| S7520 |
Darapladib (SB-480848)
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Darapladib is a reversible lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor with IC50 of 0.25 nM. Phase 3.
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Antimicrob Agents Chemother, 2025, e0047125.
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iScience, 2024, 27(12):111404
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iScience, 2024, 27(5):109774
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| S1110 |
Varespladib (LY315920)
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Varespladib (LY315920) is a potent and selective human non-pancreatic secretory phospholipase A2 (hnsPLA) inhibitor with IC50 of 7 nM, and it has reached Phase 3.
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Int J Mol Sci, 2024, 25(19)10649
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Front Immunol, 2022, 13:824746
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J Med Chem, 2019, 62(4):1999-2007
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| S7609 |
GW4869
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GW4869 (GW69A, GW554869A) is a neutral, noncompetitive inhibitor of sphingomyelinase (SMase) with an IC50 of 1 μM. It is selective for N-SMase, and does not inhibit acid SMase at up to at least 150 μM, also is a commonly used exosome inhibitor.
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J Extracell Vesicles, 2025, 14(2):e70042
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Proc Natl Acad Sci U S A, 2025, 122(8):e2421717122
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NPJ Biofilms Microbiomes, 2025, 11(1):113
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| S8011 |
U-73122
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U73122 is a potent phospholipase C (PLC) inhibitor, which reduces agonist-induced Ca2+ increases in platelets and PMN. U73122 potently inhibits human 5-lipoxygenase (5-LO).
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EMBO Rep, 2025, 10.1038/s44319-025-00444-2
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Front Immunol, 2025, 16:1491928
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Cancer Cell Int, 2025, 25(1):408
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| S2364 |
Tanshinone I
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Tanshinone I, an active principle isolated from Salvia miltiorrhiza (Danshen), is structurally similar to tanshinone IIA and may possess similar cytotoxic effects on tumor cells.
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Int J Oncol, 2023, 63(1)76
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Phytomedicine, 2022, 98:153958
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Drug Des Devel Ther, 2022, 16:3197-3213
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| S4255 |
Quinacrine 2HCl
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Quinacrine 2HCl(Quinacrine dihydrochloride) is a lipophilic cationic drug with multiple actions that is commonly used as an anti-protozoal agent. Quinacrine is an effective phospholipase A2 inhibitor.
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Molecules, 2022, 27(17)5561
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Toxicol In Vitro, 2022, 83:105420
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Mol Oncol, 2020, 10.1002/1878-0261.12853
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| S2390 |
(E/Z)-Polydatin
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(E/Z)-Polydatin is a mixture of cis- and trans-configurations of Polydatin.
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Heliyon, 2024, 10(21):e39933
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Biochem Biophys Res Commun, 2021, 556:149-155
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J Med Virol, 2019, 91(8):1440-1447
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| S9794 |
Melittin
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Melittin (MLT, Forapin, Forapine) is an activator of phospholipase A2 (PLA2) that stimulates the activity of the low molecular weight PLA2, while it does not the increase the activity of the high molecular weight enzyme.
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Mol Med Rep, 2025, 31(1)5
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Nutr Res Pract, 2024, 18(2):210-222
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EMBO J, 2022, e110439
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| S3220 |
Trigonelline
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Trigonelline (Trigenolline) is a plant alkaloid and a major component of coffee and fenugreek with anti-degranulation, anti-diabetic, antioxidant, anti-inflammatory, and neuroprotective effects. This compound inhibits FcεRI-mediated intracellular signaling pathways, such as phosphorylation of PLCγ1, PI3K, and Akt. It also inhibits the microtubule formation in RBL-2H3 cells.
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Int J Med Sci, 2025, 22(5):1194-1207
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Biochem Biophys Rep, 2025, 42:102021
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Biomed Pharmacother, 2021, 143:112204
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| S7321 |
FIPI
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FIPI (5-Fluoro-2-indolyl deschlorohalopemide), a derivative of halopemide, is a potent and selective inhibitor of phospholipase D with IC50 of 25 nM and 20 nM for PLD1 and PLD2, respectively.
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Cancer Cell Int, 2025, 25(1):408
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Cell Chem Biol, 2024, S2451-9456(24)00090-4
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