Phospholipase

Darapladib (SB-480848)(IC50=0.25 nM) is a substituted pyrimidone with inhibitory activity towards lipoprotein-associated phospholipase-A2 (Lp-PLA2).

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.

Neomycin sulfate (Framycin sulfate) is a broad-spectrum aminoglycoside antibiotic that blocks the synthesis of bacterial proteins in order to exert antimicrobial activity. Neomycin sulfate is commonly used to screen prokaryotic and eukaryotic cells for Neo resistance genes.

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

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.

CCR1/5/8 activator 1 is a cytoplasmic phospholipase A inhibitor with antifungal activity.

Indomethacin (Indometacin) is a Nonsteroidal Anti-inflammatory Drug. The mechanism of action of indomethacin is as a Cyclooxygenase Inhibitor.

Hnps-PLA Inhibitor is an inhibitor of human nonpancreatic secretory Phospholipase A (hnps-PLA).

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.

VU 0364739 hydrochloride (VU 0364739 HCl) is a selective and potent inhibitor of phospholipase D2 (PLD2) with IC50s of 20 and 1500 nM for PLD2 and PLD1, respectively.VU 0364739 hydrochloride exhibits potential anticancer activity and induces apoptosis. VU 0364739 hydrochloride has potential anticancer activity, induces apoptosis, and can be used in the study of cancer and metabolic-related diseases.

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.

Melittin Acetate (Forapin Acetate) is a PLA2 activator. Melittin Acetate stimulates the activity of the low molecular weight PLA2, while it does not increase the activity of the high molecular weight PLA2.

Melittin TFA is 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 m

BIRM 271 is a novel arachidonic acid release inhibitor that blocks leukotriene B4 and platelet-activating factor biosynthesis in human neutrophils. BIRM 271 and BIRM 270 are enantiomers that inhibit the production of leukotriene B4 with IC50 of 40 nM.

Lansoprazole sodium (Lansoprazole (sodium)) is a proton pump inhibitor (PPI) and a potent inhibitor of gastric acidity which is widely used in the therapy of gastroesophageal reflux and peptic ulcer disease.

9-Oxononanoic Acid is an oxidized fatty acid, formed by the autoxidation of linoleic acid, which enhances phospholipase A2 (PLA2) activity and increases the production of thromboxane B2 in isolated human plasma.9-Oxononanoic Acid reduces hepatic neofatty acid synthesis and enhances the activity of rat hepatic carnitine palmitoyltransferase, a marker of β-oxidation. Activity.

Anti-Inflammatory Peptide 1 Acetate (C45H82N12O14S2) possesses a potent anti-inflammatory activity in vivo and is a strong inhibitor of phospholipase A2 (PLA2), whose increased presence and activity results in inflammation and pain at certain bodily sites

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.

Lp-PLA2-IN-3 is a potent and orally bioactive lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor that inhibits recombinant human Lp-PLA2 with an IC50 value of 14 nM.

Ecopladib (PLA 725) is a sub-micromolar inhibitor of cytosolic phospholipase A2α (cPLA2α), with IC50s of 0.15 μM and 0.11 μM in the GLU micelle and rat whole blood assays, respectively.

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

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.

BMS493 is an inverse agonist of the pan-retinoic acid receptor (RAR) that inhibits retinoic acid-induced differentiation, enhances the interaction of nuclear co-inhibitors with RARs, attenuates RA signaling, potentiates TPP-induced toxicity, and inhibits the increase in phospholipase A2 activity.

5-HT1A modulator 1 displays very high affinities for the 5-HT1A, α1-adrenergic receptor, and D2 receptor (IC50s = 2 nM, 10 nM, and 40 nM).

ML299 (VU0463568) is a dual PLD1/2 inhibitor (PLD1 and PLD2, IC50 of 6 nM, 20 nM, respectively).

