Phospholipases

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  1. HnsPLA inhibitor

    LY315920 (Varespladib) is an inhibitor of the IIa, V, and X isoforms of secretory phospholipase A2 (sPLA2).
  2. PLA inhibitor

    Polydatin protects cerebral cells from ischemic damages via improvement of microcirculation and inhibition of platelet aggregation. In addition, polydatin inhibits ICAM-1 expression in endothelial cells stimulated by lipopolysaccharide; it also attenuates adhesion between white blood cells and endothelial cells.
  3. MAO-B inhibitor

    Quercetin inhibits many enzyme systems including tyrosine protein kinase, phospholipase A2, phosphodiesterases, mitochondrial ATPase, PI 3-kinase and protein kinase C.
  4. MAO-B inhibitor

    Quercetin inhibits many enzyme systems including tyrosine protein kinase, phospholipase A2, phosphodiesterases, mitochondrial ATPase, PI 3-kinase and protein kinase C.
  5. Phospholipase inhibitor

    Tanshinones are the major bioactive compounds of Salvia miltiorrhiza Bunge (Danshen) roots, which are used in many therapeutic remedies in Chinese traditional medicine.
  6. PC-PLC inhibitor

    D609 is a selective competitive phosphatidyl choline-specific phospholipase C (PC-PLC) inhibitor (Ki = 6.4 μM); antiviral and antitumor agent.
  7. PC-PLC inhibitor

    SPK-601 (LMV-601) is an inhibitor of the phosphatidylcholine-specific phospholipase C (PC-PLC). SPK-601 also can be used as an antimicrobial agent.
  8. APT-2 inhibitor

    ML349 is a potent and specific acyl protein thioesterase 2 (APT-2) inhibitor with a Ki of 120 nM. ML349 is also an inhibitor of LYPLA2 with an IC50 of 144 nM.
  9. Lipoprotein-Associated Phospholipase A2 (Lp-PLA2) inhibitor

    Rilapladib is a selective Lipoprotein-Associated Phospholipase A2 (Lp-PLA2) inhibitor with an IC50 of 230 pM.
  10. PLD inhibitor

    Isoforms of phospholipase D (PLD) cleave the head group from phospholipids, releasing the second messenger phosphatidic acid (PA), which can produce changes in Ras activation, cell spreading, stress fiber formation, chemotaxis, and membrane vesicle trafficking. FIPI is a derivative of halopemide which potently inhibits both PLD1 (IC50 = 25 nM) and PLD2 (IC50 = 20 nM).
  11. Lp-PLA2 Inhibitor

    Darapladib is a reversible lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor .
  12. Phospholipase C inhibitor

    U 73122 is a phospholipase C inhibitor. It inhibits agonist-induced platelet aggregation with IC50 values of 1-5 uM.
  13. LYPLA1 inhibitor

    ML348 is a selective and reversible lysophospholipase 1 (LYPLA1) inhibitor (IC50 = 210 nM), Exhibits 14-fold selectivity for LYPLA1 over LYPLA2, Also selective over a panel of ~30 other serine hydrolases.
  14. PTK inhibitor

    ST271 is a potent inhibitor of protein tyrosine kinase (PTK), inhibits phospholipase D activation stimulated by fMet-Leu-Phe and PAF, with IC50s of 6.7 and 9 μM, respectively.
  15. NAPE-PLD inhibitor

    ARN19874 is a selective, reversible uncompetitive N-acylphosphatidylethanolamine phospholipase D (NAPE-PLD) activity inhibitor with an IC50 of ~34 μM.
  16. cPLA2 and iPLA2 inhibitor

    MAFP (Methyl Arachidonyl Fluorophosphonate) is an selective, active-site directed and irreversible inhibitor of cPLA2 and iPLA2. MAFP is also a potent irreversible inhibitor of anandamide amidase.
  17. PLC-γ inhibitor

    3-Nitrocoumarin (3-NC) is a potent and selective Phospholipase C-γ (PLC-γ) inhibitor.
  18. PLC inhibitor

    U-73343, an inhibitor of PLC (putative phospholipase C)-dependent processes, is an analog of U-73122 and can be used as a negative control.
  19. PLD1 inhibitor

    VU0155069 (CAY10593), compound 69, is a selective phospholipase D1 (PLD1) inhibitor with an IC50 value of 46 nM in vitro.
  20. sPLA2-X inhibitor

    sPLA2-X Inhibitor 31 is a selective secreted phospholipase A2 type X (sPLA2-X) inhibitor with IC50s of 26 nM, 310 nM, and 2230 nM for sPLA2-X, sPLA2-IIa, and sPLA2-V, respectively.
  21. ACDase inhibitor

