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Phospholipase D, Streptomyces chromofuscus (PLD) is an enzyme of the phospholipase superfamily, which widely exists in bacteria, yeast, plants, animals and viruses, and is often used in biochemical research. Phospholipase D can catalyze the hydrolysis of phosphodiester bonds in glycerophospholipids to produce phosphatidic acid and soluble choline. Phospholipase D is involved in a variety of disease-related processes, including diabetes, atherogenesis, obesity, tumorigenesis, immune response, and neuroendocrine function .
Lyso-PAF C-16 is a substrate of lysoplasmalogen (LysoPls)-specific phospholipase D (LysoPLD). Lyso-PAF C-16 selective acetylates with arachidonic acid .
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 .
ST271 is a potent inhibitor of protein tyrosine kinase (PTK), inhibits phospholipase D activation stimulated by fMet-Leu-Phe and PAF, with IC50s of 6.7 and 9 μM, respectively.
LEI-401 is a first-in-class, selective, and CNS-active NAPE-PLD (N-acylphosphatidylethanolamine phospholipase D) inhibitor, with an IC50 of 27 nM. LEI-401 modulates emotional behavior in mice .
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 .
Phospholipase D, cabbage is an enzyme of the phospholipase superfamily. Phospholipase D, cabbage is widely found in bacteria, yeast, plants, animals and viruses and is often used in biochemical research. Phospholipase D, cabbage can catalyze the hydrolysis of the phosphodiester bond of glycerophospholipids to produce phosphatidic acid and soluble choline. Phospholipase D, cabbage is involved in a variety of disease-related processes, including diabetes, atherosclerosis, obesity, tumorigenesis, immune response and neuroendocrine function .
Phospholipase D, peanut is an important signaling enzyme in mammalian cells. Phospholipase D, peanut catalyzes the hydrolysis of phosphatidylcholine to produce phosphatidic acid (PA) and choline .
A4333 is biotinylated compound of A3373 (HY-155342) that inhibits Phospholipase D1 (PLD1), but not PLD2. A4333 plays an important role in antitumor activity .
ML299 is a selective allosteric modulator and a dual inhibitor of phospholipases D1 and D2 (IC50 values are 6 and 12 nM, respectively). ML299 decreases invasive migration in U87-MG glioblastoma cells .
VU 0364739 hydrochloride is a highly selective phospholipase D2 (PLD2) inhibitor with IC50s of 20 and 1500 nM for PLD2 and PLD1, respectively. VU 0364739 hydrochloride induces apoptosis and it can be used for cancer research .
VU0155069 (CAY10593), is a selective phospholipase D1 (PLD1) inhibitor with an IC50 value of 46 nM in vitro. VU0155069 (CAY10593) strongly inhibits the invasive migration of several cancer cell lines in transwell assays .
VU0155069 hydrochloride (CAY10593 hydrochloride) is a potent selective phospholipase D (PLD) inhibitor. The IC50 values for PLD1 and PLD2 are 46 and 933 nM, respectively. VU0155069 hydrochloride inhibits migration of human and mouse breast cancer cell lines .
CHS-111 is a benzyl indazole inhibitor of superoxide anion O 2- generation. CHS-111 inhibits the cell migration, and reduces the formyl-Met-Leu-Phe- but not phorbol ester-stimulated phospholipase D activity, with the IC50 of 3.9 μM .
A3373, a novel chemical inhibitor of Phospholipase D1 (PLD1) and PLD2, with IC50 of 325 nM and 15.15?μM, respectively, inhibits LPS-induced immune response and plays important roles in autoimmune arthritis, bone demineralization and osteoclastogenesis .
Dioctanoylphosphatidic acid sodium functions as a modulator of phagocyte respiratory burst, acts as a precursor to diacylglycerol and lysophosphatidic acid, and influences the phosphorylation of the mammalian target of rapamycin (mTOR) while enhancing the viability of gallbladder carcinoma cells treated with histone deacetylase inhibitors (HDACIs); it is derived from glycerophospholipid through the action of phospholipase D.
Dioleoylphosphatidylglycerol (DOPG) is a naturally occurring phospholipid that can be produced by the combined action of aquaporin 3 (AQP3) and phospholipase D2 (PLD2). Dioleoylphosphatidylglycerol inhibits macrophage inflammatory mediator production in response to heat shock protein B4 (HSPB4) activation of toll-like receptor 2 (TLR2) .
BML-280 (VU0285655-1) is a potent and selective phospholipase D2 (PLD2) inhibitor. BML-280 has the ability to prevent caspase-3 cleavage and reduction in cell viability induced by high glucose. BML-280 can be used for rheumatoid arthritis research .
DHPG ((RS)-3,5-DHPG) is an amino acid, which acts as a selective and potent agonist of group I mGluR (mGluR 1 and mGluR 5), shows no effect on Group II or Group III mGluRs . DHPG ((RS)-3,5-DHPG) is also an effective antagonist of mGluRs linked to phospholipase D .
ML395 is a potent and selective allosteric inhibitor of phospholipase D2 with antiviral activity. The cellular PLD1 IC50 value of ML395 exceeds 30,000 nM, while its cellular PLD2 IC50 value is 360 nM. ML395 shows excellent pharmacokinetic characteristics in vitro and physiochemical properties superior to other reported phospholipase inhibitors. ML395 shows interesting antiviral activity in cell-based assays against multiple influenza virus strains (H1, H3, H5, and H7) .
FIPI is a phospholipase D (PLD) inhibitor with an IC50 for PLD1 and PLD2 of about 25 nM. FIPI regulates cytoskeletal recombination, cell diffusion and chemotaxis. FIPI can be used in cancer research. In addition, FIPI can enhance the secretion and aggregation of platelet dense particles, inhibit thrombosis, reduce ischemic stroke infarct volume and improve nerve function .
CAY10594 is a potent phospholipase D2 (PLD2) inhibitor both in vitro (IC50=140 nM) and in cells (IC50=110 nM) . CAY10594 strongly inhibits the invasive migration of breast cancer cells in vitro and ameliorates acetaminophen-induced acute liver injury by regulating the phosphorylated-GSK-3β/JNK axis .