AACOCF3 (Arachidonyl trifluoromethyl ketone) is a cell-permeable trifluoromethyl ketone analog of arachidonic acid. It is a potent and 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. Moreover, AACOCF3 inhibits glucose-induced insulin secretion from isolated rat islets. Given its diverse applications, AACOCF3 holds promise for cardiovascular disease research.

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.

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.

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.

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

5alpha-Hydroxycostic acid possesses anti-angiogenic ability by interfering the VEGF- and Ang2-related pathways, and it may be a good drug candidate.

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

Niflumic acid (Nifluril) is a Ca2+-activated Cl- channel blocker and an analgesic and anti-inflammatory agent used in the therapy of rheumatoid arthritis.

U-73343 is an inactive analog of U-73122 and can be used as a negative control. It dose-dependently inhibits acid secretion irrespective of the stimulant. It is a phospholipase C (PLC) and 5-LO (5-lipoxygenase) inhibitor with an IC50 of 1-2.1 μM for PLC.

N-(p-amylcinnamoyl) Anthranilic Acid (ACA) is a broad spectrum Phospholipase A2 (PLA2) inhibitor and TRP channel blocker.

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

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

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)

ML348 (GNF-Pf-1127) is a selective and reversible lysophospholipase 1 (LYPLA1) inhibitor (IC50 = 210 nM).

LEI110 is a potent Phospholipase A2, group XVI (PLA2G16) inhibitor with an Ki value of 20 nM. LEI110 is a selective pan-inhibitor of the HRASLS family of thiol hydrolases (i.e., PLA2G16, HRASLS2, RARRES3 and iNAT).

A4333, a biotinylated derivative of A3373, selectively inhibits Phospholipase D1 (PLD1) while sparing PLD2. It is noted for its significant role in antitumor activity [1].

FAAH/cPLA2α-IN-1 is a compound that simultaneously inhibits both FAAH and cPLA2α, demonstrating potent activity with half-maximal inhibitory concentrations (IC50s) of 32 nM for FAAH and 47 nM for cPLA2α [1].

A3373 is a novel inhibitor targeting both Phospholipase D1 (PLD1) and Phospholipase D2 (PLD2), demonstrating half maximal inhibitory concentrations (IC50) of 325 nM for PLD1 and 15.15μM for PLD2. This compound effectively suppresses lipopolysaccharide (LPS)-induced immune responses and is implicated in key processes of autoimmune arthritis, bone demineralization, and osteoclastogenesis [1] [2].

Lp-PLA2-IN-14 (Compound 19), an inhibitor of rhLp-PLA2, exhibits a potent inhibitory effect with a pIC50 value of 8.4. This compound is applicable in research pertaining to neurodegenerative disorders, including Alzheimer Disease (AD), glaucoma, age-related macular degeneration (AMD), and cardiovascular diseases such as atherosclerosis [1].

Lp-PLA2-IN-15 (example 2) is an inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2) with potential application in Alzheimer's disease research [1].

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

ASM-IN-1 is a potent, orally active inhibitor of acid sphingomyelinase (ASM) with an IC50 of 1.5 µM, demonstrating antiatherosclerotic and anti-inflammatory activity. It effectively reduces lipid plaques in the aortic arch and aorta, along with decreasing plasma ceramide concentrations and oxidized LDL (Ox-LDL) levels [1].

Carbazochrome (Adchnon) is an antihemorrhagic, or hemostatic, agent that will cease blood flow by causing the aggregation and adhesion of platelets in the blood to form a platelet plug, ceasing blood flow from an open wound. It is hoped that this drug can be used in the future for preventing excessive blood flow during surgical operations and the treatment of hemorrhoids, but research on its effectiveness and the severity of possible side effects remains to be fairly inconclusive. Carbazochrome has been investigated for use in the treatment of hemorrhoids in a mixture with troxerutin.

ML-095 hydrochloride (CID-25067483 hydrochloride) is a specific placental alkaline phosphatase inhibitor. It inhibits PLAP, TNAP and IAP with IC50 of 2.1, >100 and 53 μM, respectively.