    LCL521 is an acid ceramidase (ACDase) inhibitor. LCL521 also inhibits the lysosomal acid sphingomyelinase (ASMase).
  22. phospholipase A2 inhibitor

    Varespladib methyl (A-002; LY333013) is a selective inhibitor of group II secretory phospholipase A2 (PLA2).
  23. Phospholipase D2 (PLD2) inhibitor

    ML298 (CID53393915) is a potent, specific inhibitor of Phospholipase D2 (PLD2) with IC50 of 355 nM.
  24. rabbit platelet sPLA2 inhibitor

    YM-26734 is a rabbit platelet sPLA2 inhibitor that has been used to ameliorate local inflammatory responses in TPA-induced mouse ear edema.
  25. Hnps-PLA Inhibitor

    MDK-8582, also known as Hnps-PLA Inhibitor, is an inhibitor of human nonpancreatic secretory Phospholipase A (hnps-PLA). The best one inhibited hnps-PLA(2) and LTA(4)H-h with IC(50) values of 9.2 ± 0.5 μM and 2.4 ± 1.4 μM, respectively.
  26. phospholipase A2/HDAC2 inhibitor

    Rhamnetin is a naturally occurring flavonoid and quercetin derivative found in *Coriandrum sativum*. It functions as an inhibitor of secretory phospholipase A₂ and histone deacetylase 2 (HDAC2), contributing to its broad pharmacological profile. Rhamnetin exhibits notable antitumor, antioxidant, and anti-inflammatory activities, making it a promising compound for research in cancer, oxidative stress-related conditions, and inflammatory diseases.
  27. Phospholipase C Inhibitor, Angiogenesis Modulator

    Neomycin sulfate is a phospholipase C inhibitor that modulates angiogenesis through its influence on calcium signaling pathways. This aminoglycoside antibiotic disrupts bacterial protein synthesis by binding irreversibly to the 30S ribosomal subunit. In addition to its antibacterial properties, neomycin sulfate effectively inhibits angiogenin-mediated nuclear translocation, cell proliferation, and angiogenesis. It also disrupts inositol trisphosphate (IP3)-mediated calcium release and electrical excitation-evoked calcium transients in skeletal muscle. Neomycin sulfate is utilized in cancer research and studies related to calcium signaling and angiogenesis.
  28. Phospholipase A2 Inhibitor

    (2E)-OBAA is a selective inhibitor of phospholipase A2 (PLA2) with an IC50 value of 70 nM. This compound effectively induces apoptosis in human umbilical vein endothelial cells (HUVECs) and demonstrates its capacity to inhibit melittin-induced Ca2+ influx in Trypanosoma brucei, exhibiting an IC50 of 0.4 μM. (2E)-OBAA is valuable for research focused on cell signaling, apoptosis, and parasitology.
  29. Phospholipase D Inhibitor

    PLD-IN-1 is a selective inhibitor of phospholipase D, exhibiting an IC50 of 1.97 μM. This compound reduces the expression of immune evasion markers such as CD24, CD47, and PD-L1 while promoting calreticulin, thereby enhancing phagocytosis of lung cancer cells by macrophages. PLD-IN-1 demonstrates significant cytotoxic effects on various lung cancer cell lines, including A549, HCC44, H460, and HCC15, with IC50 values ranging from 18.44 to 24.85 μM. Additionally, it induces apoptosis, inhibits cell migration, enhances M1 macrophage polarization, and exhibits antitumor efficacy in mouse models, making it a valuable tool for cancer research.
  30. Phospholipase A2 Inhibitor

    OBAA is a potent inhibitor of phospholipase A2 (PLA2), exhibiting an IC50 of 70 nM. This compound effectively blocks Melittin-induced calcium influx in Trypanosoma brucei, demonstrating an IC50 of 0.4 μM. OBAA is valuable for research applications aimed at understanding the role of PLA2 in various biological processes and cellular responses.
  31. Semaphorin3A/Phospholipase C/FabI Inhibitor

    Vinaxanthone is a selective inhibitor of semaphorin3A, phospholipase C (PLC), and FabI, exhibiting IC50 values of 0.1-0.2 μM for semaphorin3A and 0.9 mM for FabI. This compound also inhibits the substrate t-o-NAC thioester and the cofactor NADPH, with inhibition constants (Kis) of 3.1 μM and 1.0 μM, respectively. Vinaxanthone shows potential for combating infections caused by multidrug-resistant pathogens, making it a valuable tool for research in infectious diseases and drug resistance mechanisms.
  32. Phospholipase C Inhibitor, Angiogenesis Modulator