FIPI hydrochloride is a phospholipase D (PLD) inhibitor with an IC50 for PLD1 and PLD2 of about 25 nM. FIPI hydrochloride regulates cytoskeletal recombination, cell diffusion and chemotaxis. FIPI hydrochloride can be used in cancer research. In addition, FIPI hydrochloride can enhance the secretion and aggregation of platelet dense particles, inhibit thrombosis, reduce ischemic stroke infarct volume and improve nerve function .
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 .
Lysophosphatidylethanolamine (LPE) is a naturally-occurring lysophospholipid that can be generated via deacylation of phosphatidylethanolamine by phospholipase A2 (PLA2). It increases the phosphorylation of ERK1/2 in PC12 cells, an effect that can be blocked by the MEK inhibitors U-0126 (HY-12031A) and PD 98059 (HY-12028) and the EGFR inhibitor AG-1478 (HY-13524).1 LPE also increases neurite outgrowth and expression of neurofilament M in PC12 cells. LPE inhibits the activity of phospholipase D (PLD) partially purified from cabbage.3 This product contains lysophosphatidylethanolamine molecular species with variable fatty acyl chain lengths at the sn-1 position and a hydroxy group at the sn-2 position.
Choline tosylate is a nucleophilic compound that inhibits phospholipase A2 and phospholipase C. Choline tosylate inhibits tumor growth in mice by inhibiting the formation of diacylglycerol (DAG) .
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 .
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 .
Phospholipase A2 (PLA2) catalyzes the hydrolysis of the sn-2 position of membrane glycerophospholipids to liberate arachidonic acid (AA). Phospholipase A2 is a member of the class of heat-stable, calcium-dependent enzymes, is often used in biochemical studies .
PLD-IN-1 (Compound 3r) is an orally active inhibitor for phospholipase D with an IC50 of 1.97 μM. PLD-IN-1 reduces the expression of CD24, CD47 and PD-L1, enhances the calreticulin expression, and thus modulates the immune evasion mechanism in lung cancer cells by promoting the phagocytosis of cancer cells by macrophages. PLD-IN-1 inhibits the cell viability of lung cancer cell A549, HCC44, H460 and HCC15 with IC50 of 18.44, 22.31, 24.85 and 21.45 μM, respectively. PLD-IN-1 can induce apoptosis and inhibits migration in cell A549. PLD-IN-1 enhances the level of pro-inflammatory M1 macrophages and decreases the level of anti-inflammatory M2 macrophages, exhibits antitumor efficacy in mouse model .
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 lithium 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 .
Phospholipase A2, Crotalus adamanteus Venom (PLA2) catalyzes the hydrolysis of the sn-2 position of membrane glycerophospholipids to liberate arachidonic acid (AA). Phospholipase A2, Crotalus adamanteus Venom is a member of the class of heat-stable, calcium-dependent enzymes, is often used in biochemical studies .
Rhamnetin is a quercetin derivative found in Coriandrum sativum, inhibits secretory phospholipase A2, with antioxidant and anti-inflammatory activity .
N-Butylfluorescein is an alkyl-substituted fluorescein, can be used for synthesis of fluorogenic substrates for assaying phosphatidylinositol-specific phospholipase C .
Methyl γ-linolenyl fluorophosphonate (MγLnFP) is a close analog of a well-characterized, irreversible inhibitor of phospholipases, methyl arachidonyl fluorophosphonate (MAFP) .
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 .
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.
Uralsaponin D is a saponin that can be isolated from Glycyrrhiza inflata. Uralsaponin D inhibits phospholipase A2 (PLA2) with an IC50 value of 32.2 μM .
Giripladib (PLA-695) is a indole-based inhibitor of cytosolic phospholipase A2 (cPLA2). Giripladib can be used for osteoarthritis and breast cancer research .
trans-Benzylideneacetone (trans-Benzalacetone), a metabolite of gram-negative entomopathogenic bacterium Xenorhabdus nematophila, is an enzyme inhibitor against phospholipase A2 (PLA2). trans-Benzylideneacetone is an immunosuppressant .
Plipastatin A1 is a lipopeptide with enzyme inhibitory and immunosuppressive activities. Plipastatin A1 is found in Bacillus cereus and inhibits phospholipase A2 (PLA2), PLC, and PLD .
PACOCF3 (Palmityltrifluoromethylketone) is a selective phospholipase A2 inhibitor with an IC50 of 3.8 μM. PACOCF3 alters Ca 2+ signaling in renal tubular cells .
Protizinic acid is an orally active non-steroidal antiinflammatory agent with antiinflammatory and antipyretic activity. Protizinic acid inhibits phospholipase A2 (PLA2) activity, and the IC50 value is 210 μM .
Lp-PLA2-IN-16 (example 1) 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 (example 2) is a lipoprotein-associated phospholipase A2 (Lp-PLA 2) inhibitor, which can be used in the research of Alzheimer's disease, etc .
ROC-0929 (compound 13a) is a potent and selective inhibitor of secreted phospholipases A2 (sPLA2s) with an IC50 of 80 nM, specially targeting hGX. ROC-0929 inhibits the phosphorylation of ERK1/2 and p-38. Secreted phospholipases A2 (sPLA2s) are a family of disulfide-rich, Ca 2+-dependent enzymes that hydrolyze the sn-2 position of glycero-phospholipids to release a fatty acid and a lysophospholipid. ROC-0929 has the potential for researching inflammation related diseases .
Lp-PLA2-IN-4 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-4 has the potential for the research of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease (extracted from patent WO2021228159A1, compound 38) .
Lp-PLA2-IN-5 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-5 has the potential for the research of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease (extracted from patent WO2021228159A1, compound 32) .
OBAA is a potent phospholipase A2 (PLA2) inhibitor with an IC50 of 70 nM. OBAA blocks Melittin-induced Ca 2+ influx in Trypanosoma brucei with an IC50 of 0.4 μM .
7-Hydroxycoumarinyl-γ-linolenate is a cytosolic phospholipase A2 (cPLA2) fluorogenic substrate. 7-Hydroxycoumarinyl-γ-linolenate can be used to monitor the enzymatic activity of cPLA2 .
