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-13402S
    Varespladib-d7
    Varespladib-d7 (LY315920-d7) is a deuterated labeled Varespladib (HY-13402). Varespladib is a potent and selective group IIA, secretory phospholipase A2 (sPLA2) inhibitor with an IC50 of 9 nM. Varespladib 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.
    Varespladib-d<sub>7</sub>
  • HY-N6857C
    (±)-Armepavine hydrochloride
    (±)-Armepavine hydrochloride is a compound that has demonstrated immunosuppressive effects on T lymphocytes and in lupus nephritic mice.
    (±)-Armepavine hydrochloride
  • HY-108132
    Ro 23-9358
    		Inhibitor
    Ro 23-9358 is a potent secretory phospholipase A2 inhibitor with anti-inflammatory activity.
    Ro 23-9358
  • HY-162613
    ASM-IN-2
    		Inhibitor
    ASM-IN-2 (Compound 46) is a potent ASM inhibitor with an IC50 value of 0.87 μM, displaying good drug-like properties. ASM-IN-2 involves in multiple antidepressant mechanisms of actionin, which are associated with a decline of ceramide. It demostrates remarkable antidepressant effects in the CUMS-induced mouse, which is promising for research in the field of antidepressant drugs.
    ASM-IN-2
  • HY-133233
    Thioetheramide-PC
    		Inhibitor
    Thioetheramide-PC (1-Palmitylthio-2-palmitoylamido-1,2-dideoxy-sn-glycero-3-phosphorylcholine) is a structurally modified phospholipid that acts as a competitive, reversible inhibitor of secretory phospholipase A2 (sPLA2). Thioetheramide-PC has an IC50 value of 2 μM at a substrate concentration of 0.5 mM. In addition to binding to the catalytic site of sPLA2, Thioetheramide-PC also binds to the activation site of the enzyme. Thioetheramide-PC binds more tightly to the activation site than to the catalytic site. As a result of this dual interaction, at low concentrations, Thioetheramide-PC may activate phospholipase activity rather than inhibit it.
    Thioetheramide-PC
  • HY-158334
    NDs-IN-1
    		Inhibitor
    (Neurodegenerative diseases) NDs-IN-1 (Compound 3g) inhibits the activities of key enzymes such as hBACE-1, hAChE and hMAO-B. NDs-IN-1 is a novel non-covalent multi-target inhibitor. NDs-IN-1 is mainly used in the study of neurodegenerative diseases.
    NDs-IN-1
  • HY-P10053
    sPLA2-IIA Inhibitor
    		Inhibitor
    sPLA2-IIA Inhibitor is a cyclic pentapeptide analog of FLSYK (cyclic 2-Nal-Leu-Ser-2-Nal-Arg (c2)), that binds to hGIIA (human IIA phospholipase A2) and inhibits its hydrolytic ability. sPLA2 is a member of the esterase superfamily that catalyzes the hydrolysis of the ester bond at the sn-2 position of glycerophospholipids, releasing free fatty acids such as arachidonic acid and lysophospholipids.
    sPLA2-IIA Inhibitor
  • HY-142774
    Lp-PLA2-IN-6
    		Inhibitor
    Lp-PLA2-IN-6 (compound 18), a tetracyclic pyrimidinone compound, is a potent Lp-PLA2 inhibitor with a pIC50 of 10.0 for rhLp-PLA2. Lp-PLA2-IN-6 has the potential for neurodegenerative related diseases research.
    Lp-PLA2-IN-6
  • HY-153183
    Lp-PLA2-IN-12
    		Inhibitor
    Lp-PLA2-IN-12 (compound 19) is an Lp-PLA2 inhibitor. Lp-PLA2-IN-12 can be used for the study of neurodegenerative related diseases such as Alzheimer's disease (AD), glaucoma, age-related macular degeneration (AMD), or cardiovascular disease including atherosclerosis.
