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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 .
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 .
Phospholipase A2 (PLA2) is a calcium-dependent, heat-stable enzyme that catalyzes the hydrolysis of glycerophospholipids at the sn-2 position of cellular membranes, thereby releasing Arachidonic Acid (AA) (HY-109590). Phospholipase A2 is a key mediator in the biosynthesis of pro-inflammatory lipid mediators, critically involved in inflammatory processes. Phospholipase A2 can be used for cardiovascular and inflammatory diseases research .
DHPG is the agonist for mGluR 1/5 (EC50 for mGluR 1 is 60 nM) that activates the phospholipase C (PLC) pathway, and leads ultimately to the activation of protein kinase C (PKC) .
Rhamnetin is a quercetin derivative found in Coriandrum sativum, inhibits secretory phospholipase A2 and histone deacetylase 2 (HDAC2). Rhamnetin exhibits antitumor, antioxidant and anti-inflammatory activity .
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 .
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 .
3-Nitrocoumarin is an inhibitor for phospholipase C that blocks the generation of inositol triphosphate (IP3), thereby affecting the calcium signaling pathway .
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 .
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 .
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.
PACOCF3 (Palmityltrifluoromethylketone) is a selective phospholipase A2 inhibitor with an IC50 of 3.8 μM. PACOCF3 alters Ca 2+ signaling in renal tubular cells .
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 .
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 .
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 Ca 2+ 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 .
Giripladib (PLA-695) is a indole-based inhibitor of cytosolic phospholipase A2 (cPLA2). Giripladib can be used for osteoarthritis and breast cancer research .
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 .
Choline tosylate (Choline p-toluenesulfonate) is an intermediate and also a substrate of choline acetyltransferase (CHAT). Choline tosylate inhibits phospholipase A2 and phospholipase C .
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 .
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 .
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 .
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.
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 .
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 .
Phospholipase C (PLCs) is a class of phospholipases. Phospholipase C participates in cellular signaling and regulation by virtue of its ability to hydrolyze membrane phospholipids into di-acyl-glycerol (DAG) and inositol triphosphate (IP3), which further causes the activation of other signaling pathways involved in various processes, including immune response .
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 .
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 .
LY433771 (LSN433771) (Compound 8) is a type X secretory phospholipase A2 (sPLA2) inhibitor with an IC50 value of 3 nM, which can be used in the study of cardiovascular diseases .
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 .
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 .
(S)-Albuterol hydrochloride is a muscarinic receptor and phospholipase C activator. (S)-Albuterol hydrochloride increases intracellular free calcium in airway smooth muscle .
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 .
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 .
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 .
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 .
A4333 is biotinylated compound of A3373 (HY-155342) that inhibits Phospholipase D1 (PLD1), but not PLD2. A4333 plays an important role in antitumor activity .
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 .
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.
Halopemide (Standard) is the analytical standard of Halopemide. This product is intended for research and analytical applications. 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 .
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 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 .
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 .
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) .
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-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) .
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-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 .
ST271 (Standard) is the analytical standard of ST271 (HY-103097). This product is intended for research and analytical applications. 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.
VU0155069 (Standard) is the analytical standard of VU0155069 (HY-108612). This product is intended for research and analytical applications. 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 .
PIP5K1B participates in the biosynthesis of PI(4,5)P2. PIP5K1B is at the crossroad of different signaling pathways, mediating RAC1-dependent reorganization of actin filaments and contributing to the activation of phospholipase D2. PIP5K1B Recombinant Human Active Lipid Kinase can be used for the study of Friedreich’s ataxia (FRDA) .
VU0359595 (Standard) is the analytical standard of VU0359595 (HY-101293). This product is intended for research and analytical applications. 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 .