    Neomycin is an aminoglycoside antibiotic known for its role as a phospholipase C (PLC) inhibitor and angiogenesis modulator. It effectively inhibits the nuclear translocation of angiogenin, resulting in reduced cell proliferation and angiogenesis. Additionally, Neomycin interferes with IP3-mediated calcium release and MgATP-dependent calcium uptake, influencing skeletal muscle calcium transients. Its ability to modulate crucial biological pathways makes Neomycin a valuable tool for cancer research and understanding microbial impact on health. Prolonged exposure may lead to adverse effects such as hearing impairment and kidney damage.
  33. Phospholipase D Inhibitor

    Halopemide is a potent inhibitor of phospholipase D (PLD), exhibiting IC50 values of 220 nM for human PLD1 and 310 nM for PLD2. In addition to its enzymatic inhibition, Halopemide functions as a dopamine receptor antagonist and exhibits psychotropic properties. This reagent is valuable for research applications exploring PLD-mediated signaling pathways and dopamine receptor interactions in various biological contexts.
  34. Phospholipase Inhibitor

    ML-211 is a carbamate-based inhibitor targeting acyl-protein thioesterase 1 (APT1) and lysophospholipase 1 (LYPLA1), with an IC50 of 17 nM, as well as lysophospholipase 2 (LYPLA2) with an IC50 of 30 nM. Additionally, it inhibits the serine hydrolase ABHD11 at an IC50 of 10 nM while demonstrating greater than 50-fold selectivity for LYPLA in a diverse panel of 20 serine hydrolases. ML-211 is valuable for research involving lipid metabolism and signaling pathways, particularly those associated with phospholipase activity.
  35. cPLA2 Inhibitor

    AACOCF3, or Arachidonyl trifluoromethyl ketone, is a potent and selective inhibitor of cytosolic phospholipase A2 (cPLA2), exerting its effects through slow binding interactions. This compound is capable of blocking the production of both arachidonate and 12-hydroxyeicosatetraenoic acid in platelets stimulated by calcium ionophores. Additionally, AACOCF3 has been shown to inhibit glucose-induced insulin secretion from isolated rat islets, suggesting its potential utility in studying pathways related to cardiovascular disease and metabolic regulation.
  36. PLA2 Inhibitor

    Pyrrophenone is a highly selective inhibitor of cytosolic phospholipase A2α (cPLA2α), exhibiting an IC50 value of 4.2 nM. This compound is valuable for research on phospholipid metabolism and inflammatory processes, as cPLA2α plays a critical role in the release of arachidonic acid and the production of inflammatory mediators. Pyrrophenone can be used to study the physiological effects of cPLA2α inhibition in various cellular and animal models.
  37. PGAM5 Inhibitor

    LFHP-1c is a selective inhibitor of PGAM5, known for its neuroprotective properties in the context of brain ischemic stroke. This compound enhances the integrity of the blood-brain barrier by preventing ischemia-induced damage. LFHP-1c functions by binding to endothelial PGAM5, thereby inhibiting its phosphatase activity and disrupting its interaction with NRF2. It demonstrates protective effects both in vitro and in vivo, making it a valuable tool for research on ischemic conditions and related therapeutic strategies.
  38. N-SMase 2 Inhibitor

    DPTIP is a selective inhibitor of neutral sphingomyelinase 2 (N-SMase 2), demonstrating a potent inhibitory activity with an IC50 of 30 nM. This compound effectively penetrates the blood-brain barrier, making it a valuable tool for studying the biological roles of N-SMase 2 in various neurobiological processes. Its application in research includes investigating exosome biogenesis and sphingolipid metabolism, providing insights into cellular signaling pathways in neurological disorders.
  39. NAPE-PLD Inhibitor

    LEI-401 is a selective inhibitor of N-acylphosphatidylethanolamine phospholipase D (NAPE-PLD), exhibiting an IC50 of 27 nM. This CNS-active compound has been shown to modulate emotional behavior in mice, making it a valuable tool for research into neurochemistry and behavioral science. Its unique mechanism of action positions LEI-401 as a candidate for exploring therapeutic pathways in mood disorders and related conditions.
  40. Phospholipase Inhibitor