    Lp-PLA2-IN-12
  • HY-162368
    cPLA2α-IN-2
    		Inhibitor
    cPLA2α-IN-2 (Compound 122) is an inhibitor of cytosolic phospholipase A2α (cPLA2α).
    cPLA2α-IN-2
  • HY-135564A
    RK-682
    		Inhibitor 99.0%
    RK-682 is the inhibitor for protein tyrosine phosphatase (PTPase), heparanase, phospholipase A2 and HIV-1 protease. RK-682 inhibits the dephosphorylation of CD45 (IC50 is 54 μM) and VHR (IC50 is 2.0 μM), and thereby inhibits the ERK signaling pathway. RK-682 inhibits the cell viability of cancer cell MGH-U3, T24 and UROtsa with IC50s of 78.2, 43.2 and 145 nM, respectively, arrests the cell cycle at G1/S phase, inhibits the cell migration and autophagy in MGH-U3 and T24.
    RK-682
  • HY-116671
    Folipastatin
    		Inhibitor
    Folipastatin is a potent inhibitor of phospholipase A2 with an IC50 of 39 μM. Folipastatin is a new depsidone compound from Aspergillus unguis.
    Folipastatin
  • HY-168372
    1-Myristoyl-2-Linoleoyl-sn-glycero-3-PC
    		Ligand
    1-Myristoyl-2-Linoleoyl-sn-glycero-3-PC is a phospholipid that contains Myristic acid (HY-N2041) and Linoleic acid (HY-N0729) at the sn-1 and sn-2 positions, respectively, which is found in human plasma.
    1-Myristoyl-2-Linoleoyl-sn-glycero-3-PC
  • HY-112747
    Soy PE
    Phosphatidylethanolamine is the most abundant phospholipid in prokaryotes and the second most abundant found in the membrane of mammalian, plant, and yeast cells, comprising approximately 25% of total mammalian phospholipids. In the brain, phosphatidylethanolamine comprises almost half of the total phospholipids. It is synthesized mainly through the cytidine diphosphate-ethanolamine and phosphatidylserine decarboxylation pathways, which occur in the endoplasmic reticulum (ER) and mitochondrial membranes, respectively. It is a precursor in the synthesis of phosphatidylcholine and arachidonoyl ethanolamide and is a source of ethanolamine used in various cellular functions. In E. coli, phosphatidylethanolamine deficiency prevents proper assembly of lactose permease, suggesting a role as a lipid chaperone. It is a cofactor in the propagation of prions in vitro and can convert recombinant mammalian proteins into infectious molecules even in the absence of RNA. This product contains phosphatidylethanolamine molecular species with variable fatty acyl chain lengths at the sn-1 and sn-2 positions.
    Soy PE
  • HY-150559
    SMS2-IN-3
    		Inhibitor
    SMS2-IN-3 is a potent and selective SMS2inhibitor (IC50=2.2 nM), significantly reduces the hepatic SM (22:0) levels.
    SMS2-IN-3
  • HY-177003
    SM (d18:1/15:0)
    		Inhibitor
    SM (d18:1/15:0) is a sphingomyelinase inhibitor. SM (d18:1/15:0) is promising for research of neurodegenerative diseases (e.g., Alzheimer's) and metabolic syndrome.
    SM (d18:1/15:0)
  • HY-118725
    Luffariellolide
    		Inhibitor
    Luffariellolide is an inhibitor of human synovial fluid phospholipase A2 (HSF-PLA2) (IC50=5 μM). Luffariellolide effectively inhibits phorbol ester (PMA)-induced ear edema (ED50=50 μg/ear).
    Luffariellolide
  • HY-129944
    MJ33-OH
    		Inhibitor
    MJ33-OH is a metabolite of MJ33. 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-OH
  • HY-153561
    Lp-PLA2-IN-15
    		Inhibitor
    Lp-PLA2-IN-15 (example 2) is a lipoprotein-associated phospholipase A2 (Lp-PLA 2) inhibitor, which can be used in the research of Alzheimer's disease, etc.
    Lp-PLA2-IN-15
  • HY-153560
    Lp-PLA2-IN-14
    		Inhibitor
    Lp-PLA2-IN-14 (Compound 19) is an Lp-PLA2 inhibitor with a pIC50 of 8.4 against rhLp-PLA2. Lp-PLA2-IN-14 can be used for the research of neurodegenerative related diseases, such as Alzheimer Disease (AD), glaucoma, age-related macular degeneration (AMD) or cardiovascular diseases including atherosclerosis and the like.
    Lp-PLA2-IN-14
Cat. No. Product Name / Synonyms Application Reactivity
Phospholipase Isoform Comparison

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