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-142778
    Lp-PLA2-IN-10
    Lp-PLA2-IN-10 is a potent inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2). Lp-PLA2 previously known as platelet- activating factor acetylhydrolase (PAF-AH), is a phospholipase A2 enzyme involved in hydrolysis of lipoprotein lipids or phospholipids. Lp-PLA2-IN-10 has the potential for the research of neurodegenerative-related diseases such as Alzheimer's disease (AD), glaucoma, age-related macular degeneration (AMD), or cardiovascular diseases including atherosclerosis (extracted from patent WO2022001881A1, compound 4).
    Lp-PLA2-IN-10
  • 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-128762
    ML256
    		Inhibitor
    ML256 is a covalent lipoprotein-associated phospholipase A2 (Lp-PLA2 inhibitor. ML256 can be used for the study of neoplasms harboring a constitutively active variant of one or both of KRAS or HRAS.
    ML256
  • HY-165327
    AGN-190383
    		Inhibitor
    AGN-190383 is a bee venom phospholipase A2 inhibitor. AGN 190383 inhibits both hormone-operated and depolarization-dependent calcium mobilization as well as fMLP stimulated increases in free cytosolic calcium. AGN-190383 has anti-inflammatory activity.
    AGN-190383
  • 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-128020
    ML114
    		Inhibitor
    ML114 is a specific inhibitor of RBBP9 serine hydrolase, with an IC50 of 0.63 μM against recombinant RBBP9. ML114 can inhibit the proliferation of human pluripotent stem cells (hPSCs) by regulating the expression of NFYA and other factors, but does not induce differentiation. ML114 can be used in the research of diseases such as retinoblastoma.
    ML114
  • HY-17569S2
    Difluprednate-d3-1
    		Inhibitor
    Difluprednate-d3-1 is the deuterium labeled Difluprednate (HY-17569). 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-d<sub>3</sub>-1
  • HY-133233
    Thioetheramide-PC
    		Inhibitor 98%
    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-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-182680
    Manoalogue
    		Inhibitor
    Manoalogue is an irreversible secretory phospholipase A2 (sPLA2) inhibitor. Manoalogue covalently modifies K94 of bee venom phospholipase A2 (bvPLA2) to inactivate the enzyme and shows selective inhibition on bvPLA2. Manoalogue can suppress PLA2-mediated contractions of guinea pig lung pleural strips. Manoalogue is used for sPLA2 mechanism and respiratory physiology research.
    Manoalogue
  • HY-108654
    PSB 0474
    PSB 0474 (3-phenacyl-UDP) is a UDP (HY-113359) analog and selective P2Y6 receptor agonist, with an EC50 value of 70 nM for the hP2Y6 receptor. PSB 0474 activates Phospholipase C-coupled receptors to increase intracellular inositol phosphate levels. PSB 0474 enhances NO release by upregulating inducible iNOS and induces Apoptosis. PSB 0474 increases micturition frequency in urine of anesthetized rats, without altering bladder contraction amplitude/duration or causing urothelial damage. PSB 0474 can be used in studies related to chronic brain inflammation.
    PSB 0474
  • 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-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
Cat. No. Product Name / Synonyms Application Reactivity
Phospholipase Isoform Comparison

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