Phospholipase

Darapladib (SB-480848) is a lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor with an IC50 value of 0.25 nM, which can exert cardiovascular protective effects [1,3].

GW4869 (GW69A) is a selective and non-competitive inhibitor of neutral sphingomyelinase N-SMase (IC50=1 μM). GW4869 also inhibits exosome synthesis release and is commonly used in exosome-related studies.Usually prepared as a suspension for experiments.

Giripladib (PLA695)(PLX-695) is a cPLA2-specific inhibitor that inhibits the radiation-induced increase of phosphorylated ERK and phosphorylated Akt in endothelial cells.

Varespladib methyl (LY333013), a bioavailable prodrug of Varespladib, is a selective group II secretory phospholipase A2 inhibitor.

Varespladib (LY315920), a specific and effective human non-pancreatic secretory phospholipase A2 (hnsPLA) inhibitor(IC50=7 nM), has been investigated for the treatment and prevention of sickle cell disease, vaso-occlusive crisis, and acute coronary syndrome.

Vinaxanthone (SM-345431) is a small molecule compound derived from Penicillium chrysogenum that acts as a selective and potent inhibitor of semaphorin3A, phospholipase C (PLC), and FabI, exhibiting antimicrobial activity by blocking intracellular fatty acid synthesis and inhibiting the growth of Staphylococcus aureus.

Rilapladib (SB 659032) is a selective inhibitor of Lipoprotein-Associated Phospholipase A2 (Lp-PLA2, IC50 = 230 pM) and acts as an antagonist of the platelet-activating factor receptor.

ML348 (GNF-Pf-1127) is a selective, reversible inhibitor of lysophospholipase 1 (LYPLA1) with an IC50 of 210 nM.

DPTIP is an effective inhibitor of neutral sphingomyelinase 2 with an IC50 value of 30 nM.

Melittin, a small protein containing 26 amino acid residues, is the principal toxic component of bee venom. Melittin is a PLA2 activator, stimulates the activity of the low molecular weight PLA2, while it does not the increase activity of the high molecul

Amentoflavone (3',8''-Biapigenin), as a potent inhibitor of CYP3A4 and CYP2C9, can interact with many other medications. CYP3A4 and CYP2C9 are proteins used for drug metabolism in the body. Amentoflavone also is an inhibitor of human cathepsin B. It has antimalarial activity in trials significant affinities towards the Delta-1, kappa opioid receptors (as an antagonist) and binds to benzodiazepine receptors. Amentoflavone may be a potential lead for a new type of anti-inflammatory agents having the dual inhibitory activity of group II phospholipase A2 and cyclooxygenase. Amentoflavone and quercetin differentially exerted suppression of PGE2 biosynthesis via downregulation of COX-2/iNOS expression.

Tris(2,4-di-tert-butylphenyl)phosphate (TDTBPP) isolated from Vitex negundoL inhibits secretory phospholipase A2 (sPLA2). Tris(2,4-di-tert-butylphenyl)phosphate has anti-inflammatory activity.

Rhamnetin (beta-Rhamnocitrin), a quercetin derivative found in Coriandrum sativum, has antioxidant and anti-inflammatory activities. Rhamnetin inhibits secretory phospholipase A2.

VU0359595 (ML-270) is a potent and selective pharmacological phospholipase D1 (PLD1) inhibitor with an IC50 of 3.7 nM. VU0359595 is >1700-fold selective for PLD1 over PLD2 (IC50 of 6.4 μM). VU0359595 can be used for the research of cancer, diabetes, neurodegenerative and inflammatory diseases.

Fuzapladib (IS-741) (IS-741) is a phospholipase A2 inhibitor that can inhibits the expression of Mac-1, a cell adhesion molecule. Fuzapladib blocks activation of adhesion molecules (integrin) expressed on the inflammatory cell surface to prevent inflammatory cells from adhering to vascular endothelial cells and infiltrating tissue and to control exacerbation of pancreatitis.

