases and conditions associated with phospholipase activity. Its ability to modulate inflammatory responses makes it a useful tool for studying mechanisms of inflammation and potential therapeutic interventions.
  14. Phospholipase Inhibitor

    A3373 is a novel inhibitor of Phospholipase D1 (PLD1) and Phospholipase D2 (PLD2), exhibiting IC50 values of 325 nM and 15.15 μM, respectively. This compound effectively inhibits lipopolysaccharide (LPS)-induced immune responses, making it valuable for research in autoimmune arthritis, bone demineralization, and osteoclastogenesis. Its action on phospholipase pathways underscores its potential for studying related inflammatory and osteological disorders.
  15. Lp-PLA2 Inhibitor

    Lp-PLA2-IN-13 is a selective inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2). This compound exhibits strong inhibitory activity, making it a valuable tool for investigating neurodegenerative diseases. It serves as a potential therapeutic candidate for research focused on the modulation of inflammatory processes associated with neurodegeneration.
  16. aSMase Inhibitor

    C10 Bisphosphonate is a potent inhibitor of acid sphingomyelinase (aSMase) with an IC50 value of 0.02 μM in rat models. This compound demonstrates significant effectiveness in preventing Dexamethasone-induced apoptosis and mitigating platelet-activating factor (PAF)-induced pulmonary edema. C10 Bisphosphonate serves as a valuable tool for research focused on pulmonary edema and related cellular mechanisms.
  17. Phospholipase Inhibitor

    Lp-PLA2-IN-3 is a powerful inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2), exhibiting an IC50 of 14 nM against recombinant human Lp-PLA2 (rhLpPLA2). This compound demonstrates significant biological activity in modulating inflammation and atherosclerosis-associated pathways. It is applicable in research focused on cardiovascular diseases and other conditions linked to phospholipid metabolism.
  18. Phospholipase Inhibitor

    PDDC is a selective phospholipase inhibitor, specifically targeting neutral sphingomyelinase 2 (nSMase2). This compound effectively reduces tau-induced nSMase2 activity and mitigates ceramide elevation, thereby slowing tau propagation in mouse models. PDDC is utilized in research related to Alzheimer's disease, providing insights into the modulation of neurodegenerative pathways.
  19. EA4

    rPLA/cPLA Inhibitor

    EA4 is a quinone derivative that acts as an inhibitor of both secretory and cytosolic phospholipase A2 (rPLA and cPLA). It exhibits rPLA2 inhibition with a Ki value of 130 μM, making it a valuable tool for investigating the mechanisms of hemostasis, thrombosis, and erythropoiesis. This compound aids in the study of lipid metabolism and its implications in various physiological and pathological processes.
  20. PLCδ1 Inhibitor

    N-Stearoylsphingomyelin is a sphingolipid that acts as an inhibitor of Phospholipase Cδ1 (PLCδ1). This compound plays a significant role in modulating cellular signaling pathways and is valuable in studying the physiological effects of PLCδ1 inhibition. Its applications include research in cell biology, signal transduction, and neurobiology, making it a useful reagent for investigating various biological processes.
  21. sPLA2-IIA Inhibitor

    Ochnaflavone is a potent inhibitor of IIA-type secretory phospholipase A2 (sPLA2-IIA) with an IC50 value of 3.45 µM. It demonstrates notable anti-inflammatory and hepatoprotective properties, effectively inhibiting both phosphatidylethanolamine (PE) degradation and carbon tetrachloride (CCl4)-induced lipid peroxidation in rat liver, with an IC50 of 7.16 µM for lipid peroxidation. Ochnaflavone is valuable in research related to liver injury and inflammatory conditions.
  22. sPLA Inhibitor

    LY433771 is a selective inhibitor of type X secretory phospholipase A2 (sPLA2), exhibiting an IC50 value of 3 nM. This compound is valuable for research applications focused on cardiovascular diseases, facilitating the investigation of sPLA2's role in lipid metabolism and inflammatory processes. Its potent inhibition makes it a crucial tool for understanding the underlying mechanisms of cardiovascular pathologies.
  23. sPLA2 Inhibitor

