VU0285655-1 is a potent, selective inhibitor of PLD2, induces autophagy in colorectal cancer cells

(2E)-OBAA is a potent phospholipase A2 (PLA2) inhibitor, with an IC50 of 70 nM. (2E)-OBAA induces apoptosis of HUVEC cells. (2E)-OBAA blocks Melittin-induced Ca2+ influx in Trypanosoma brucei, with an IC50 of 0.4 μM.

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.

VU534 is a small molecule activator of N-acyl-phosphatidylethanolamine hydrolyzing phospholipase D (NAPE-PLD) with EC50 of 0.3 uM, enhances efferocytosis by macrophages.

VU533 is a small molecule activator of N-acyl-phosphatidylethanolamine hydrolyzing phospholipase D (NAPE-PLD) with EC50 of 0.3 uM, enhances efferocytosis by macrophages.

KT-203 (KT203) is a potent, selective inhibitor of α/β-hydrolase domain 6 (ABHD6) with IC50 of 3.9 nM in 2-AG hydrolysis assays.

ABD298 is a potent, selective ABHD13 inhibitor, inhibits HEK293T cells expressing recombinant mouse ABHD13 with IC50 of 0.98 uM.

LEI-401 is a first-in-class, selective, and CNS-active NAPE-PLD (N-acylphosphatidylethanolamine phospholipase D) inhibitor, with an IC50 of 27 nM. LEI-401 modulates emotional behavior in mice.

7-Hydroxycoumarinyl arachidonate (7-HCA) is a fluorogenic substrate of cytosolic phospholipase A2 (PLA2). 7-Hydroxycoumarinyl arachidonat e is also a fluorogenic substrate for monoacylglycerol lipase (MAGL). MAGL protein catalyzes the hydrolysis of 7-Hydroxycoumarinyl arachidonat to generate Arachidonic acid (AA) and the highly fluorescent 7-hydroxyl coumarin. Release of 7-HC can be measured using a fluorometer.

EA4, a derivative of quinone, is an inhibitor for both rPLA and cPLA. EA4 can inhibit rPLA2 with a Ki value of 130 μM. EA4 can be used for the research of hemostasis, thrombosis, and erythropoiesis.

Potent phosholipase D (PLD) inhibitor (IC50 values are 20 and 25 nM for PLD2 and PLD1 respectively).

ML 348(ML348) is a selective and reversible lysophospholipase 1 (LYPLA1) inhibitor (IC50 = 210 nM).

LY315920 (Varespladib) is a potent and selective human non-pancreatic secretory phospholipase A2 (hnsPLA) inhibitor with IC50 of 7 nM,. Phase 3.

Darapladib is a selective and orally active inhibitor of Lp-PLA2 (IC50= 270 pM)

CAY10590 (GK115) is an inhibitor of secreted phospholipase A2 (sPLA2) and can be used for the research of chronic inflammatory kidney diseases.

DPTIP-prodrug 18 (P18) is a orally active and brain-penetrable prodrug of DPTIP. DPTIP-prodrug 18 is a potent nSMase2 inhibitor. DPTIP-prodrug 18 significantly inhibits IL-1β-induced EV (extracellular vesicle) release by inhibition of nSMase2 (neutral sphingomyelinase-2) activity. DPTIP-prodrug 18 can be used for brain injury research.

Protizinic acid is an orally active non-steroidal antiinflammatory agent with antiinflammatory and antipyretic activity. Protizinic acid inhibits phospholipase A2 (PLA2) activity, and the IC50 value is 210 μM.

Luffariellolide is an inhibitor of human synovial fluid phospholipase A2 (HSF-PLA2) (IC50=5 μM). Luffariellolide effectively inhibits phorbol ester (PMA)-induced ear edema (ED50=50 μg/ear).

Lp-PLA2-IN-4 is a potent inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2). Lp-PLA2 previously known as platelet- activating factor acetylhydrolase (PAF-AH), is a phospholipase A2 enzyme involved in hydrolysis of lipoprotein lipids or phospholipids. Lp-PLA2-IN-4 has the potential for the research of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease (extracted from patent WO2021228159A1, compound 38).

Lp-PLA2-IN-5 is a potent inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2). Lp-PLA2 previously known as platelet- activating factor acetylhydrolase (PAF-AH), is a phospholipase A2 enzyme involved in hydrolysis of lipoprotein lipids or phospholipids. Lp-PLA2-IN-5 has the potential for the research of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease (extracted from patent WO2021228159A1, compound 32).

Lp-PLA2-IN-6 (compound 18), a tetracyclic pyrimidinone compound, is a potent Lp-PLA2 inhibitor with a pIC50 of 10.0 for rhLp-PLA2. Lp-PLA2-IN-6 has the potential for neurodegenerative related diseases research.

Lp-PLA2-IN-9 (compound 17), a tetracyclic pyrimidinone compound, is a potent Lp-PLA2 inhibitor with a pIC50 of 10.1 for rhLp-PLA2. Lp-PLA2-IN-9 has the potential for neurodegenerative related diseases research.

Lp-PLA2-IN-11 is a potent inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2). Lp-PLA2 previously known as platelet- activating factor acetylhydrolase (PAF-AH), is a phospholipase A2 enzyme involved in hydrolysis of lipoprotein lipids or phospholipids. Lp-PLA2-IN-11 has the potential for the research of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease (extracted from patent WO2014114249A1, compound E145).

PACOCF3 (Palmityltrifluoromet​hylketone) is a selective phospholipase A2 inhibitor with an IC50 of 3.8 μM. PACOCF3 alters Ca2+ signaling in renal tubular cells.

Vinaxanthone (SM-345431) is a potent and selective semaphorin3A inhibitor. Vinaxanthone exhibits semaphorin3A inhibiting activity with an IC50 of 0.1-0.2 μM. Vinaxanthone shows selective inhibitory activity against phospholipase C (PLC) from rat brain, mutine colon 26 Adenocarcinoma and murine fibroblasts NIH3T3 with IC50s being 5.4, 9.3 and 44 μM, respectively.

Lp-PLA2-IN-10 is a potent inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2). Lp-PLA2 previously known as platelet- activating factor acetylhydrolase (PAF-AH), is a phospholipase A2 enzyme involved in hydrolysis of lipoprotein lipids or phospholipids. Lp-PLA2-IN-10 has the potential for the research of neurodegenerative-related diseases such as Alzheimer's disease (AD), glaucoma, age-related macular degeneration (AMD), or cardiovascular diseases including atherosclerosis (extracted from patent WO2022001881A1, compound 4).

GSK2647544 is an orally available, selective inhibitor of Lp-PLA2. Lipoprotein-associated phospholipase (Lp-PLA2) is a calcium-independent phospholipase A2 with proinflammatory activities that is primarily secreted by monocyte-derived macrophages.

(S)-Bromoenol lactone ((S)-BEL) is an irreversible, chiral, mechanism-based inhibitor of calcium-independent phospholipase A2β (iPLA2β) that inhibits the vasopressin-induced release of arachidonate from cultured rat aortic smooth muscle (A10) cells with an IC50 of 2 µM.

CAY10502 is a potent, calcium-dependent cytosolic phospholipase A2 α (cPLA2α) inhibitor with an IC50 of 4.3 nM for isolated enzyme. CAY10502 can be used in the research of retinopathy and inflammatory diseases.

(R)-Bromoenol lactone ((R)-BEL) is an irreversible, chiral, mechanism-based inhibitor of calcium-independent phospholipaseγ(iPLA2γ)(/b). (R)-BEL inhibits human recombinant iPLA2γ with an IC50 of approximately 0.6 µM.