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.

Neomycin sulfate, an aminoglycoside antibiotic, exerts antibacterial activity through irreversible binding of the nuclear 30S ribosomal subunit, thereby blocking bacterial protein synthesis. Neomycin sulfate is a known phospholipase C (PLC) inhibitor. Neomycin sulfate potently inhibits both the nuclear translocation of angiogenin and angiogenin-induced cell proliferation and angiogenesis. Neomycin sulfate inhibits IP3-mediated Ca²⁺ release, MgATP-dependent Ca²⁺ uptake, and electrical excitation-evoked skeletal muscle Ca²⁺ transients. Neomycin sulfate depletes gut microbiota in specific mouse models, causes hearing impairment, and kidney damage with prolonged exposure. Neomycin sulfate can be used for the research of cancer.

U-73122 is a phospholipase C (PLC) and 5-LO (5-lipoxygenase) inhibitor with an IC₅₀of 1-2.1 µM for PLC.

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.

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.

Varespladib (LY315920) is a potent and selective group IIA, secretory phospholipase A₂ (sPLA₂) inhibitor with an IC₅₀ of 9 nM. Varespladib exhibits the significant inhibitory effect on sPLA2 activity in serum from various species including rat, rabbit, guinea pig and human with IC₅₀s of 8.1 nM, 5.0 nM, 3.2 nM and 6.2 nM, respectively.

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.

D-Erythro-dihydrosphingosin directly inhibits cytosolic phospholipase A₂α (cPLA₂α) activity.

Pyrrophenone is a potent and specific cytosolic phospholipase A₂α (cPLA₂α) inhibitor with an IC₅₀ value of 4.2 nM.

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.

FIPI is a phospholipase D (PLD) inhibitor with an IC₅₀ for PLD1 and PLD2 of about 25 nM. FIPI regulates cytoskeletal recombination, cell diffusion and chemotaxis. FIPI can be used in cancer research. In addition, FIPI can enhance the secretion and aggregation of platelet dense particles, inhibit thrombosis, reduce ischemic stroke infarct volume and improve nerve function.

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.