Rhamnetin (Standard) is the analytical standard of Rhamnetin. This product is intended for research and analytical applications. Rhamnetin is a quercetin derivative found in Coriandrum sativum, inhibits secretory phospholipase A2, with antioxidant and anti-inflammatory activity .
CAY10650 is a highly potent cytosolic phospholipase A2α (cPLA2α) inhibitor with an IC50 value of 12 nM. CAY10650 suppresses lipid droplets formation and PGE2 secretion .
LY-311727 is a potent secretory non-pancreatic phospholipase A2 (sPLA2) inhibitor (IC50 <1 μM for group IIA sPLA2). sPLA2 is an important proinflammatory enzyme .
Goxalapladib is a 5-HT6 receptor modulator that blocks lipoprotein-associated phospholipase A2 (Lp-PLA2) activity. Goxalapladib is promising for research of atherosclerosis-associated cardiovascular diseases .
Lp-PLA2-IN-11 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-11 has the potential for the research of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease (extracted from patent WO2014114249A1, compound E145) .
Ecopladib is a sub-micromolar inhibitor of cytosolic phospholipase A2α (cPLA2α), with IC50s of 0.15 μM and 0.11 μM in the GLU micelle and rat whole blood assays, respectively.
D609, an antitumoural xanthate, is a specific and competitive phosphatidyl choline-specific phospholipase C (PC-PLC) inhibitor with a Ki of 6.4 μM. D609 is an antioxidative protector and has antiviral and anti-inflammatory activity .
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 .
Lp-PLA2-IN-2 is a potent and selective lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor, with an IC50 0f 120 nM for recombinant human Lp-PLA2 .
Alminoprofen (EB-382) is a nonsteroidal anti-inflammatory agent (NSAID) of the phenylpropionic acid class. Alminoprofen possesses a dual anti-inflammatory action, by inhibiting both secretory phospholipase A2 (sPLA2) and COX-2 .
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-1 is a potent Lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor. Lp-PLA2-IN-1 has the potential for atherosclerosis, Alzheimer's disease research .
Lp-PLA2-IN-3 is a potent and orally bioavailable lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor, with an IC50 of 14 nM for recombinant human Lp-PLA2 (rhLpPLA2) .
Tris(2,4-di-tert-butylphenyl)phosphate is an active compound from the leaves of Vitex negundo L. shows anti-inflammatory activity with evidence of inhibition for secretory Phospholipase A2 (sPLA2) through molecular docking .
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 .
CCT129957 is an indole derivative and a potent phospholipase C-γ (PLC-γ) inhibitor with an IC50 of ~3 μM and a GC50 of 15 μM. CCT129957 inhibits Ca 2+ release in squamous carcinoma cells at ~15 μM .
(R)-Bromoenol lactone ((R)-BEL) is an irreversible, chiral, mechanism-based inhibitor of calcium-independent phospholipase γ (iPLA2γ). (R)-BEL inhibits human recombinant iPLA2γ with an IC50 of approximately 0.6 µM .
FKGK11 is a potent and selective inhibitor of GVIA iPLA2 (Group VIA calcium-independent phospholipase A2). FKGK11 can be used for the research of ovarian cancer and neurological disorders such as peripheral nerve injury and multiple sclerosis .
p-Nitrophenyl phosphorylcholine (4-Nitrophenylphosphorylcholine) is a chromogenic substrate that is used to measure phospholipase C (PLC) activity. Hydrolysis of p-nitrophenylphosphorylcholine by PLC results in the liberation of p-nitrophenol, which can be measured at 405 nm at pH 7.2-7.5.
Mastoparan X is a GTP-binding regulatory protein (G protein)-activating peptide, and a tetradecapeptide from wasp venom. Mastoparan X acts function by the direct activation of G protein that couple to phospholipase C to cause secretion from various kinds of cells .
Difluprednate (Standard) is the analytical standard of Difluprednate. This product is intended for research and analytical applications. 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.
Aristolochic acid C (Standard) is the analytical standard of Aristolochic acid C. This product is intended for research and analytical applications. 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 .
Parinaric acid is a polyunsaturated fatty acid and can be isolated from the seeds of the Makita tree. Parinaric acid provides for a natural fluorescence at 432 nm with an excitation wavelength at 320 nm. Parinaric acid can be used for the measurement of phospholipase activity, lipase activity, and as an indicator of lipid peroxidation .
LY 178002 is a potent inhibitor of 5-lipoxygenase (5-LPO), phospholipase A2, with IC50 of 0.6 μM for 5-lipoxygenase, inhibits cellular production of LTB4 by human polymorphonuclear leukocytes, and shows relatively weak inhibition on cyclooxygenase.
SKF83822 hydrobromide is a potent dopamine D1 receptor agonist. SKF83822 hydrobromide activates Gs/olf/adenylyl cyclase (AC)-coupled D1 receptors, but not phospholipase C (PLC)-coupled D1-like receptors .
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.
Phosphatidylinositol 4,5-bisphosphate (L-alpha-Phosphatidylinositol-4,5-bisphosphate), a phospholipid component of cell membranes, is a substrate for phospholipase C (PLC) and phosphoinositide 3-kinase (PI3K) and as a primary messenger .
SKF 83822 is an atypical agonist of dopamine D1 receptor. SKF 83822 activates adenylyl cyclase (AC), but not phospholipase C (PLC). SKF 83822 is also proved to stimulate AC via cAMP production. SKF 83822 can be used for research of schizophrenia .
2-(E-2-decenoylamino)ethyl 2-(cyclohexylethyl) sulfide is a compound that inhibits stress-induced ulcer and low toxicity, and can maintain the content of phospholipase A2 and prostaglandin E2 in ulcerated rats induced by water immersed restrained stress.
Compound 48/80 (Poly-p-methoxyphenethylmethylamine) is widely used in animal and tissue models as a "selective" mast cell activator. Compound 48/80 acts at the mast cell membrane to stimulate trimeric G-proteins and induces degranulation via phospholipase C and D pathways .
