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-123070
    ONO-RS-082
    		Inhibitor 99.89%
    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.
    ONO-RS-082
  • 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-100168A
    BAPTA tetrasodium
    		Inhibitor
    BAPTA tetrasodium is a selective chelator for calcium. BAPTA tetrasodium, as calcium indicator, has high selectivity against magnesium and calcium. BAPTA tetrasodium is widely used as an intracellular buffer for investigating the effects of Ca2+ release from intracellular stores or influx via Ca2+-permeable channels in the plasma membrane. BAPTA tetrasodium can also inhibit phospholipase C activity independently of their role as Ca2+ chelators.
    BAPTA tetrasodium
  • HY-102004
    Rilapladib
    		Inhibitor 99.71%
    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.
    Rilapladib
  • HY-N7036
    Rhamnetin
    		Inhibitor 99.18%
    Rhamnetin is a quercetin derivative found in Coriandrum sativum, inhibits secretory phospholipase A2, with antioxidant and anti-inflammatory activity.
    Rhamnetin
  • HY-111346
    1-Linoleoyl Glycerol
    		Inhibitor ≥98.0%
    1-Linoleoyl Glycerol is a fatty acid glycerol.
    1-Linoleoyl Glycerol
  • HY-17569
    Difluprednate
    		Inhibitor 99.64%
    Difluprednate is a topical corticosteroid, which is thought to act by the induction of phospholipase A2 inhibitory proteins (lipocortins). Difluprednate is used for the symptomatic treatment of inflammation and pain associated with ocular surgery.
    Difluprednate
  • 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-N9480
    Vinaxanthone
    		Inhibitor 98.56%
    Vinaxanthone (SM-345431) is a potent and selective semaphorin3A, phospholipase C (PLC) and FabI inhibitor, with IC50s of 0.1-0.2 μM and 0.9 mM for semaphorin3A and FabI. Vinaxanthone inhibits the substrate (t-o-NAC thioester) and the cofactor (NADPH) with Kis of 3.1 μM and 1.0 μM, respectively. Vinaxanthone can be used to handle infections caused by multidrug-resistant pathogens.
    Vinaxanthone
  • 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-101015A
    OBAA
    		Inhibitor 99.27%
    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.
    OBAA
  • 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-115062
    MJ33 lithium salt
    		Inhibitor ≥99.0%
    MJ33 is an active-site-directed, specific, competitive, and reversible phospholipase A2 (PLA2) inhibitor. MJ33 blocks the calcium-independent phospholipase A2 (iPLA2) activity of Prdx6.
    MJ33 lithium salt
  • HY-107416
    RHC 80267
    		Inhibitor 98.08%
    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-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-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-103593
    LCL521
    		Inhibitor 99.39%
    LCL521 is an acid ceramidase (ACDase) inhibitor. LCL521 also inhibits the lysosomal acid sphingomyelinase (ASMase).
    LCL521
  • HY-101293
    VU0359595
    		Inhibitor 99.65%
    VU0359595 (CID-53361951; ML-270) is a potent and selective pharmacological phospholipase D1 (PLD1) inhibitor with an IC50 of 3.7 nM. VU0359595 is >1700-fold selective for PLD1 over PLD2 (IC50 of 6.4 μM). VU0359595 can be used for the research of cancer, diabetes, neurodegenerative and inflammatory diseases.
    VU0359595
  • 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-11059
    sPLA2 inhibitor 1
    		Inhibitor 99.47%
    sPLA2 inhibitor 1, 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). sPLA2 inhibitor 1 has anti-inflammatory activity.
    sPLA2 inhibitor 1
Phospholipase Isoform Comparison

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