2. シグナル伝達
  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
製品番号 製品名 製品効果 純度 構造式
  • HY-111346
    1-Linoleoyl Glycerol

    1-Linoleoyl Glycerol

    		Inhibitor 99.52%
    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-125254
    LEI110 Inhibitor 99.72%
    LEI110 is a potent, selective and cell-permeable pan-inhibitor of the HRASLS family of thiol hydrolases. LEI110 inhibits PLA2G16, HRASLS2, RARRES3 and iNAT, with pIC50 values of 7.0, 6.8, 6.8, and 7.6, respectively. LEI110 reduces cellular arachidonic acid levels and oleic acid-induced lipolysis in HepG2 cells.
    LEI110
  • HY-101015A
    OBAA

    OBAA

    		Inhibitor 99.31%
    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-173371
    BRI-50460 Inhibitor 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.
    BRI-50460
  • HY-11059
    KH064 Inhibitor 99.84%
    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-18522
    AA26-9 Inhibitor 99.83%
    AA26-9 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 .
    AA26-9
  • HY-107416
    RHC 80267

    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-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-149120
    ASM-IN-1 Inhibitor 98.65%
    ASM-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.
    ASM-IN-1
  • HY-103593
    LCL521 Inhibitor 98.53%
    LCL521 is an acid ceramidase (ACDase) inhibitor. LCL521 also inhibits the lysosomal acid sphingomyelinase (ASMase).
    LCL521
  • HY-17569
    Difluprednate

    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-19415
    SB-435495 Inhibitor 99.71%
    SB-435495 is a potent, selective, reversible, non-covalent and orally active Lp-PLA2 inhibitor with an IC50 of 0.06 nM.
    SB-435495
  • HY-P1341
    OXA(17-33) Activator
    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.
    OXA(17-33)
  • HY-116301
    CAY10502 Inhibitor ≥99.0%
    CAY10502 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.
    CAY10502
  • HY-17448
    Varespladib methyl Inhibitor 99.64%
    Varespladib methyl (A-002; LY333013) is a selective inhibitor of group II secretory phospholipase A2 (PLA2).
    Varespladib methyl
  • HY-13402A
    Varespladib sodium Inhibitor 98.83%
    Varespladib 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.
    Varespladib sodium
  • 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
  • HY-W012595
    Benzylideneacetone

    Benzalacetone

    		Inhibitor 99.66%
    Benzylideneacetone (Benzalacetone) is an orally active antibiotic, tyrosinase inhibitor, phospholipase A2 inhibitor, and immunosuppressant. Benzylideneacetone has antibacterial activity against some gram-negative plant-pathogenic bacteria. Benzylideneacetone can also be used in the synthesis of chemicals and drugs, and as a flavoring additive for some foods.
    Benzylideneacetone
  • HY-P0233A
    Melittin TFA Activator 99.85%
    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-145653
    GSK2647544 Inhibitor 99.50%
    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
製品番号 製品名 / Synonyms Application Reactivity
Phospholipase Isoform Comparison

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