(S)-Bromoenol lactone ((S)-BEL) is an irreversible, chiral, mechanism-based inhibitor of calcium-independent phospholipase A2β (iPLA2β) that inhibits the vasopressin-induced release of arachidonate from cultured rat aortic smooth muscle (A10) cells with an IC50 of 2 µM .
GK241 (compound 31a-c) is a 2-oxoamide-based compound that has inhibitory activity against human and mouse group IIA secretory phospholipase A2 (GIIA sPLA2) (IC50 of 143 nM and 68 nM, respectively), and its inhibitory mechanism was studied by molecular dynamics simulation.
Compound 48/80 trihydrochloride (C48/80 trihydrochloride) is a mixture of condensation products of N-methyl-p-methoxyphenethylamine with formaldehyde. Compound 48/80 trihydrochloride is also a histamine releaser and a mast cell degranulator. Compound 48/80 inhibits phosphatidylinositol-specific phospholipase C activity from human platelets .
Alminoprofen (Standard) is the analytical standard of Alminoprofen. This product is intended for research and analytical applications. Alminoprofen (EB-382) is a nonsteroidal anti-inflammatory agent (NSAID) of the phenylpropionic acid class. Alminoprofen possesses a dual anti-inflammatory action, by inhibiting both secretory phospholipase A2 (sPLA2) and COX-2 .
Bromoenol lactone ((6E)-Bromoenol lactone) is a suicide-based irreversible, selective, potent inhibitor of calcium-independent phospholipase A2 (iPLA2β) with an IC50 value of approximately 7 μM, which inhibits antigen-stimulated mast cell exocytosis without blocking Ca 2+ influx .
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 .
Protein kinase inhibitor H-7 dihydrochloride is a potent PKC (protein kinase C) inhibitor. At 100 μM, Protein kinase inhibitor H-7 dihydrochloride completely inhibits both TPA (skin tumour promoter, 12-O-tetradecanoylphorbol-13-acetate) and phospholipase C-induced ODC (ornithine decarboxylase) .
(2E)-OBAA is a potent phospholipase A2 (PLA2) inhibitor, with an IC50 of 70 nM. (2E)-OBAA induces apoptosis of HUVEC cells. (2E)-OBAA blocks Melittin-induced Ca 2+ influx in Trypanosoma brucei, with an IC50 of 0.4 μM .
Fuzapladib (IS-741), an orally active leukocyte-function-associated antigen type 1 (LFA-1) activation inhibitor, is a leukocyte adhesion molecule. Fuzapladib is also a phospholipase A2 (PLA2) inhibitor. Fuzapladib exerts anti-inflammatory effects by inhibiting leukocyte migration into the inflammatory site .
Fuzapladib (IS-741) sodium, an orally active leukocyte-function-associated antigen type 1 (LFA-1) activation inhibitor, is a leukocyte adhesion molecule. Fuzapladib sodium is also a phospholipase A2 (PLA2) inhibitor. Fuzapladib sodium exerts anti-inflammatory effects by inhibiting leukocyte migration into the inflammatory site .
Lipstatin is a pancreatic lipase inhibitor (IC50=0.14 μM), whose structure is closely related to the known inhibitor, Esterastin. Lipstatin inhibits the absorption of triglycerides without affecting the absorption of oleic acid. Lipstatin has no inhibitory effects on other pancreatic enzymes, such as phospholipase A2 and trypsin (<200 μM) .
2-Methylbutyrylcarnitine (chloride) is a gut microbial metabolite which binds to integrin α2β1 in platelets, potentiating cytosolic phospholipase A2 (cPLA2) activation and platelet hyperresponsiveness. 2-Methylbutyrylcarnitine (chloride) enhances platelet hyperreactivity and thrombus formation in mice. 2-Methylbutyrylcarnitine (chloride) is a branched-chain acylcarnitine .
Fuzapladib (IS-741) potassium, an orally active leukocyte-function-associated antigen type 1 (LFA-1) activation inhibitor, is a leukocyte adhesion molecule. Fuzapladib potassium is also a phospholipase A2 (PLA2) inhibitor. Fuzapladib potassium exerts anti-inflammatory effects by inhibiting leukocyte migration into the inflammatory site .
Fuzapladib calcium, an orally active leukocyte-function-associated antigen type 1 (LFA-1) activation inhibitor, is a leukocyte adhesion molecule. Fuzapladib calcium is also a phospholipase A2 (PLA2) inhibitor. Fuzapladib calcium exerts anti-inflammatory effects by inhibiting leukocyte migration into the inflammatory site .
Neomycin sulfate, an aminoglycoside antibiotic, exerts antibacterial activity through irreversible binding of the nuclear 30S ribosomal subunit, thereby blocking bacterial protein synthesis. Neomycin sulfate is a known phospholipase C (PLC) inhibitor. Neomycin sulfate potently inhibits both nuclear translocation of angiogenin and angiogenin-induced cell proliferation and angiogenesis .
(E/Z)-BML264 (N-(p-amylcinnamoyl) Anthranilic Acid) is a broad spectrum Phospholipase A2 (PLA2) inhibitor and TRP channel blocker . (E/Z)-BML264 (N-(p-amylcinnamoyl) Anthranilic Acid) is also an effective reversible inhibitor of calcium-activated chloride channels, has potential to treat arrhythmia .
sPLA2-X Inhibitor 31 is a selective secreted phospholipase A2 type X (sPLA2-X) inhibitor with IC50s of 26 nM, 310 nM, and 2230 nM for sPLA2-X, sPLA2-IIa, and sPLA2-V, respectively .
U-73343, works as a protonophore, is an inactive analog of U-73122 and can be used as a negative control. U-73343 dose-dependently inhibits acid secretion irrespective of the stimulant. U-73122 is a phospholipase C (PLC) and 5-LO (5-lipoxygenase) inhibitor with an IC50 of 1-2.1 μM for PLC .
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 .
9-Oxononanoic acid (9-ONA) is secondary reaction product of lipid peroxidation. 9-Oxononanoic acid induces phospholipase A2 (PLA2) activity and thromboxane A2 (HY-113350) production (TXA2). 9-Oxononanoic acid induces the platelet aggregation in human blood. 9-Oxononanoic acid is orally active .