Phospholipase C, Bacillus cereus (EC 3.1.4.3) is induced by thrombin and platelet-activating factor, forming 1,2-diacylglycerol and phosphatidic acid. Phospholipase C, Bacillus cereus (EC 3.1.4.3) hydrolyzes the phosphate bond on phosphatidylcholine and other glycerophospholipids yielding diacylglycerol. Phospholipase C, Bacillus cereus (EC 3.1.4.3) hydrolyzes the phosphate bonds of sphingomyelin, cardiolipin, choline plasmalogen and ceramide phospholipids.
Secreted Phospholipase A2-IIA, Human (EC 3.1.1.4), belongs to the family of antimicrobial peptides, hydrolyzes phospholipids to liberate lysophospholipids and fatty acids. Secreted Phospholipase A2-IIA, Human (EC 3.1.1.4) efficiently hydrolyzes bacterial membranes .
Ranakinin is a NK1R agonist. Ranakinin inhibits the binding of selective NK1 radioligands to NK1 receptors. Ranakinin activates phospholipase C (Phospholipase C), thereby enhancing polyphosphoinositide hydrolysis. Ranakinin stimulates inositol phosphate production and reduces membrane polyphosphoinositide levels. Ranakinin stimulates corticosterone and aldosterone secretion .
Phospholipase A2, Porcine (EC 3.1.1.4) hydrolyzes the β-ester bond of zwitterionic glycerophospholipids. Preferred substrates are phosphatidylcholine, phosphatidylethanolamine, and their plasmalogen analogues. Phosphatidylinositol and phosphatidylserine are also hydrolyzed. Phospholipase A2specifically recognizes the sn-2 acyl bond of phospholipids and catalytically hydrolyzes the bond releasing arachidonic acid and lysophospholipids.
Phospholipase A2, Streptomyces violaceoruber (EC 3.1.1.4) hydrolyzes the β-ester bond of zwitterionic glycerophospholipids. Preferred substrates are phosphatidylcholine, phosphatidylethanolamine, and their plasmalogen analogues. Phosphatidylinositol and phosphatidylserine are also hydrolyzed. Phospholipase A2specifically recognizes the sn-2 acyl bond of phospholipids and catalytically hydrolyzes the bond releasing arachidonic acid and lysophospholipids.
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 .
Phospholipase A2, Naja mossambica mossambica (EC 3.1.1.4) hydrolyzes the β-ester bond of zwitterionic glycerophospholipids. Preferred substrates are phosphatidylcholine, phosphatidylethanolamine, and their plasmalogen analogues.
Phospholipase A2, Honey bee venom (Apis mellifera) (EC 3.1.1.4) hydrolyzes the β-ester bond of zwitterionic glycerophospholipids. Preferred substrates are phosphatidylcholine, phosphatidylethanolamine, and their plasmalogen analogues.
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 .
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) .
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 .
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 .
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 .
Phosphodiesterase I, Bothrops atrox (EC 3.1.4.1) breaks phosphodiester bonds and catalyzes the hydrolysis of various nucleotide polyphosphates. Phosphodiesterase I is released from eucaryotic plasma membranes by phosphatidylinositol-specific phospholipase C.
BAPTA is a selective and cell-impermeant chelator for calcium. BAPTA has high selectivity against magnesium and calcium. BAPTA can also inhibit phospholipase C activity independently of their role as Ca 2+ chelators .
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 .
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.
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) .
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 .
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 .
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 .
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) .
Phosphodiesterase I, Crotalus atrox (Western Diamondback Rattlesnake) (EC 3.1.4.1) breaks phosphodiester bonds and catalyzes the hydrolysis of various nucleotide polyphosphates. Phosphodiesterase I is released from eucaryotic plasma membranes by phosphatidylinositol-specific phospholipase C.
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 .
BAPTA tetrasodium is a selective and cell-impermeant chelator for calcium. BAPTA tetrasodium has high selectivity against magnesium and calcium. BAPTA can also inhibit phospholipase C activity independently of their role as Ca 2+ chelators .
