Phospholipase Inhibitor

GW4869 is a noncompetitive neutral sphingomyelinase (N-SMase) inhibitor with an IC₅₀ of 1 μM. GW4869 is an inhibitor of exosome biogenesis/release.

BAPTA is a selective and cell-impermeant chelator for calcium. BAPTA has high selectivity against magnesium and calcium. BAPTA can also inhibit phospholipase C activity independently of their role as Ca²⁺ chelators.

Darapladib (SB-480848) is an orally active, selective and reversible Lp-PLA2 inhibitor (IC₅₀=0.25 nM). Darapladib can trigger irreversible actions on glioma cell apoptosis and induce cycle arrest. Darapladib can be used in the study of atherosclerosis and cancer.

ML348 (GNF-Pf-1127) is a selective and reversible acyl-protein thioesterase 1 (APT1)/lysophospholipase 1 (LYPLA1) inhibitor with an IC₅₀ of 210 nM, and barely inhibits LYPLA2.

(E/Z)-BML264 (N-(p-amylcinnamoyl) Anthranilic Acid) is a broad spectrum Phospholipase A₂ (PLA₂) inhibitor and TRP channel blocker. (E/Z)-BML264 is a SLC13A3 inhibitor. (E/Z)-BML264 (N-(p-amylcinnamoyl) Anthranilic Acid) is also an effective reversible inhibitor of calcium-activated chloride channels, has potential to treat arrhythmia.

CDIBA is a cytosolic phospholipase A2 (cPLA2) inhibitor. CDIBA inhibits the activation of cPLA2 in rat diaphragm tissue. CDIBA reduces the level of mitochondrial reactive oxygen species in rat diaphragm tissue after prolonged mechanical ventilation. CDIBA attenuates protein degradation, muscle atrophy and decreased muscle strength in the diaphragm of rats after prolonged mechanical ventilation. CDIBA can be used in studies related to ventilator-induced diaphragmatic dysfunction.

Compound 48/80 trihydrochloride (C48/80 trihydrochloride) is a mixture of condensation products of N-methyl-p-methoxyphenethylamine with formaldehyde. Compound 48/80 trihydrochloride is also a histamine releaser and a mast cell degranulator. Compound 48/80 inhibits phosphatidylinositol-specific phospholipase C activity from human platelets .

ML349 is a potent and specific acyl protein thioesterase 2(APT2)/lysophospholipase 2 (LYPLA2) inhibitor with a K_i of 120 nM. ML349 is also an inhibitor of LYPLA2 with an IC₅₀ of 144 nM.

AACOCF3 (Arachidonyl trifluoromethyl ketone) is a cell-permeant trifluoromethyl ketone analog of arachidonic acid. AACOCF3 is a potent and selective slow binding inhibitor of the 85-kDa cytosolic phospholipase A2 (cPLA2). AACOCF3 blocks production of arachidonate and 12-hydroxyeicosatetraenoic acid by calcium ionophore-challenged platelets. AACOCF3 inhibits glucose-induced insulin secretion from isolated rat islets. AACOCF3 has the potential for the research of cardiovascular disease.

Lansoprazole (AG 1749) is an orally active proton pump inhibitor which prevents the stomach from producing acid. Lansoprazole (AG 1749) is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).

m-3M3FBS is a potent phospholipase C (PLC) activator. m-3M3FBS stimulates superoxide generation in human neutrophils, upregulates intracellular calcium concentration, and stimulates inositol phosphate generation in various cell lines. m-3M3FBS induces monocytic leukemia cell apoptosis.

D609, an antitumoural xanthate, is a specific and competitive phosphatidyl choline-specific phospholipase C (PC-PLC) inhibitor with a K_i of 6.4 μM. D609 is an antioxidative protector and has antiviral and anti-inflammatory activity.

Ly93 is a selective and orally active sphingomyelin synthase 2 (SMS2) inhibitor, with an IC₅₀ of 91 nM.

CAY10650 is a highly potent cytosolic phospholipase A2α (cPLA2α) inhibitor with an IC₅₀ value of 12 nM. CAY10650 suppresses lipid droplets formation and PGE2 secretion.

LFHP-1c is an PGAM5 inhibitor with neuroprotective activity in brain ischemic stroke. LFHP-1c protects blood-brain barrier integrity from ischemia-induced injury. LFHP-1c binds to endothelial PGAM5 to inhibit the activity of PGAM5 phosphatase and the interaction of PGAM5 with NRF2. LFHP-1c exhibits in vitro and in vivo protection.

Malabaricone C is an orally active and noncompetitive sphingomyelin synthase (SMS) inhibitor with IC₅₀ values of 3 μM and 1.5 μM for SMS 1 and SMS 2, respectively. Malabaricone C reduces body weight gain, improves glucose tolerance, and decreases lipid accumulation in the liver, showing significant prevention of high fat diet-induced fatty liver in mice. Malabaricone C has anti-inflammatory effects, which is found in the fruits of Myristica cinnamomea King. Malabaricone C is promising for research of obesity and immunological disorders caused due to hyper-activation of T-cells.

Manumycin A is a polyketide antibiotic and an inhibitor of thioredoxin reductase 1 (TrxR-1). Manumycin A can inhibit the growth of breast cancer cells and exert its anti-tumor activity through LC3. Manumycin A can downregulate the release of pro-inflammatory cytokines in human monocytes stimulated by TNF α, and has potential anti-inflammatory activity. Manumycin A can inhibit the Ras/Raf/ERK1/2 signaling and hnRNP H1 in castration resistant prostate cancer cells to suppress exosome biogenesis and secretion.

Tanshinone I is an inhibitor of type IIA human recombinant sPLA₂ (IC₅₀=11 μM) and rabbit recombinant cPLA₂ (IC₅₀=82 μM).

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

DPTIP is a potent brain penetrant neutral sphingomyelinase 2 (N-SMase 2) inhibitor (exosome inhibitor), with an IC₅₀ of 30 nM.