Tanshinone I (Tanshinone A), an active principle isolated from the herbal medicine Salvia miltiorrhiza, displays cytotoxicity against tumor cells.

U-73122 (U73122) , an effective PLC inhibitor, reduces agonist-induced Ca2+ increases in platelets and PMN.

Omeprazole (Losec) is a proton pump inhibitor (PPI), Omeprazole(Losec) is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).

VU0285655-1(BML-280) is a potent and selective phospholipase D2 (PLD2) inhibitor that inhibits the proliferation of PLD2-deficient cells.VU0285655-1 has an inhibitory effect on high glucose-induced caspase-3 cleavage and reduction of cell viability.VU0285655-1 is used in the study of diabetic retinopathy.

ML-298 (CID53393915) is a potent, specific inhibitor of Phospholipase D2 (PLD2, IC50 of 355 nM).

VU534 is a NAPE-PLD agonist with an EC50 of 0.30 μM.VU534 is a dual inhibitor of FAAH and sEH, with an IC50 of 1.2 μM for sEH.VU534 is used in diseases related to cardiometabolism.

Indomethacin (Indomethacin) is a COX1 and COX2 inhibitor (IC50=18 26 nM) with blood-brain barrier permeability and non-selectivity. Indomethacin is a non-steroidal anti-inflammatory agent with anti-tumor and anti-infective activity.

D-Erythro-dihydrosphingosine (C18-Dihydrosphingosine) inhibits arachidonic acid release and cPLA2α activity.

Quinacrine dihydrochloride (Mepacrine dihydrochloride) is the dihydrochloride salt of the 9-aminoacridine derivative quinacrine with potential antineoplastic and antiparasitic activities.

ML349 is an inhibitor of LYPLA2 (IC50: 144 nM). ML349 is an effective and specific acyl protein thioesterase 2 (APT-2) inhibitor (Ki: 120 nM).

Maltoheptaose (aka amyloheptaose) is a activater of phosphorylase B specifically to prepare (neurosin)heptulose-2-phosphate.

CAY10594 is a potent phospholipase D2(PLD2) inhibitor. CAY10594 ameliorates acetaminophen-induced acute liver injury by regulating the phosphorylated-GSK-3β JNK axis.

m-3M3FBS is a phospholipase C (PLC) activator.

FIPI (5-Fluoro-2-indolyl deschlorohalopemide) is a derivative of halopemide which potently inhibits both PLD1 (IC50 = 25 nM) and PLD2 (IC50 = 20 nM); prevents PLD regulation of F-actin cytoskeleton reorganization, cell spreading, and chemotaxis.

Lansoprazole (A-65006) is a 2, 2, 2-trifluoroethoxypyridyl derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS. Lansoprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)

Fluticasone propionate (CCI-187881), derived from fluticasone used to remedy asthma and allergic rhinitis, is a high affinity, selective GR (glucocorticoid receptor) agonist.

Cambinol (SIRT1/2 Inhibitor IV) is a cell-permeable b-naphthol compound that inhibits the NAD-dependent deacetylase activity of SIRT1/2 (IC50: 56/59 μM, respectively) in a substrate-, but not NAD-, competitive manner. Cambinol inhibits SIRT5 deacetylase activity only at much higher concentrations (IC50 >300 μM) and no inhibitory for the class I and II HDACs. In BCL6-expressing Burkitt lymphoma cell lines, Cambinol-induced apoptosis has been attributed to the hyperacetylation of p53 and BCL6.Cambinol is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)

1-Linoleoyl Glycerol (Monolinolein) is fatty acid glycerol that has been isolated from Saururus Chinensis roots. The (R)-1-Linoleoyl Glycerol and (S)-1-Linoleoyl Glycerol exhibit Lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitory activities with IC50 values of 45.0 and 52.0 μM, respectively.