    (Z)-Oleyloxyethyl phosphorylcholine is a selective inhibitor of secreted Phospholipase A2 (sPLA2), an enzyme that plays a crucial role in the production of proinflammatory lipid mediators. This compound is valuable for investigating inflammatory diseases and their underlying mechanisms. Additionally, (Z)-OPC has been shown to modify red blood cell membranes and can be utilized in the development of oxygen-carrying liquids, such as perfluorocarbons, for applications in reducing toxin-induced hemolysis.
  24. cPLA2α Inhibitor

    Efipladib is a selective inhibitor of cytosolic phospholipase A2 alpha (cPLA2α) with an IC50 of 0.04 μM and a Kd of 0.067 μM. This compound demonstrates significant inhibition of arachidonic acid release, contributing to its potential in modulating inflammatory responses. Efipladib is valuable for research applications aimed at understanding cPLA2α-driven pathways in various disease models, including neuroinflammation and cardiovascular conditions.
  25. PLA2 Inhibitor

    MJ33-OH lithium is a metabolite of MJ33 and serves as a specific inhibitor of phospholipase A2 (PLA2). Acting as a competitive and reversible inhibitor, MJ33-OH lithium effectively blocks the activity of calcium-independent phospholipase A2 (iPLA2), particularly in the context of Prdx6. This compound is valuable for research applications focused on inflammation, cellular signaling, and lipid metabolism.
  26. PLD2 Inhibitor

    VU 0364739 hydrochloride is a selective inhibitor of phospholipase D2 (PLD2), exhibiting an IC50 of 20 nM for PLD2 while having significantly lower activity against PLD1 (IC50 of 1500 nM). This compound has been shown to induce apoptosis, making it a valuable reagent for cancer research. Its specificity and potent biological activity position VU 0364739 as an important tool for studying PLD2's role in cellular processes and cancer pathophysiology.
  27. Phospholipases A Inhibitor

    ROC-0929 is a potent and selective inhibitor of secreted phospholipases A2 (sPLA2s), specifically targeting hGX with an IC50 of 80 nM. By inhibiting the phosphorylation of ERK1/2 and p-38, ROC-0929 demonstrates significant anti-inflammatory activity. This compound holds promise for investigating the role of sPLA2s in inflammation-related diseases, making it a valuable tool for research in this area.
  28. Phospholipase Inhibitor

    Ecopladib is a selective inhibitor of cytosolic phospholipase A2α (cPLA2α), exhibiting sub-micromolar potency with IC50 values of 0.15 μM and 0.11 μM in GLU micelle and rat whole blood assays, respectively. This compound effectively modulates the release of arachidonic acid and subsequent eicosanoid synthesis, making it a valuable tool for studying inflammatory processes. Ecopladib is applicable in research focused on the mechanisms of inflammation and related pathways.
  29. GVIA iPLA2 Inhibitor

    FKGK11 is a potent and selective inhibitor of GVIA iPLA2 (Group VIA calcium-independent phospholipase A2). It exhibits significant biological activity by modulating phospholipid metabolism, making it a valuable tool for studying ovarian cancer and neurological disorders, including peripheral nerve injury and multiple sclerosis. Researchers can utilize FKGK11 to explore the roles of iPLA2 in disease mechanisms and therapeutic interventions.
  30. GVIA iPLA2 Inhibitor

    GK187 is a potent and selective inhibitor of Group VIA calcium-independent phospholipase A2 (GVIA iPLA2), exhibiting an XI(50) value of 0.0001. This compound demonstrates significant biological activity and potential for research in various neurological disorders, allowing for deeper insights into phospholipid metabolism and its implications in neurobiology. Its selectivity makes it a valuable tool for investigating the roles of GVIA iPLA2 in cellular processes and disease mechanisms.
  31. sPLA2 Inhibitor

    AZD2716 is a selective inhibitor of secretory phospholipase A2 (sPLA2), specifically targeting sPLA2-IIa, sPLA2-V, and sPLA2-X with IC50 values of 10 nM, 40 nM, and 400 nM, respectively. By effectively reducing pro-inflammatory lipid production, AZD2716 diminishes macrophage activation and foam cell formation. This compound is valuable for investigating the pathways involved in atherosclerosis and various inflammatory diseases linked to sPLA2 activity.
  32. iPLA2γ Inhibitor