BAPTA tetrapotassium is a selective and cell-impermeant chelator for calcium. BAPTA has high selectivity against magnesium and calcium. BAPTA tetrapotassium can also inhibit phospholipase C activity independently of their role as Ca 2+ chelators .
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 .
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 .
5-Bromo-4-chloro-3-indoxyl myo-inositol-1-phosphate ammonium is a chromogenic substrate that can be used to detect the activity of phosphatidylinositol-specific phospholipase C (PI-PLC) .
BAPTA tetracesium is a selective and cell-impermeant chelator for calcium. BAPTA tetracesium has high selectivity against magnesium and calcium. BAPTA tetracesium can also inhibit phospholipase C activity independently of their role as Ca 2+ chelators .
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.
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 .
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 .
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 .
1,2-Bis(heptanoylthio)-sn-glycero-3-PG (1,2-Bis(heptanoylthio) glycerophosphatidylglycerol) sodium is a fatty acylthioesterified phosphatidylglycerol derivative that can be used to mimic the action of phospholipases or as a probe molecule for membrane fusion studies .
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.
DHPG (Standard) is the analytical standard of DHPG. This product is intended for research and analytical applications. DHPG is the agonist for mGluR 1/5 (EC50 for mGluR 1 is 60 nM) that activates the phospholipase C (PLC) pathway, and leads ultimately to the activation of protein kinase C (PKC) .
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.
U 84569 is a potent low-Km cAMP-dependent Phosphodiesterase inhibitor, with an IC50 value of 300 nM in platelet cytosol. By inhibiting phosphodiesterase and elevating cAMP levels, U 84569 indirectly blocks receptor-mediated Phospholipase C activation, thereby inhibiting platelet aggregation .
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 .
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 .
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 .
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 and histone deacetylase 2 (HDAC2). Rhamnetin exhibits antitumor, antioxidant and anti-inflammatory activity .
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 .
trans-Benzylideneacetone (Standard) is the analytical standard of trans-Benzylideneacetone. This product is intended for research and analytical applications. 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[1].
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 .
PACOCF3 (Standard) is the analytical standard of PACOCF3. This product is intended for research and analytical applications. PACOCF3 (Palmityltrifluoromethylketone) is a selective phospholipase A2 inhibitor with an IC50 of 3.8 μM. PACOCF3 alters Ca2+ signaling in renal tubular cells .
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.
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 .
(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 .
Parameritannin A-1 is a tetrameric proanthocyanidin (PAC) that can be isolated from the bark of Parameria laevigata Moldenke (Apocynaceae). Parameritannin A-1 is a COX-2 inhibitor. Parameritannin A-1 also inhibits the activity of phospholipase A2 (PLA2) .
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 .
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 .
Plipastatin A1 (Fengycin IX; SNA-60-367-3) is a lipopeptide with phospholipase A2 inhibitory activity. Plipastatin A1 inhibits conidial germination of Botrytis cinerea in vitro and reduces the incidence of gray mold on tomato leaves. Plipastatin A1 is applicable to research related to gray mold [1][2].
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 .
BAY-439 is a human Group V Phospholipase A2 (hPLA2-G5) inhibitor. BAY-439 can be used as a chemical probe for investigating hPLA2-G5-mediated inflammatory-related diseases, especially inflammatory pain.
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 .
(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 .
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) .
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) .
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 .
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 .
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 .
CAY10650 (Standard) is the analytical standard of CAY10650 (HY-10801). This product is intended for research and analytical applications. 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 .
Rilapladib (Standard) is the analytical standard of Rilapladib (HY-102004). This product is intended for research and analytical applications. 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 .
(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 .
PLA2-IN-1 (Compound 7) is a potent and selective inhibitor of phospholipase A2 (PLA2) with an IC50 value of 1 nM PLA2-IN-1 inhibits PLA2-induced coagulopathy in vitro. PLA2-IN-1 is promising for research of snakebite envenomation caused by cobra venom .
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 .
