Phospholipase

Phospholipase A2 (PLA2) is an enzyme that hydrolyzes fatty acids present in the sn-2 position of phospholipids, and is closely related to lipid metabolism and immune function.

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.

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.

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.

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

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

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)

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

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.

Omeprazole Sodium is a proton pump inhibitor(PPI) and suppresses gastric acid secretion. Omeprazole Sodium is a potent neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor). Omeprazole Sodium shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM. Omeprazole Sodium inhibits growth of Gram-positive and Gram-negative bacteria.

Difluprednate (Myser)(Durezol) is a corticosteroid, approved for the treatment of post-operative ocular inflammation and pain.

BAPTA is a neuroprotective agent in cerebral ischemia, acting as an intercellular Ca2+ chelator.

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

trans-Benzylideneacetone (Acetocinnamone) is used in various synthetic preparations.

1-Naphthaleneacetic acid (Transplantone) , is widely used in agriculture for various purposes. It is a synthetic plant hormone in the auxin family and is an ingredient in many commercial plant rooting horticultural products.

ST271 is an effective protein tyrosine kinase (PTK) 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.

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.

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.

CCT129957 is a novel and potent phospholipase C-γ (PLC-γ) inhibitor with an IC50 of about 3 μM and a GC50 of 15 μM.CCT129957 exhibits anticancer activity and inhibits Ca2+ release in squamous cells.

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.

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).

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.