spla2-iia

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].

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.

AZD2716 is a selective secretory phospholipase A2(sPLA2) inhibitor, which can inhibit sPLA2-IIa, sPLA2-V and sPLA2-X, and its IC₅₀ is 10 nM, 40 nM and 400 nM respectively. AZD2716 can reduce the production of pro-inflammatory lipids, thus reducing macrophage activation and foam cell formation, and has been used in the study of atherosclerosis and inflammatory diseases related to sPLA2.

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.

1-Palmitoyl-2-linoleoyl PE is a kind of phosphatidylethanolamine lipid, which can be used as a component of liposomes or lipid nanoparticles to promote the delivery and cell uptake of nucleic acids (such as sRNA).

Varespladib sodium is a potent and selective inhibitor of secretory phospholipase A2 (sPLA2), with an IC50 of approximately 9 nM against group IIA sPLA2. It exhibits nanomolar inhibitory activity in serum from various species, including rat, rabbit, guinea pig, and human. It is commonly used in research related to inflammation and lipid metabolism.

Tanshinone I (Standard) is a reference standard for research and analysis in studies involving Tanshinone I. Tanshinone I (Tanshinone A), an active principle isolated from the herbal medicine Salvia miltiorrhiza, displays cytotoxicity against tumor cells.

12-HETE (Standard) is a reference standard for research and analysis in studies involving 12-HETE. 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.