Varespladib (LY315920) 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 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 .
GK187 is a potent and selective Group VIA calcium-independent phospholipase A2 (GVIA iPLA2) inhibitor with an XI(50) value of 0.0001. GK187 can be used for researching various neurological disorders . [The XI(50) is the mole fraction of the inhibitor in the total substrate interface required to inhibit the enzyme by 50%.]
BAPTA is a selective chelator for calcium. BAPTA, as calcium indicator, has high selectivity against magnesium and calcium. BAPTA is widely used as an intracellular buffer for investigating the effects of Ca 2+ release from intracellular stores or influx via Ca 2+-permeable channels in the plasma membrane. BAPTA can also inhibit phospholipase C activity independently of their role as Ca 2+ chelators .
D-myo-Inositol 1,4,5-trisphosphate tripotassium, a second messenger, elicits Ca 2+ mobilization. D-myo-Inositol 1,4,5-trisphosphate tripotassium inhibits the binding of phosphoinositide-specific phospholipase C-delta 1 (PLC-delta 1) to bilayer membranes composed of phosphatidylcholine (PC) and phosphatidylinositol 4,5-bisphosphate (PIP2) .
Diheptanoyl Thio-PC is a substrate for all phospholipase A2s (PLA2s) with the exception of cPLA2 and PAF-acetyl hydrolase (PAF-AH).1 Interaction of this compound with a PLA2 results in cleavage of the sn-2 fatty acid generating a free thiol on the lysophospholipid. This free thiol can be detected using chromogenic substrates such as DTNB (Ellman’s reagent) and DTP.
AK106-001616 is a potent and selective inhibitor of cytosolic phospholipase A2 (cPLA2) (IC50=3.8 nmol/L). AK106-001616 is able to reduce the production of prostaglandins (PG) E2 and leukotrienes (LT) B4 by stimulated cells. AK106-001616 can be used in the study of inflammatory diseases, neuropathic pain and pulmonary fibrosis .
(R)-Bromoenol lactone-d7 ((R,E)-Bromoenol lactone-d7) is deuterium labeled (R)-Bromoenol lactone. (R)-Bromoenol lactone ((R)-BEL) is an irreversible, chiral, mechanism-based inhibitor of calcium-independent phospholipase γ (iPLA2γ). (R)-BEL inhibits human recombinant iPLA2γ with an IC50 of approximately 0.6 μM .
BAPTA tetrapotassium is a selective chelator for calcium. BAPTA, as calcium indicator, has high selectivity against magnesium and calcium. BAPTA tetrapotassium is widely used as an intracellular buffer for investigating the effects of Ca 2+ release from intracellular stores or influx via Ca 2+-permeable channels in the plasma membrane. BAPTA tetrapotassium can also inhibit phospholipase C activity independently of their role as Ca 2+ chelators .
GK563 is a selective Ca 2+-independent phospholipase A2 (GVIA iPLA2) inhibitor with an IC50 value of 1 nM. GK563 is 22000 times more active against GVIA iPLA2 than GIVA cPLA2. GK563 reduces β-cell apoptosis induced by proinflammatory cytokines, raising the possibility that it can be beneficial in countering autoimmune diseases, such as type 1 diabetes .
(Z)-Oleyloxyethyl phosphorylcholine ((Z)-OPC) is an isomer of Oleyloxyethyl phosphorylcholine (OPC). Oleyloxyethyl phosphorylcholine is an inhibitor of secreted Phospholipase A2 (sPLA2), which is involved in the biosynthesis of proinflammatory lipid media. Oleyloxyethyl phosphorylcholine can be used to study inflammatory diseases. Oleyloxyethyl phosphorylcholine also modified the red blood membrane and was used to bind the oxygen-carrying liquid perfluorocarbons as an antivenom agent to reduce toxin-induced hemolysis .
Scalaradial is an inhibitor for bee venom phospholipase A2 (PLA2) and transient receptor potential melastatin 2 (TRPM2) ion channels, with IC50 of 0.07 and 0.21 μM. Scalaradial regulates the phosphorylation of ERK, by inhibiting secretory PLA2 and Akt. Scalaradial inhibits the PMA (HY-18739)-induced release of Arachidonic acid (HY-109590) in the mouse peritoneal macrophage .
m-3M3FBS is a potent phospholipase C (PLC) activator. m-3M3FBS stimulates superoxide generation in human neutrophils, upregulates intracellular calcium concentration, and stimulates inositol phosphate generation in various cell lines. m-3M3FBS induces monocytic leukemia cell apoptosis .
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 .
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 Ca 2+ release from intracellular stores or influx via Ca 2+-permeable channels in the plasma membrane. BAPTA tetrasodium can also inhibit phospholipase C activity independently of their role as Ca 2+ chelators .
Melittin free acid is a basic 26-amino-acid polypeptide, the major active ingredient of honeybee venom. Melittin free acid is an activator of phospholipase A2 (PLA2). Melittin free acid has broad-spectrum antifungal activity with MIC values of 0.4-60 μM. Melittin free acid hinders fungal growth by inducing cell apoptosis, repressing (1,3)-β-D-glucan synthase and participating in other pathways .
5,7,3' -tri-O-Methyl (-)-epicatechin (Compound 13) is a phospholipase Cγ1 (PLCγ1) inhibitor. 5,7,3' -tri-o-methyl (-)-epicatechin has a methylene dioxy benzene ring and can express inhibitory activity against PLCγ1. 5,7,3' -tri-O-Methyl (-)-epicatechin can be used in the study of chemotherapy and chemopexic agents for cancer .
GTPγS (tetralithium) (Guanosine 5'-[γ-thio]triphosphate (tetralithium)) is a G-protein activator that protects proteins from proteolytic degradation, stimulates GLUT4 translocation in a tyrosine kinase-dependent manner, stimulate phospholipases and induce actin polymerization. GTPγS (tetralithium) to couple with G- protein α, to study its effect on kinase activity. GTPγS (tetralithium) acts as a component of lysis buffer .