Compound 48 80 trihydrochloride (C48 80 trihydrochloride) is a mixture of N-methyl-p-methoxyphenethylamine and formaldehyde produced via a condensation reaction. It acts as a mast cell degranulator and histamine releaser and inhibits phosphatidylinositol-specific phospholipase C activity in human platelets.

Linocinnamarin (3-[4-(beta-D-Glucopyranosyloxy)phenyl]acrylic acid methyl ester) is isolated from Fragaria ananassa Duch. (strawberry). The inhibition of antigen-stimulated degranulation by LN is mainly due to inactivation of Syk/phospholipase Cgamma (PLCgamma) pathways.

MAFP (Methyl Arachidonyl Fluorophosphonate) is an effective, active-site directed irreversible inhibitor of anandamide amidase, cPLA2, and iPLA2.

VU533 (Nape-Pld activator) is a NAPE-PLD activator with an EC50 value of 0.30 µM.VU533 enhances NAPE-PLD activity and increases macrophage cytosolic burial.VU533 may be used in diseases associated with cardiometabolism.

Lp-PLA2-IN-1 (Lp-PLA2 inhibitor 1) suppresses Lp-PLA2 activity processes for their preparation. Lp-PLA2-IN-1 (Lp-PLA2 inhibitor 1) also inhibits to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example, atherosclerosis, Alzheimer's disease.

LEI-401 is a selective and potent NAPE-PLD inhibitor that crosses the blood-brain barrier (IC50: 27 nM).LEI-401 reduces the level of n-acylethanolamines (NAEs) in the brain of free-ranging mice and modulates their emotional behaviour.

Bromoenol lactone ((6E)-Bromoenol lactone) is a selective calcium-dependent phospholipase A2 (iPLA2β) and serine protease inhibitor that attenuates nicotine-induced breast cancer cell proliferation and migration, inhibits voltage-gated Ca2+ and transient receptor potential classical channels, and inhibits carrageenan-induced prostaglandin production and hyperalgesia in rat hind paws.

Halopemide is a potent inhibitor of PLD (IC50 = 220 and 310 nM for human PLD1 and PLD2). Halopemid is an antagonist of dopamine receptors. Halopemid can be used in psychotropic research.

Levamisole hydrochloride ((-)-Tetramisole hydrochloride) is an antihelminthic drug that has been tried experimentally in rheumatic disorders where it apparently restores the immune response by increasing macrophage chemotaxis and T-lymphocyte function. Paradoxically, this immune enhancement appears to be beneficial in rheumatoid arthritis where dermatitis, leukopenia, and thrombocytopenia, and nausea and vomiting have been reported as side effects.

3-Nitrocoumarin (3-nitrochromen-2-one) (3-NC) is a potent and selective Phospholipase C-γ (PLCγ) inhibitor.

AACOCF3 (Arachidonyl trifluoromethyl ketone) is a cell-permeable trifluoromethyl ketone analog of arachidonic acid and a potent, selective slow binding inhibitor of the 85-kDa cytosolic phospholipase A2 (cPLA2). By blocking the production of arachidonate and 12-hydroxyeicosatetraenoic acid in calcium ionophore-challenged platelets, AACOCF3 hinders their synthesis. Additionally, AACOCF3 inhibits glucose-induced insulin secretion from isolated rat islets, making it promising for cardiovascular disease research.

Rapanone (2,5-Dihydroxy-3-tridecyl-[1,4]benzoquinone) is a natural benzoquinone that is a potent and selective inhibitor of human synovial PLA2.

CAY10650 is an effective inhibitor of cytosolic phospholipase A2α (cPLA2α, IC50: 12 nM).

VU0155069 strongly inhibits the invasive migration of several cancer cell lines in transwell assays. VU0155069 is a selective phospholipase D1 inhibitor (IC50: 46 nM in vitro).

AA26-9 is an effective and broad-spectrum inhibitor of serine hydrolase.