    (R)-Bromoenol lactone is an irreversible chiral inhibitor targeting calcium-independent phospholipase γ (iPLA2γ). It exhibits potent inhibition of human recombinant iPLA2γ, with an IC50 value of approximately 0.6 µM. This compound is significant for research applications involving lipid signaling, inflammatory responses, and cellular metabolism.
  33. PLD Inhibitor

    FIPI hydrochloride is a potent inhibitor of phospholipase D (PLD), exhibiting an IC50 of approximately 25 nM for both PLD1 and PLD2. This compound plays a critical role in regulating cytoskeletal reorganization, cell migration, and chemotactic responses, making it valuable for cancer research. Additionally, FIPI hydrochloride enhances the secretion and aggregation of platelet dense granules, contributes to thrombosis inhibition, reduces infarct volume in ischemic stroke models, and promotes recovery of neuronal function.
  34. Lp-PLA2 Inhibitor

    Lp-PLA2-IN-2 is a potent and selective inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2), exhibiting an IC50 of 120 nM for recombinant human Lp-PLA2. This small molecule plays a significant role in modulating lipid metabolism and inflammatory processes associated with cardiovascular disease. It is valuable for research applications focused on understanding the biological implications of Lp-PLA2 in various pathophysiological conditions.
  35. Lp-PLA2 Inhibitor

    Lp-PLA2-IN-5 is a selective inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2), an enzyme implicated in the hydrolysis of lipoprotein and phospholipids. This compound demonstrates significant potential in research focused on various diseases related to Lp-PLA2 activity, including atherosclerosis and Alzheimer's disease. Its inhibition of Lp-PLA2 may provide insights into therapeutic strategies for managing lipid-related pathologies.
  36. Lp-PLA2 Inhibitor

    Lp-PLA2-IN-4 is a potent inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2), an enzyme that plays a crucial role in the hydrolysis of lipoprotein lipids and phospholipids. This compound is valuable for investigating the biological effects of Lp-PLA2 in various pathological conditions, including atherosclerosis and Alzheimer's disease. Research applications include elucidating the enzyme's role in lipid metabolism and inflammation pathways.
  37. Phospholipase A2 Iinhibitor

    Plipastatin A1 is a lipopeptide that serves as an inhibitor of phospholipase A2. It demonstrates significant inhibitory effects on the conidial germination of Botrytis cinerea, leading to a reduction in the occurrence of gray mold on tomato leaves. This compound is valuable for research focused on agricultural pathogens and plant protection strategies against gray mold disease.
  38. PLD Inhibitor

    VU0155069 hydrochloride is a potent and selective inhibitor of phospholipase D (PLD), with IC50 values of 46 nM for PLD1 and 933 nM for PLD2. This compound effectively inhibits the migration of both human and mouse breast cancer cell lines, making it a valuable tool for studying the role of PLD in cancer biology. Its unique mechanism of action allows researchers to explore therapeutic strategies targeting PLD-related pathways in oncology.
  39. Lp-PLA2 Inhibitor

    SB-435495 hydrochloride is a highly potent and selective inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2), characterized by its reversible and non-covalent action. With an IC50 value of 0.06 nM, it demonstrates significant inhibitory efficacy, making it a valuable tool for research into cardiovascular diseases and inflammatory conditions. This compound is suitable for studies focused on the role of Lp-PLA2 in atherosclerosis and other lipid metabolism-related disorders.
  40. LYPLA1/LYPLA2 Inhibitor

    ML378 is a dual inhibitor of LYPLA1 and LYPLA2, demonstrating IC50 values of 122 nM and 245 nM, respectively. In addition, ML378 exhibits potent inhibition of ABHD6 with an IC50 of 3.15 nM. This compound is valuable for investigating the physiological and pathological roles of LYPLA1 and LYPLA2 in various biological processes and disease models.
  41. Lp-PLA2 Inhibitor

