Phospholipase
Phospholipase is a member of a very complex group of enzymes that break down phospholipids into fatty acids and other compounds. Phospholipases are defined by the enzymatic reaction they catalyze. The classes are phospholipase A, which has members A1 and A2; phospholipase B, which can carry out the reactions of both A1 and A2; phospholipase C; and phospholipase D.
Phospholipase A2 (PLA2) catalyses the hydrolysis of the sn-2 position of glycerophospholipids to yield fatty acids and lysophospholipids. Phospholipase C (PLC) converts phosphatidylinositol 4,5-bisphosphate (PIP2) to inositol 1,4,5-trisphosphate (IP3) and diacylglycerol (DAG). DAG and IP3 each control diverse cellular processes and are also substrates for synthesis of other important signaling molecules. PLC is thus central to many important interlocking regulatory networks. Phospholipase D (PLD) is an essential enzyme responsible for the production of the lipid second messenger phosphatidic acid (PA), which is involved in fundamental cellular processes, including membrane trafficking, actin cytoskeleton remodeling, cell proliferation and cell survival.
Phospholipase Isoform Specific Products
All Product Categories
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Phospholipase Related Products (326)
Related Products (326)
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Antibodies (9)
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Phospholipase Isoform Comparison
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Rilapladib
0 ImagesSynonyms: SB 659032Rilapladib (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.
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1-Linoleoyl Glycerol
0 ImagesSynonyms: 1-Linoleoyl-rac-glycerol; 1-Monolinolein1-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).
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LEI110
0 ImagesLEI110 is a pan-inhibitor of the HRASLS family and an inhibitor of AP-2α, with a Ki of 20 nM against PLA2G16. LEI110 exhibits inhibitory activity against PLA2G16, HRASLS2, RARRES3 and iNAT, with pIC50 values of 7.0, 6.8, 6.8 and 7.6, respectively. LEI110 binds to the active site of PLA2G16, reduces intracellular arachidonic acid levels, and attenuates oleic acid-induced lipolysis. LEI110 stabilizes AP-2α, impairs its DNA-binding ability, inhibits the transcription of DNA damage repair genes, induces the accumulation of oxidative DNA damage, suppresses cell proliferation and clonogenicity, and sensitizes HCC cells to DNA-damaging agents. LEI110 can be used in research related to obesity, fatty liver disease, the common cold and hepatocellular carcinoma.
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OBAA
0 ImagesOBAA 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.
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BRI-50460
0 ImagesCat. No.: HY-173371Purity: 99.62%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.
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PF-04217903
0 ImagesPF-04217903 is an orally active, highly selective ATP-competitive c-Met kinase inhibitor with a Ki value of 4.8 nM and a Kd 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).
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KH064
0 ImagesKH064, 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.
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LCL521
0 ImagesLCL521 is an acid ceramidase (ACDase) inhibitor. LCL521 also inhibits the lysosomal acid sphingomyelinase (ASMase).
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SMS2-IN-2
0 ImagesSMS2-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.
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Difluprednate
0 ImagesDifluprednate is a glucocorticoid receptor (GC receptor) agonist with a Ki of 0.78 nM. Difluprednate's active metabolite 21-deacetylated difluprednate (DFB) is a competitive agonist of GC receptors with a Ki 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.
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AA26-9
0 ImagesAA26-9 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 .
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SB-435495
0 ImagesSB-435495 is a potent, selective, reversible, non-covalent and orally active Lp-PLA2 inhibitor with an IC50 of 0.06 nM.
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OXA(17-33)
0 ImagesCat. No.: HY-P1341CAS No.: 343268-91-7Synonyms: Orexin A (17-33) (human, mouse, rat, bovine)OXA (17-33) (Orexin A (17-33) (human, mouse, rat, bovine)) is the shortest active orexin peptide that selectively targets OX1 (EC50=8.29 nM), with 23-fold selectivity for the OX1 receptor over the OX2 receptor. The activity of OXA (17-33) depends on the Tyr17, Leu20, Asn25, His26 residues and the spatial conformation of the α-helix. OXA (17-33) activates signaling pathways involving inositol-1,4,5-trisphosphate receptor (IP3R), phospholipase D (PL-D) and choline-Sigma-1R, thereby increasing the cytoplasmic Ca2+ level in nucleus accumbens neurons, an effect that is blocked by Sigma-1R antagonists. OXA (17-33) serves as an important biological probe for investigating the function of the OX1 receptor. OXA (17-33) can be modified via incorporation of mixed disulfide bonds of homocysteine and cysteamine, and is widely used in studies related to insomnia and narcolepsy.
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ASM-IN-1
0 ImagesASM-IN-1 is a potent and orally active acid sphingomyelinase (ASM) inhibitor with an IC50 value of 1.5 µM. ASM-IN-1 reduces lipid plaques in the aortic arch and aorta and reduces plasma ceramide concentration and Ox-LDL levels. ASM-IN-1 shows antiatherosclerotic and anti-inflammatory activity.
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CAY10502
0 ImagesCAY10502 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.
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Varespladib methyl
0 ImagesSynonyms: A-002; LY333013Varespladib methyl (A-002; LY333013) is a selective inhibitor of group II secretory phospholipase A2 (PLA2).
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RHC 80267
0 ImagesSynonyms: U-57908RHC 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).
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Varespladib sodium
0 ImagesSynonyms: LY315920 sodiumVarespladib 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.
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Giripladib
0 ImagesSynonyms: PLA-695Giripladib (PLA-695) is a indole-based inhibitor of cytosolic phospholipase A2 (cPLA2). Giripladib can be used for osteoarthritis and breast cancer research.
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LY-311727
0 ImagesLY-311727 is a potent secretory non-pancreatic phospholipase A2 (sPLA2) inhibitor (IC50 <1 μM for group IIA sPLA2). sPLA2 is an important proinflammatory enzyme.
