2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. Phospholipase

Phospholipase

Phospholipase

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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:

Phospholipase Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-111346
    1-Linoleoyl Glycerol
    		Inhibitor ≥98.0%
    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).
    1-Linoleoyl Glycerol
  • HY-115403
    FKGK18
    		Inhibitor ≥99.0%
    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.
    FKGK18
  • HY-17448
    Varespladib methyl
    		Inhibitor 99.90%
    Varespladib methyl (A-002; LY333013) is a selective inhibitor of group II secretory phospholipase A2 (PLA2).
    Varespladib methyl
  • HY-112713
    SMS2-IN-2
    		Inhibitor ≥98.0%
    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.
    SMS2-IN-2
  • HY-17569
    Difluprednate
    		Inhibitor 99.64%
    Difluprednate 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.
    Difluprednate
  • HY-119093
    Halopemide
    		Inhibitor 99.65%
    Halopemide is a potent phospholipase D (PLD) inhibitor, with IC50s of 220 and 310 nM for human PLD1 and PLD2, respectively. Halopemid is a dopamine receptors antagonist, and acts a psychotropic agent.
    Halopemide
  • HY-116165
    ML-298
    		Inhibitor ≥98.0%
    ML298 is a potent and selective inhibitor of Phospholipase D2 (PLD2) with an IC50 of 355 nM. ML298 decreases invasive migration in U87-MG glioblastoma cells.
    ML-298
  • HY-108607
    PACOCF3
    		Inhibitor ≥98.0%
    PACOCF3 (Palmityltrifluoromet​hylketone) is a selective phospholipase A2 inhibitor with an IC50 of 3.8 μM. PACOCF3 alters Ca2+ signaling in renal tubular cells.
    PACOCF3
  • HY-P0233A
    Melittin TFA
    		Activator 99.17%
    Melittin TFA is a PLA2 activator, stimulates the activity of the low molecular weight PLA2, while it does not the increase activity of the high molecular weight PLA2.
    Melittin TFA
  • HY-107416
    RHC 80267
    		Inhibitor 99.41%
    RHC 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).
    RHC 80267
  • HY-103593
    LCL521
    		Inhibitor 99.39%
    LCL521 is an acid ceramidase (ACDase) inhibitor. LCL521 also inhibits the lysosomal acid sphingomyelinase (ASMase).
    LCL521
  • HY-11059
    KH064
    		Inhibitor 99.47%
    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.
    KH064
  • HY-141570
    Lyso-PAF C-16
    		99.84%
    Lyso-PAF C-16 is a substrate of lysoplasmalogen (LysoPls)-specific phospholipase D (LysoPLD). Lyso-PAF C-16 selective acetylates with arachidonic acid.
    Lyso-PAF C-16
  • HY-150412
    VU0364739
    		Inhibitor 99.33%
    VU0364739 is a selective PLD2 inhibitor (IC50: 22 nM). VU0364739 decreases cancer cell proliferation.
    VU0364739
  • HY-157562
    DS68591889
    		Antagonist 99.18%
    DS68591889 is an inhibitor of phosphatidylserine synthase 1 (PTDSS1). DS68591889 can be used in tumor research.
    DS68591889
  • HY-N8213
    Rapanone
    		Inhibitor 99.20%
    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.
    Rapanone
  • HY-145653
    GSK2647544
    		Inhibitor 99.46%
    GSK2647544 is an orally available, selective inhibitor of Lp-PLA2. Lipoprotein-associated phospholipase (Lp-PLA2) is a calcium-independent phospholipase A2 with proinflammatory activities that is primarily secreted by monocyte-derived macrophages.
    GSK2647544
  • HY-116141
    7-Hydroxycoumarinyl arachidonate
    		≥98.0%
    7-Hydroxycoumarinyl arachidonate (7-HCA) is a fluorogenic substrate of cytosolic phospholipase A2 (PLA2). 7-Hydroxycoumarinyl arachidonate is also a fluorogenic substrate for monoacylglycerol lipase (MAGL). MAGL protein catalyzes the hydrolysis of 7-Hydroxycoumarinyl arachidonat to generate Arachidonic acid (AA) and the highly fluorescent 7-hydroxyl coumarin (7-HC; HY-N0573). Release of 7-HC can be measured using a fluorometer.
    7-Hydroxycoumarinyl arachidonate
  • HY-N1450
    Aristolochic acid C
    		Inhibitor 99.77%
    Aristolochic acid C is a derivative of Aristolochic acid. Aristolochic acid is a phospholipase A2 (PLA2) inhibitor, which disrupts cortical microtubule arrays and root growth in Arabidopsis.
    Aristolochic acid C
  • HY-14952
    Giripladib
    		Inhibitor 99.68%
    Giripladib (PLA-695) is a indole-based inhibitor of cytosolic phospholipase A2 (cPLA2). Giripladib can be used for osteoarthritis and breast cancer research.
    Giripladib
Cat. No. Product Name / Synonyms Application Reactivity
Phospholipase Isoform Comparison

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