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 .
Tris(2,4-di-tert-butylphenyl)phosphate (Standard) is the analytical standard of Tris(2,4-di-tert-butylphenyl)phosphate. This product is intended for research and analytical applications. Tris(2,4-di-tert-butylphenyl)phosphate is an active compound from the leaves of Vitex negundo L. shows anti-inflammatory activity with evidence of inhibition for secretory Phospholipase A2 (sPLA2) through molecular docking .
Ochnaflavone is an inhibitor of IIA-type secretory phospholipase A2 (sPLA2-IIA) with an IC50 of 3.45 µM. Ochnaflavone exhibits significant anti-inflammatory and liver-protective effects, capable of inhibiting the degradation of phosphatidylethanolamine (PE) and lipid peroxidation induced by carbon tetrachloride (CCl4) in rat liver, with an IC50 of 7.16 µM for lipid peroxidation. Ochnaflavone can be used in research on liver damage and inflammatory diseases .
Neomycin (sulfate) (Standard) is the analytical standard of Neomycin (sulfate). This product is intended for research and analytical applications. Neomycin sulfate, an aminoglycoside antibiotic, exerts antibacterial activity through irreversible binding of the nuclear 30S ribosomal subunit, thereby blocking bacterial protein synthesis. Neomycin sulfate is a known phospholipase C (PLC) inhibitor. Neomycin sulfate potently inhibits both nuclear translocation of angiogenin and angiogenin-induced cell proliferation and angiogenesis .
Arachidonoyl Thio-PC is a substrate of many phospholipase A2 (PLA2), including sPLA2, cPLA2 and iPLA2. Cleavage of sn-2 fatty acids by PLA2 results in the production of free thiols, which react with chromogenic reagents such as DTNB (Ellman's reagent) and DTP, allowing quantification of PLA2 activity. Isozyme-specific cPLA2 activity can be measured by depleting or inhibiting sPLA2 and iPLA2 activity in the assay.
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 .
AACOCF3 (Arachidonyl trifluoromethyl ketone) is a cell-permeant trifluoromethyl ketone analog of arachidonic acid. AACOCF3 is a potent and selective slow binding inhibitor of the 85-kDa cytosolic phospholipase A2 (cPLA2). AACOCF3 blocks production of arachidonate and 12-hydroxyeicosatetraenoic acid by calcium ionophore-challenged platelets. AACOCF3 inhibits glucose-induced insulin secretion from isolated rat islets. AACOCF3 has the potential for the research of cardiovascular disease .
GK470 (compound 28) is an inhibitor of group IVA cytosolic phospholipase A2 (GIVA cPLA2) with an IC50 of 300 nM in vesicle assays. GK470 has anti-inflammatory activity, inhibiting the release of arachidonic acid in SW982 fibroblast-like synoviocytes with an IC50 value of 0.6 μM. GK470 exhibits comparable anti-inflammatory effects to Methotrexate (HY-14519) in a preventive collagen-induced arthritis model and significantly reduces plasma PGE2 levels .
AZD2716 is a selective sPLA2 (secretory phospholipase A2) inhibitor. AZD2716 significantly reduces the production of pro-inflammatory lipids by inhibiting sPLA2-IIa (IC50 = 10 nM), sPLA2-V (IC50 = 40 nM), and sPLA2-X (IC50 = 400 nM), thereby decreasing macrophage activation and foam cell formation. AZD2716 is promising for studying mechanisms related to atherosclerosis and inflammatory diseases associated with sPLA2 .
1,2-Di-O-(9Z-octadecenyl)-sn-glycero-3-phosphocholine is a surfactant that has the activity of promoting liposome formation. 1,2-Di-O-(9Z-octadecenyl)-sn-glycero-3-phosphocholine can effectively study the biological effects of ceramide and ceramide phosphate. 1,2-Di-O-(9Z-octadecenyl)-sn-glycero-3-phosphocholine shows important application in the determination of phospholipase A activity of lecithin-cholesterol acyltransferase in ether matrix.
KT109 is a potent and an isoform-selective inhibitor of diacylglycerol lipase-β (DAGLβ) with an IC50 of 42 nM. KT109 has ~60-fold selectivity for DAGLβ over DAGLα. KT109 shows inhibitory activity against PLA2G7 (IC50=1 µM). KT109 shows negligible activity against FAAH, MGLL, ABHD11, and cytosolic phospholipase A2 (cPLA2 or PLA2G4A). KT109 perturbs a lipid network involved in macrophage inflammatory responses and lowers 2-arachidonoylglycerol (2-AG), arachidonic acid and eicosanoids in mouse peritoneal macrophages .
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 hemicalcium is the hemicalcium salt form of RK-682 (HY-135564A). RK-682 hemicalcium is the inhibitor for protein tyrosine phosphatase (PTPase), heparanase, phospholipase A2 and HIV-1 protease. RK-682 hemicalcium 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 hemicalcium 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 [2] .
S 32212 hydrochloride is an inverse agonist of 5-HT receptors5-HT2(CINI) and 5-HT2(CVSV) (Kis=6.6, 8.9 nM) and an antagonist of 5-HT2A and α2β-adrenergic receptors (Ki=5.8, 5.8 nM). S 32212 hydrochloride can reduce the binding of GTPγS to Gαq, and reduce the activity of phospholipase C (PLC) in HEK293 cells expressing 5-HT2(CINI) receptor and CHO cells expressing 5-HT2(CVSV) receptor (EC50=38 and 18.6 nM, respectively). S 32212 hydrochloride (2.5 mg/kg) reduces 5-HT receptor agonist-induced head twitches and penile erections in mice and rats. S 32212 hydrochloride (10, 40 mg/kg) reduces immobility time in the forced swim test and marble burying behavior in mice and rats, exerting antidepressant and anxiolytic activities.
7-Hydroxycoumarinyl-γ-linolenate is a cytosolic phospholipase A2 (cPLA2) fluorogenic substrate. 7-Hydroxycoumarinyl-γ-linolenate can be used to monitor the enzymatic activity of cPLA2 .
p-Nitrophenyl phosphorylcholine (4-Nitrophenylphosphorylcholine) is a chromogenic substrate that is used to measure phospholipase C (PLC) activity. Hydrolysis of p-nitrophenylphosphorylcholine by PLC results in the liberation of p-nitrophenol, which can be measured at 405 nm at pH 7.2-7.5.