Lauric acid leelamide is the lauric acid (C-12) amide analog of Leelamine (HY-W005629). Leelamine exhibits inhibitory activity against pyruvate dehydrogenase kinase (PDHK) with an IC50 value of 9.5 µM. Leelamine derivatives possess anti-inflammatory effects and can inhibit phospholipase A2 activity from various sources .
Benzylideneacetone (Standard) is the analytical standard of Benzylideneacetone. This product is intended for research and analytical applications. 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 .
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 .
BAY-163 is a tertiary urea derivative and inactive negative control probe for BAY-439 (HY-178123). BAY-163 does not inhibit phospholipase A2 group V (PLA2-G5) activity in immune cells. BAY-163 can be used for research on endometriosis .
DPPI-5-P (ammonium) (PtdIns-(5)-P1) can be phosphorylated to form disphosphates such as PtdIns-(4,5)-P2. DPPI-5-P (ammonium) can also be cleaved by PI-specific phospholipase C (PLC) to give inositol triphosphates .
1,2-Dilinoleoyl-sn-glycerol is a diacylglycerol (DAG) with linoleic acid (HY-N0729) (18:2) side chains attached at both the sn-1 and sn-2 positions . 1,2-Dilinoleoyl-sn-glycerol can be prepared from L-dilinoleoylphosphatidylcholine via hydrolysis with phospholipase C .
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 .
M119 (NSC 119910) is a selective Gβγ-subunit inhibitor. M119 selectively potentiates μ-opioid-dependent antinociception. M119 inhibits μ-receptor-dependent phospholipase (PLC) activation. M119 can enhance opioid analgesia and attenuate its acute tolerance and dependence in mice. M119 can be used for pain research .
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 .
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%.]
BMS-229724 is an orally active and tight-binding cytosolic phospholipase A2 (cPLA2) inhibitor with an IC50 of 2.8 μM. BMS-229724 can inhibit the production of arachidonic acid and eicosanoids in U937 cells, neutrophils, platelets, and other cells. BMS-229724 has anti-inflammatory activity and can be used in the research of diseases such as skin inflammation .
Org 274178-0 is a selective thyroid-stimulating hormone receptor (TSHR) antagonist with a pIC50 value for TSHR is 5.03. Org 274178-0 inhibits the activation of cAMP signaling pathway and phospholipase C (PLC) signaling pathway mediated by thyroid-stimulating hormone (TSH) and TSH receptor-stimulating immunoglobulins (TSIs). Org 274178-0 is promising for research of Graves’ disease and Graves’ ophthalmopathy .
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.
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) .
WAY-196025 is a selective and orally active indole cytosolic phospholipase A2 alpha (cPLA2α) inhibitor with an IC50 of 0.01μM and a Kd of 0.013 μM. WAY-196025 can inhibit the production of prostaglandins (such as PGE2) and leukotrienes (such as LTB4), and reduce the release of inflammatory mediators. WAY-196025 can be used for the researches of inflammation and immunology, such as asthma .
15:0 Lyso PC is a lysophosphatidylcholine (Lyso PC), a product of phospholipase A2 (PLA2) hydrolysis of phosphatidylcholine (PC) and is involved in cell membrane remodeling and inflammatory signaling. 15:0 Lyso PC demonstrates significant lipid metabolism disturbances in the serum with ischemic heart disease (IHD) and ischemic cardiomyopathy (ICM). 15:0 Lyso PC can be used as a lipid biomarker for cardiovascular disease .
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 .
GTPγS (Guanosine 5'-[γ-thio]triphosphate) 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 to couple with G- protein α, to study its effect on kinase activity. GTPγS acts as a component of lysis buffer .
AURKA-IN-3 (Compound AL8) is an irreversible covalent Aurora kinase A (AURKA) inhibitor with an IC50 value of 23.0 nM. AURKA-IN-3 inhibits the activation of cAMP signaling pathway and phospholipase C (PLC) signaling pathway mediated by AURKA, and reduces the autophosphorylation level of AURKA. AURKA-IN-3 is promising for research of malignant tumors associated with high AURKA expression (e.g., leukemia, lymphoma) .