    Bromoenol lactone is a selective and potent irreversible inhibitor of calcium-independent phospholipase A2 (iPLA2β), exhibiting an IC50 of approximately 7 μM. This compound effectively inhibits antigen-stimulated mast cell exocytosis without interfering with calcium influx. Bromoenol lactone is valuable for research applications aimed at understanding the roles of phospholipases in cellular processes and inflammatory responses.
  41. sPLA2 Inhibitor

    Tris(2,4-di-tert-butylphenyl)phosphate is a potent inhibitor of secretory Phospholipase A2 (sPLA2), demonstrating significant anti-inflammatory activity. Isolated from the leaves of Vitex negundo L., this compound has been supported by molecular docking studies that confirm its inhibitory effects. It is particularly useful in research applications focused on inflammatory processes and lipid metabolism.
  42. PLC-γ Inhibitor

    CCT129957 is a selective inhibitor of phospholipase C-γ (PLC-γ) with an IC50 of approximately 3 μM, demonstrating significant potency. This indole derivative effectively inhibits Ca2+ release in squamous carcinoma cells at a concentration of around 15 μM. CCT129957 is valuable for research applications targeting PLC-γ signaling pathways, providing insights into cellular function and disease mechanisms.
  43. Phospholipase Inhibitor

    1-Naphthaleneacetic acid is an auxin that primarily acts as a phospholipase A2 (PLA2) inhibitor, exhibiting an IC50 of 13.16 μM. This compound is instrumental in promoting plant growth by modulating hormone levels and enhancing cell elongation. Additionally, its role in inhibiting PLA2 has made it a valuable tool in studying signaling pathways and inflammation in various biological systems.
  44. Phospholipase Inhibitor

    MJ33 lithium salt is a competitive, reversible inhibitor targeting phospholipase A2 (PLA2). This compound specifically inhibits calcium-independent phospholipase A2 (iPLA2) activity of Prdx6, making it a valuable tool for researching phospholipid signaling pathways. MJ33 is utilized in studies focused on inflammation and cell signaling related to phospholipid metabolism.
  45. PTDSS1 Inhibitor

    DS55980254 is an orally active inhibitor of phosphatidylserine synthase 1 (PTDSS1), effectively blocking the synthesis of intracellular phosphatidylserine. Inhibition of PTDSS1 disrupts the balance of cell membrane phospholipid components, which can subsequently activate B cell receptor (BCR) signaling pathways. This compound is valuable for research focused on phospholipid metabolism and its implications in B cell signaling and immune responses.
  46. SMS1 Inhibitor

    SMS1-IN-1 is a potent sphingomyelin synthase 1 (SMS1) inhibitor with an IC50 of 2.1 μM. This compound demonstrates significant biological activity relevant to lipid metabolism and cellular signaling pathways. SMS1-IN-1 is primarily utilized in research focused on atherosclerosis, offering insights into its molecular mechanisms and potential therapeutic strategies.
  47. PLA2 Inhibitor

    ONO-RS-082 is a selective inhibitor of phospholipase A2 (PLA2), demonstrating an IC50 of 1.0 μM. This compound uniquely lacks activity against phospholipase C (PLC), even at concentrations up to 100 μM. ONO-RS-082 is applicable for research involving the modulation of PLA2 activity and can facilitate studies related to inflammatory processes and cell membrane dynamics.
  48. PLD2 Inhibitor

    VU0364739 is a selective inhibitor of phospholipase D2 (PLD2) with an IC50 of 22 nM. This compound has been shown to decrease cancer cell proliferation, making it a valuable tool for studying the role of PLD2 in tumor biology. Its application in cancer research allows for further exploration of the molecular mechanisms underlying cell growth and proliferation.
  49. sPLA2 Inhibitor

    KH064 is a potent inhibitor of secretory phospholipase A2 (sPLA2), specifically targeting human nonpancreatic secretory PLA2 isoform IIa (hnpsPLA2-IIa) with an IC50 of 29 nM. This D-tyrosine derivative exhibits significant anti-inflammatory activity, making it suitable for research applications in inflammation and related disease models. Its oral bioavailability further enhances its potential for in vivo studies in pharmacological and toxicological research.
  50. ASM Inhibitor

    ASM-IN-1 is a potent inhibitor of acid sphingomyelinase (ASM) with an IC50 value of 1.5 µM. It exhibits significant bioactivity by reducing lipid plaques in the aortic arch and aorta, as well as decreasing plasma ceramide concentration and oxidized low-density lipoprotein (Ox-LDL) levels. ASM-IN-1 demonstrates antiatherosclerotic and anti-inflammatory properties, making it valuable for research in cardiovascular diseases and lipid metabolism.

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