Diheptanoyl Thio-PC is a substrate for all phospholipase A2s (PLA2s) with the exception of cPLA2 and PAF-acetyl hydrolase (PAF-AH).1 Interaction of this compound with a PLA2 results in cleavage of the sn-2 fatty acid generating a free thiol on the lysophospholipid. This free thiol can be detected using chromogenic substrates such as DTNB (Ellman’s reagent) and DTP.
Choline tosylate is a nucleophilic compound that inhibits phospholipase A2 and phospholipase C. Choline tosylate inhibits tumor growth in mice by inhibiting the formation of diacylglycerol (DAG) .
BAPTA is a selective chelator for calcium. BAPTA, as calcium indicator, has high selectivity against magnesium and calcium. BAPTA is widely used as an intracellular buffer for investigating the effects of Ca 2+ release from intracellular stores or influx via Ca 2+-permeable channels in the plasma membrane. BAPTA can also inhibit phospholipase C activity independently of their role as Ca 2+ chelators .
BAPTA tetrapotassium is a selective chelator for calcium. BAPTA, as calcium indicator, has high selectivity against magnesium and calcium. BAPTA tetrapotassium is widely used as an intracellular buffer for investigating the effects of Ca 2+ release from intracellular stores or influx via Ca 2+-permeable channels in the plasma membrane. BAPTA tetrapotassium can also inhibit phospholipase C activity independently of their role as Ca 2+ chelators .
Dioleoylphosphatidylglycerol (DOPG) is a naturally occurring phospholipid that can be produced by the combined action of aquaporin 3 (AQP3) and phospholipase D2 (PLD2). Dioleoylphosphatidylglycerol inhibits macrophage inflammatory mediator production in response to heat shock protein B4 (HSPB4) activation of toll-like receptor 2 (TLR2) .
Arachidonoyl Thio-PC is a substrate of many phospholipase A2 (PLA2), including sPLA2, cPLA2 and iPLA2. Cleavage of sn-2 fatty acids by PLA2 results in the production of free thiols, which react with chromogenic reagents such as DTNB (Ellman's reagent) and DTP, allowing quantification of PLA2 activity. Isozyme-specific cPLA2 activity can be measured by depleting or inhibiting sPLA2 and iPLA2 activity in the assay.
1,2-Di-O-(9Z-octadecenyl)-sn-glycero-3-phosphocholine is a surfactant that has the activity of promoting liposome formation. 1,2-Di-O-(9Z-octadecenyl)-sn-glycero-3-phosphocholine can effectively study the biological effects of ceramide and ceramide phosphate. 1,2-Di-O-(9Z-octadecenyl)-sn-glycero-3-phosphocholine shows important application in the determination of phospholipase A activity of lecithin-cholesterol acyltransferase in ether matrix.
Mastoparan X is a GTP-binding regulatory protein (G protein)-activating peptide, and a tetradecapeptide from wasp venom. Mastoparan X acts function by the direct activation of G protein that couple to phospholipase C to cause secretion from various kinds of cells .
Plipastatin A1 is a lipopeptide with enzyme inhibitory and immunosuppressive activities. Plipastatin A1 is found in Bacillus cereus and inhibits phospholipase A2 (PLA2), PLC, and PLD .
MARCKS Peptide(151-175), Phosphorylated is a phosphorylated peptide corresponding to the basic effector domain of myristoylated alanine-rich protein kinase C substrate protein (MARCKS). Phosphorylation of MARCKS Peptide (151-175) reverses its inhibition of phospholipase C (PLC)-catalyzed hydrolysis of phosphatidylinositol 4,5-bisphosphate (PIP2) .
Melittin free acid is a basic 26-amino-acid polypeptide, the major active ingredient of honeybee venom. Melittin free acid is an activator of phospholipase A2 (PLA2). Melittin free acid has broad-spectrum antifungal activity with MIC values of 0.4-60 μM. Melittin free acid hinders fungal growth by inducing cell apoptosis, repressing (1,3)-β-D-glucan synthase and participating in other pathways .
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 .
Lyso-PAF C-16 is a substrate of lysoplasmalogen (LysoPls)-specific phospholipase D (LysoPLD). Lyso-PAF C-16 selective acetylates with arachidonic acid .
Rhamnetin is a quercetin derivative found in Coriandrum sativum, inhibits secretory phospholipase A2, with antioxidant and anti-inflammatory activity .
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 .
trans-Benzylideneacetone (trans-Benzalacetone), a metabolite of gram-negative entomopathogenic bacterium Xenorhabdus nematophila, is an enzyme inhibitor against phospholipase A2 (PLA2). trans-Benzylideneacetone is an immunosuppressant .
Tris(2,4-di-tert-butylphenyl)phosphate is an active compound from the leaves of Vitex negundo L. shows anti-inflammatory activity with evidence of inhibition for secretory Phospholipase A2 (sPLA2) through molecular docking .
Uralsaponin D is a saponin that can be isolated from Glycyrrhiza inflata. Uralsaponin D inhibits phospholipase A2 (PLA2) with an IC50 value of 32.2 μM .
Rhamnetin (Standard) is the analytical standard of Rhamnetin. This product is intended for research and analytical applications. Rhamnetin is a quercetin derivative found in Coriandrum sativum, inhibits secretory phospholipase A2, with antioxidant and anti-inflammatory activity .
Aristolochic acid C (Standard) is the analytical standard of Aristolochic acid C. This product is intended for research and analytical applications. 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 .
Phosphatidylinositol 4,5-bisphosphate (L-alpha-Phosphatidylinositol-4,5-bisphosphate), a phospholipid component of cell membranes, is a substrate for phospholipase C (PLC) and phosphoinositide 3-kinase (PI3K) and as a primary messenger .
