spla2-iia

sPLA2-X Inhibitor 31 is a selective inhibitor of secreted phospholipase A2 type X (sPLA2-X) with IC50 values of 26 nM for sPLA2-X, 310 nM for sPLA2-IIa, and 2230 nM for sPLA2-V.

The sPLA2-IIA Inhibitor is a cyclic pentapeptide analog of FLSYK, specifically cyclic 2-Nal-Leu-Ser-2-Nal-Arg (c2), which interacts with human IIA phospholipase A2 (hGIIA) to impede its ester bond hydrolyzing function. As part of the esterase superfamily, sPLA2 enzymatically cleaves the sn-2 ester bond in glycerophospholipids, releasing arachidonic acid and lysophospholipids[1].

GK241 (compound 31a-c), a 2-oxoamide-based compound, exhibits inhibitory activity against group IIA secretory phospholipase A2 (GIIA sPLA2) in humans and mice, with IC50 values of 143 nM and 68 nM, respectively. The mechanism of inhibition has been explored through molecular dynamics simulations.

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.

KH064 is a sPLA2-IIA inhibitor of oral activity.

Tanshinone I (Tanshinone A), an active principle isolated from the herbal medicine Salvia miltiorrhiza, displays cytotoxicity against tumor cells.

CGP 43182 is an effective inhibitor of group IIA secretory phospholipase A2 (Group IIA sPLA2) activity in vitro, which can be used to prevent the synergistic effect of pro-inflammatory genes stimulated by cytokines mediated by NFkappaB.

12-HETE ((±)12-HETE) is a modulator of PGE2, with both anti-thrombotic and pro-thrombotic effects, inducing PGE2 release and COX-2 expression via phospholipase A2 (sPLA2-IIA) inducers. It is also a neuroregulator activating retinal cell endothelial dysfunction in diabetic retinopathy.

Phosphatidylethanolamines are important components of cell membranes and biochemical pathways of fatty acid synthesis. 1-Palmitoyl-2-linoleoyl PE (PLPE) is one of the many phosphatidylethanolamines that may be present in cellular membranes. It has been used in studies involving the biosynthesis of anandamide via the phospholipase A2 (PLA2) and lysoPLD pathways. PLPE can also be used as a specific substrate to assess the activity of sPLA2-IIA in the presence of other phospholipids.

Varespladib sodium (LY315920 sodium) is a highly potent and selective inhibitor of group IIA secretory phospholipase A2 (sPLA2), with an IC50 of 9 nM. It shows significant inhibitory activity against sPLA2 in serum samples from multiple species, including rat (IC50 of 8.1 nM), rabbit (IC50 of 5.0 nM), guinea pig (IC50 of 3.2 nM), and human (IC50 of 6.2 nM).