    Lp-PLA2-IN-11 is a potent inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2), an enzyme involved in the hydrolysis of lipoprotein lipids. This compound demonstrates significant biological activity, making it a valuable tool for exploring the role of Lp-PLA2 in various pathological conditions, including atherosclerosis and Alzheimer’s disease. Lp-PLA2-IN-11 is suitable for research applications focused on the modulation of lipoprotein metabolism and the investigation of Lp-PLA2's contribution to disease progression.
  42. nSMase2 Inhibitor

    DPTIP-prodrug 18 is an orally active prodrug that demonstrates high brain penetrability and functions as a potent nSMase2 inhibitor. It effectively inhibits IL-1β-induced release of extracellular vesicles by targeting and inhibiting the activity of neutral sphingomyelinase-2. This compound is suitable for research in brain injury studies, providing insights into the molecular mechanisms of neuroinflammation and extracellular signaling.
  43. Lp-PLA2 Inhibitor

    Lp-PLA2-IN-9 is a tetracyclic pyrimidinone compound that functions as a potent inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2), exhibiting a pIC50 of 10.1 for recombinant human Lp-PLA2. This compound demonstrates significant biological activity that may be valuable in the study of neurodegenerative diseases and related pathologies, making it a useful tool for research aimed at understanding Lp-PLA2's role in neuroinflammation and its therapeutic potential.
  44. PLA2 Inhibitor

    Ikshusterol 3-O-glucoside is a potent phospholipase A2 (PLA2) inhibitor derived from plant sources. This compound exhibits significant biological activity by effectively modulating inflammatory responses associated with PLA2 activity. Its applications in research include studying snake venom toxicity and exploring anti-inflammatory pathways, making it a valuable tool for investigations into immune response and venom pharmacology.
  45. Lp-PLA2 Inhibitor

    Lp-PLA2-IN-17 is a selective inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2). This compound is utilized in research to investigate the role of Lp-PLA2 in the hydrolysis of oxidized lipids, leading to the production of inflammatory mediators. Lp-PLA2-IN-17 is valuable in studying various inflammatory disorders and cardiovascular diseases linked to lipid metabolism.
  46. cPLA2 Inhibitor

    AX048 is a selective inhibitor of calcium-dependent phospholipase A2 (cPLA2), exhibiting a potent inhibitory effect with an XI(50) of 0.022 mole fraction. This compound demonstrates significant antihyperalgesic efficacy, making it a valuable tool for research into pain mechanisms and inflammatory pathways. AX048 is applicable in studies focusing on neuropathic pain and the modulation of lipotoxicity-related conditions.
  47. cPLA2 Inhibitor

    BMS-229724 is a potent, orally active inhibitor of cytosolic phospholipase A2 (cPLA2), exhibiting an IC50 of 2.8 μM. This compound effectively inhibits the production of arachidonic acid and eicosanoids in various cell types, including U937 cells, neutrophils, and platelets. With demonstrated anti-inflammatory properties, BMS-229724 is valuable for research into skin inflammation and related inflammatory diseases.
  48. cPLA2α Inhibitor

    WAY-196025 is a selective, orally active inhibitor of cytosolic phospholipase A2 alpha (cPLA2α) with an IC50 of 0.01 μM and a Kd of 0.013 μM. This compound effectively inhibits the production of inflammatory mediators, including prostaglandins and leukotrienes, which are crucial in inflammatory responses. WAY-196025 is valuable for research applications in inflammation and immunology, particularly in studies related to asthma and other inflammatory diseases.
  49. Lp-PLA2 Inhibitor

    Lp-PLA2-IN-10 is a potent inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2), an enzyme involved in the hydrolysis of lipoprotein lipids and phospholipids. This compound exhibits significant biological activity in the context of neurodegenerative diseases, including Alzheimer's disease, as well as ophthalmic conditions such as glaucoma and age-related macular degeneration. Additionally, Lp-PLA2-IN-10 may have implications in cardiovascular research, particularly in relation to atherosclerosis.
  50. Lp-PLA2 Inhibitor

    ML256 is a covalent inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2), a key enzyme involved in lipid metabolism and inflammation. This compound exhibits biological activity by selectively targeting Lp-PLA2, making it valuable in the investigation of neoplasms with constitutively active variants of KRAS or HRAS. It is useful for research applications focusing on cancer biology and the modulation of inflammatory pathways.

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