Lipstatin is a pancreatic lipase inhibitor (IC50=0.14 μM), whose structure is closely related to the known inhibitor, Esterastin. Lipstatin inhibits the absorption of triglycerides without affecting the absorption of oleic acid. Lipstatin has no inhibitory effects on other pancreatic enzymes, such as phospholipase A2 and trypsin (<200 μM) .
2-Methylbutyrylcarnitine (chloride) is a gut microbial metabolite which binds to integrin α2β1 in platelets, potentiating cytosolic phospholipase A2 (cPLA2) activation and platelet hyperresponsiveness. 2-Methylbutyrylcarnitine (chloride) enhances platelet hyperreactivity and thrombus formation in mice. 2-Methylbutyrylcarnitine (chloride) is a branched-chain acylcarnitine .
Neomycin sulfate, an aminoglycoside antibiotic, exerts antibacterial activity through irreversible binding of the nuclear 30S ribosomal subunit, thereby blocking bacterial protein synthesis. Neomycin sulfate is a known phospholipase C (PLC) inhibitor. Neomycin sulfate potently inhibits both nuclear translocation of angiogenin and angiogenin-induced cell proliferation and angiogenesis .
9-Oxononanoic acid (9-ONA) is secondary reaction product of lipid peroxidation. 9-Oxononanoic acid induces phospholipase A2 (PLA2) activity and thromboxane A2 (HY-113350) production (TXA2). 9-Oxononanoic acid induces the platelet aggregation in human blood. 9-Oxononanoic acid is orally active .
Scalaradial is an inhibitor for bee venom phospholipase A2 (PLA2) and transient receptor potential melastatin 2 (TRPM2) ion channels, with IC50 of 0.07 and 0.21 μM. Scalaradial regulates the phosphorylation of ERK, by inhibiting secretory PLA2 and Akt. Scalaradial inhibits the PMA (HY-18739)-induced release of Arachidonic acid (HY-109590) in the mouse peritoneal macrophage .
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 .
5,7,3' -tri-O-Methyl (-)-epicatechin (Compound 13) is a phospholipase Cγ1 (PLCγ1) inhibitor. 5,7,3' -tri-o-methyl (-)-epicatechin has a methylene dioxy benzene ring and can express inhibitory activity against PLCγ1. 5,7,3' -tri-O-Methyl (-)-epicatechin can be used in the study of chemotherapy and chemopexic agents for cancer .
Tris(2,4-di-tert-butylphenyl)phosphate (Standard) is the analytical standard of Tris(2,4-di-tert-butylphenyl)phosphate. This product is intended for research and analytical applications. Tris(2,4-di-tert-butylphenyl)phosphate is an active compound from the leaves of Vitex negundo L. shows anti-inflammatory activity with evidence of inhibition for secretory Phospholipase A2 (sPLA2) through molecular docking .
Ochnaflavone is an inhibitor of IIA-type secretory phospholipase A2 (sPLA2-IIA) with an IC50 of 3.45 µM. Ochnaflavone exhibits significant anti-inflammatory and liver-protective effects, capable of inhibiting the degradation of phosphatidylethanolamine (PE) and lipid peroxidation induced by carbon tetrachloride (CCl4) in rat liver, with an IC50 of 7.16 µM for lipid peroxidation. Ochnaflavone can be used in research on liver damage and inflammatory diseases .
Neomycin (sulfate) (Standard) is the analytical standard of Neomycin (sulfate). This product is intended for research and analytical applications. Neomycin sulfate, an aminoglycoside antibiotic, exerts antibacterial activity through irreversible binding of the nuclear 30S ribosomal subunit, thereby blocking bacterial protein synthesis. Neomycin sulfate is a known phospholipase C (PLC) inhibitor. Neomycin sulfate potently inhibits both nuclear translocation of angiogenin and angiogenin-induced cell proliferation and angiogenesis .
PLD4 Protein, a phospholipase, plays a crucial role in immune responses and inflammation. Dysregulation of PLD4 Protein has been associated with autoimmune disorders and inflammatory diseases. Targeting PLD4 Protein may provide potential therapeutic interventions in these conditions by modulating immune responses, suppressing inflammation, and managing related disorders. PLD4 Protein, Human (HEK293, His) is the recombinant human-derived PLD4 protein, expressed by HEK293 , with C-His labeled tag. The total length of PLD4 Protein, Human (HEK293, His) is 455 a.a., with molecular weight of 68-75 kDa.
PLD4 Protein, with 5'->3' DNA exonuclease activity, efficiently digests single-stranded DNA (ssDNA). It crucially regulates inflammatory cytokine responses by degrading nucleic acids, reducing ssDNA concentrations activating TLR9. Additionally, PLD4 actively participates in the phagocytosis process of activated microglia, emphasizing its role in immune responses. PLD4 Protein, Mouse (HEK293, His) is the recombinant mouse-derived PLD4 protein, expressed by HEK293 , with C-His labeled tag.
(R)-Bromoenol lactone-d7 ((R,E)-Bromoenol lactone-d7) is deuterium labeled (R)-Bromoenol lactone. (R)-Bromoenol lactone ((R)-BEL) is an irreversible, chiral, mechanism-based inhibitor of calcium-independent phospholipase γ (iPLA2γ). (R)-BEL inhibits human recombinant iPLA2γ with an IC50 of approximately 0.6 μM .
Dioleoylphosphatidylglycerol (DOPG) is a naturally occurring phospholipid that can be produced by the combined action of aquaporin 3 (AQP3) and phospholipase D2 (PLD2). Dioleoylphosphatidylglycerol inhibits macrophage inflammatory mediator production in response to heat shock protein B4 (HSPB4) activation of toll-like receptor 2 (TLR2) .
1,2-Di-O-(9Z-octadecenyl)-sn-glycero-3-phosphocholine is a surfactant that has the activity of promoting liposome formation. 1,2-Di-O-(9Z-octadecenyl)-sn-glycero-3-phosphocholine can effectively study the biological effects of ceramide and ceramide phosphate. 1,2-Di-O-(9Z-octadecenyl)-sn-glycero-3-phosphocholine shows important application in the determination of phospholipase A activity of lecithin-cholesterol acyltransferase in ether matrix.
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