Phospholipase A Inhibitor

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.

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

Bromoenol lactone ((6E)-Bromoenol lactone) is a suicide-based irreversible, selective, potent inhibitor of calcium-independent phospholipase A₂ (iPLA₂β) with an IC₅₀ value of approximately 7 μM, which inhibits antigen-stimulated mast cell exocytosis without blocking Ca²⁺ influx.

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

OBAA is a potent phospholipase A2 (PLA2) inhibitor with an IC₅₀ of 70 nM. OBAA blocks Melittin-induced Ca²⁺ influx in Trypanosoma brucei with an IC₅₀ of 0.4 μM.

(R)-Bromoenol lactone ((R,E)-Bromoenol lactone) is an isomer of Bromoenol lactone (HY-107411). (R)-Bromoenol lactone acts as a selective inhibitor of microsomal calcium-independent phospholipase A2γ (iPLA2γ). (R)-Bromoenol lactone induces mild activation of p38 mitogen-activated protein kinase in prostate cancer cells, resulting in slight increases in the expressions of phosphorylated p53, total p53 and p21. (R)-Bromoenol lactone is applicable to prostate cancer-related research.

PTAD-ergosta-3-one is a snake venom enzyme inhibitor. PTAD-ergosta-3-one inhibits the procoagulant activity of citrated plasma mediated by serine protease (SVSP) from Bothrops asper venom. PTAD-ergosta-3-one inhibits the esterase activity of PLA2 from Bothrops asper venom. PTAD-ergosta-3-one can be used in the research of snakebite envenoming.

KH064, a D-tyrosine derivative, is an orally active, potent secretory phospholipase A₂ (sPLA₂) inhibitor with an IC₅₀ of 29 nM for human nonpancreatic secretory PLA₂ isoform IIa (hnpsPLA₂-IIa). KH064 has anti-inflammatory activity.

SB-435495 is a potent, selective, reversible, non-covalent and orally active Lp-PLA₂ inhibitor with an IC₅₀ of 0.06 nM.

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 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 indole-based inhibitor of cytosolic phospholipase A₂ (cPLA₂). Giripladib can be used for osteoarthritis and breast cancer research.

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.

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.

N-Palmitoyl-l-leucine (GK144) is a secreted phospholipases A₂ inhibitor. N-Palmitoyl-l-leucine can be used for inflammatory diseases.

Lp-PLA2-IN-1 is a potent Lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor. Lp-PLA2-IN-1 has the potential for atherosclerosis, Alzheimer's disease research.

Alminoprofen (EB-382) is a nonsteroidal anti-inflammatory agent (NSAID) of the phenylpropionic acid class. Alminoprofen possesses a dual anti-inflammatory action, by inhibiting both secretory phospholipase A₂ (sPLA₂) and COX-2.

(S)-Bromoenol lactone ((S)-BEL) is an irreversible, chiral, mechanism-based inhibitor of calcium-independent phospholipase A₂β (iPLA₂β) that inhibits the vasopressin-induced release of arachidonate from cultured rat aortic smooth muscle (A10) cells with an IC₅₀ of 2 µM.