Phospholipase Inhibitor

3-Nitrocoumarin is an inhibitor for phospholipase C that blocks the generation of inositol triphosphate (IP₃), thereby affecting the calcium signaling pathway.

CAY10594 is an orally active PLD2 inhibitor with an IC₅₀ of 140 nM. CAY10594 has activities such as anti-tumor, anti-oxidation and liver protection. CAY10594 can be used for the research of diseases like breast cancer, acute liver injury and colitis.

Rhamnetin is a quercetin derivative found in Coriandrum sativum, inhibits secretory phospholipase A2 and histone deacetylase 2 (HDAC2). Rhamnetin exhibits antitumor, antioxidant and anti-inflammatory activity.

Magnesium sulfate heptahydrate, for cell culture (Epsom salts, for cell culture) is a hydrate of magnesium sulfate (HY-Y1267) suitable for cell culture applications. Magnesium sulfate is a calcium antagonist and a potent L-type calcium channel inhibitor, as well as a tocolytic. Magnesium sulfate has anti-inflammatory, anticonvulsant, vasodilatory, and neuroprotective effects. Magnesium sulfate can be used in the research of diseases such as preeclampsia/eclampsia.

VU0364739 is a selective PLD2 inhibitor (IC₅₀: 22 nM). VU0364739 decreases cancer cell proliferation.

ONO-RS-082 is an inhibitor of phospholipase A (PLA). ONO-RS-082 inhibits PLA2 with the IC₅₀ of 1.0 μM, but does not inhibit PLC even at 100 μM.

Magnesium sulfate, for cell culture is a bioreagent. Magnesium sulfate is a calcium antagonist and a potent L-type calcium channel inhibitor, as well as a tocolytic. Magnesium sulfate has anti-inflammatory, anticonvulsant, vasodilatory, and neuroprotective effects. Magnesium sulfate can be used in the research of diseases such as preeclampsia/eclampsia.

VU0155069 (CAY10593), is a selective phospholipase D1 (PLD1) inhibitor with an IC₅₀ value of 46 nM in vitro. VU0155069 (CAY10593) strongly inhibits the invasive migration of several cancer cell lines in transwell assays.

FKGK18 is a selective group VIA calcium-independent phospholipase A₂ (GVIA iPLA₂) inhibitor. FKGK18 is a fluoroketone (FK)-based compound with IC₅₀s of 50 nM and 3 μM for iPLA₂β and iPLA₂γ. FKGK18 can be used for the research of beta-cell apoptosis and diabetes.

ML-211 is a potent dual inhibitor of LYPLA1 and LYPLA2 enzymes, with an IC₅₀ value of 17 nM against LYPLA1, 30 nM against LYPLA2, and 10 nM against ABHD11.

Rilapladib (SB 659032) is a selective Lp-PLA₂ (lipoprotein-associated phospholipase A₂) inhibitor with an IC₅₀ of 230 pM. Rilapladib (SB 659032) is also a PAFR (Platelet Activating Factor Receptor) antagonist.

1-Linoleoyl glycerol is a LpPLA2 inhibitor. 1-Linoleoyl glycerol acts as a precursor for synthesizing various functional lipids, such as phospholipids. 1-Linoleoyl glycerol mitigates inflammation induced by Apolipoprotein CIII (reduction of IL-6).

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.

BRI-50460 is an inhibitor of cytosolic calcium-dependent phospholipase A2 (cPLA2) that has the ability to penetrate the blood-brain barrier, with an IC₅₀ of 0.88 nM. BRI-50460 exerts the activities of regulating neuroinflammation and restoring lipid homeostasis by inhibiting cPLA2, regulating the downstream inflammatory lipid signaling pathway, and alleviating the effects of amyloid β42 oligomers on the activation of cPLA2, the hyperphosphorylation of tau protein, and the reduction of synapses and dendrites. BRI-50460 can be applied to the research in the fields of Alzheimer's disease and other neurodegenerative diseases.

PF-04217903 is an orally active, highly selective ATP-competitive c-Met kinase inhibitor with a K_i value of 4.8 nM and a K_d value of 4.5 nM. PF-04217903 blocks c-Met and HGF signaling pathways, inhibits MET phosphorylation, and blocks downstream MAPK, PI3K/AKT and PLCγ1 pathways. PF-04217903 suppresses tumor proliferation, survival, migration, invasion, angiogenesis and metastasis, induces apoptosis, and enhances efferocytosis, Annexin A1 expression and resolution of inflammation. PF-04217903 retains activity against several c-Met mutants (M1131T, V1220I, H1094R). PF-04217903 increases the incidence of subarachnoid hemorrhage and reduces survival rate without altering aneurysm formation, and also prevents lymph node metastasis induced by VEGF inhibition. PF-04217903 is applicable to research related to tumors (pancreas, stomach, lung, brain, colon, breast, kidney, melanoma, etc.), intracranial aneurysms and inflammatory diseases (gouty arthritis, neutrophilic pleuritis).

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.

LCL521 is an acid ceramidase (ACDase) inhibitor. LCL521 also inhibits the lysosomal acid sphingomyelinase (ASMase).

SMS2-IN-2 is a potent, highly selective and orally active sphingomyelin synthase 2 (SMS2) inhibitor, with IC₅₀s of 100 nM and 56 μM for SMS2 and SMS1, respectively. Anti-chronic inflammatory activity.

Difluprednate is a glucocorticoid receptor (GC receptor) agonist with a K_i of 0.78 nM. Difluprednate's active metabolite 21-deacetylated difluprednate (DFB) is a competitive agonist of GC receptors with a K_i of 0.061 nM. Difluprednate binds to GC receptors through metabolism to DFB, regulating the transcription of inflammatory mediator genes, thereby exerting anti-inflammatory activity. Difluprednate can be used for research related to ocular inflammation, such as postoperative inflammation, anterior uveitis, etc.

AA26-9 is a potent and broad spectrum serine hydrolase inhibitor. AA26-9 targets included serine peptidases, lipases, amidases, esterases, and thioesterases. AA26-9 shows inhibitory activity against approximately 1/3 of the 40+ serine hydrolases detected in immortalized T cell lines .