Phospholipase Inhibitor

Avenanthramide C is an orally active polyphenolic compound that penetrates the blood-brain barrier. Avenanthramide C is derived from oats. Avenanthramide C inhibits NF-κB nuclear translocation and inhibits the phosphorylation of PI3K, PLCγ1, Lyn, Syk, and Akt. Avenanthramide C inhibits the expression and activity of MMP-9 and inhibits MAPK phosphorylation. Avenanthramide C scavenges DPPH radicals, reduces intracellular ROS, and inhibits pro-inflammatory cytokine release and adhesion molecule expression. Avenanthramide C inhibits cell degranulation. Avenanthramide C attenuates active systemic anaphylaxis and inhibits passive cutaneous anaphylaxis. Avenanthramide C ameliorates PHZ-induced blood stasis. Avenanthramide C inhibits neuroinflammation, restores long-term potentiation, and improves recognition and spatial memory in Alzheimer's disease models. Avenanthramide C can be used for research on allergic inflammation, thrombosis, atherosclerosis, and Alzheimer's disease.

CAY10502 is a potent, calcium-dependent cytosolic phospholipase A2 α (cPLA₂α) inhibitor with an IC₅₀ of 4.3 nM for isolated enzyme. CAY10502 can be used in the research of retinopathy and inflammatory diseases.

Varespladib methyl (A-002; LY333013) is a selective inhibitor of group II secretory phospholipase A2 (PLA2).

RHC 80267 (U-57908) is a potent and selective inhibitor of diacylglycerol lipase (DAGL) (with IC₅₀ of 4 μM in canine platelets). RHC-80267 inhibits cholinesterase activity with an IC₅₀ of 4 μM, thereby enhancing the relaxation evoked by acetylcholine. RHC 80267 also inhibits COX and the hydrolysis of phosphatidylcholine (PC).

Varespladib sodium (LY315920 sodium) is a potent and selective group IIA, secretory phospholipase A₂ (sPLA₂) inhibitor with an IC₅₀ of 9 nM. Varespladib sodium 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.

Giripladib (PLA-695) is a selective cPLA_2α inhibitor. Giripladib attenuates CKD serum-induced PUFA accumulation, MDA and ROS levels, restores the GSH/GSSG ratio, and alleviates mitochondria-Ferroptosis-related morphological changes. Giripladib exhibits anti-inflammatory and disease-modifying effects in collagen-induced arthritis. Giripladib can be used in research on chronic kidney disease-associated plaque vulnerability, rheumatoid arthritis, and breast cancer.

LY-311727 is a potent secretory non-pancreatic phospholipase A₂ (sPLA₂) inhibitor (IC₅₀ <1 μM for group IIA sPLA₂). sPLA₂ is an important proinflammatory enzyme.

Benzylideneacetone (Benzalacetone) is an orally active antibiotic, tyrosinase inhibitor, phospholipase A₂ inhibitor, and immunosuppressant. Benzylideneacetone has antibacterial activity against some gram-negative plant-pathogenic bacteria. Benzylideneacetone can also be used in the synthesis of chemicals and drugs, and as a flavoring additive for some foods.

GSK2647544 is an orally available, selective inhibitor of Lp-PLA2. Lipoprotein-associated phospholipase (Lp-PLA2) is a calcium-independent phospholipase A2 with proinflammatory activities that is primarily secreted by monocyte-derived macrophages.

ABC47 is a potent inhibitor of serine hydrolases. ABC47 shows IC₅₀s of 0.03 and 0.1 μM for ABHD4 and ABHD3, respectively. ABC47 plays an important role in infantile neuronal ceroid lipofuscinosis research.

Choline tosylate (Choline p-toluenesulfonate) is an intermediate and also a substrate of choline acetyltransferase (CHAT). Choline tosylate inhibits phospholipase A2 and phospholipase C.

Rapanone is a natural benzoquinone. Rapanone exhibits a broad spectrum of biological actions, including anti-tumor, antioxidant, anti-inflammatory, antibacterial and antiparasitic. Rapanone also is a potent and selective human synovial PLA₂ inhibitor, with an IC₅₀ of 2.6 μM.

trans-Benzylideneacetone (trans-Benzalacetone), a metabolite of gram-negative entomopathogenic bacterium Xenorhabdus nematophila, is an enzyme inhibitor against phospholipase A2 (PLA2). trans-Benzylideneacetone is an immunosuppressant.

Lp-PLA2-IN-13 (compound 15) is a potent Lp-PLA2 inhibitor. Lp-PLA2-IN-13 has the potential for the research of neurodegenerative related diseases.

P11 is a selective inhibitor of platelet-activating factor acetylhydrolases (PAFAHs) 1b2 and 1b3 that impairs cancer cell survival. P11 exhibits IC₅₀ values of ~40 and 900 nM for PAFAH1b2 and 1b3, respectively.

DL-erythro-Dihydrosphingosine is a sphingosine-based PKC inhibitor. DL-erythro-Dihydrosphingosine directly inhibits the enzymatic activity of PLA2. DL-erythro-Dihydrosphingosine inhibits the activity of Bcl-2 protein involved in apoptosis. DL-erythro-Dihydrosphingosine inhibits the activity of matrix metalloproteinases (MMP). DL-erythro-Dihydrosphingosine is applicable for research on cancer and inflammatory diseases.

PACOCF3 (Palmityltrifluoromet​hylketone) is a selective phospholipase A2 inhibitor with an IC₅₀ of 3.8 μM. PACOCF3 alters Ca²⁺ signaling in renal tubular cells.

1-Naphthaleneacetic acid potassium salt (Potassium 1-Naphthaleneacetate), a synthetic auxin, can promote plant growth. 1-Naphthaleneacetic acid potassium salt is also an inhibitor of PLA₂, with an IC₅₀ of 13.16 μM.

KARI 201 hydrochloride is a selective, brain penetrant pand competitive acid sphingomyelinase (ASM) inhibitor with an IC₅₀ of 338.3?nM. KARI 201 hydrochloride is a ghrelin receptor agonist. KARI 201 hydrochloride improves neuropathological features of Alzheimer's disease.

Halopemide is a potent phospholipase D (PLD) inhibitor, with IC₅₀s of 220 and 310 nM for human PLD1 and PLD2, respectively. Halopemid is a dopamine receptors antagonist, and acts a psychotropic agent.