(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 .
(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 .
GTPγS (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 .
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 .
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 .
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 .
CDIBA is a cytosolic phospholipase A2 (cPLA2) inhibitor. CDIBA inhibits the activation of cPLA2 in rat diaphragm tissue. CDIBA reduces the level of mitochondrial reactive oxygen species in rat diaphragm tissue after prolonged mechanical ventilation. CDIBA attenuates protein degradation, muscle atrophy and decreased muscle strength in the diaphragm of rats after prolonged mechanical ventilation. CDIBA can be used in studies related to ventilator-induced diaphragmatic dysfunction .
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 .
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 .
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 .
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 .
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 .
Varespladib (sodium) (Standard) is the analytical standard of Varespladib (sodium). This product is intended for research and analytical applications. 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 .
LY256548 (LY25648) is an orally available anti-ischemic and anti-inflammatory compound with central nervous system activity. LY256548 is an inhibitor of phospholipase A2, 5-lipoxygenase (5-LOX), and COX, and inhibits A23187 (HY-N6687)-stimulated leukotriene B4 production. LY256548 inhibits bone damage and paw swelling in the rat Freund's complete adjuvant-induced arthritis (FCA) model .
Varespladib (Standard) is the analytical standard of Varespladib. This product is intended for research and analytical applications. 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 .
Glycerophosphoinositol 4-phosphate (GroPIns-4-P) is a metabolite of phospholipase A and an inhibitor of adenylylcyclase. Glycerophosphoinositol 4-phosphate can regulate cAMP-dependent cellular functions. Glycerophosphoinositol 4-phosphate can also induce the formation of membrane ruffles and stress fibers in serum-starved Swiss 3T3 cells by activating the small GTPases Rac and Rho, respectively. Glycerophosphoinositol 4-phosphate can be used in research on cancer cell motility and invasiveness .
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 .
Glycerophosphoinositol 4-phosphate (GroPIns-4-P) disodium is a metabolite of phospholipase A and an inhibitor of adenylylcyclase. Glycerophosphoinositol 4-phosphate disodium can regulate cAMP-dependent cellular functions. Glycerophosphoinositol 4-phosphate disodium can also induce the formation of membrane ruffles and stress fibers in serum-starved Swiss 3T3 cells by activating the small GTPases Rac and Rho, respectively. Glycerophosphoinositol 4-phosphate disodium can be used in research on cancer cell motility and invasiveness .
BAPTA (Standard) is the analytical standard of BAPTA. This product is intended for research and analytical applications. BBAPTA is a selective and cell-impermeant 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 .
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 .
U-73343 (Standard) is the analytical standard of U-73343 (HY-108630). This product is intended for research and analytical applications. 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 .
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 .
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 .
Myristinin A (YM 26567-1) is a trans-isomer flavan compound found in Horsfieldia amygdaline and Myristica cinnamomea. Myristinin A can selectively inhibit COX-2 activity with an IC50 of 16.9 μg/mL. Myristinin A can reduce the production of prostaglandin E2 (PGE2) and inhibit phospholipase A2 (PLA2), thereby blocking the release of inflammatory mediators. Myristinin A can inhibit Candida albicans with an IC50 of 8.8 μg/mL. Myristinin A can be used for the research of inflammation and infection, such as rheumatoid arthritis .
Protein kinase inhibitor H-7 (dihydrochloride) (Standard) is the analytical standard of Protein kinase inhibitor H-7 (dihydrochloride). This product is intended for research and analytical applications. 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) .
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 .
D-myo-Inositol-4-phosphate monoammonium is a metabolite of D-myo-Inositol 1,4,5-trisphosphate. D-myo-Inositol 1,4,5-trisphosphate, a second messenger, elicits Ca 2+ mobilization. D-myo-Inositol 1,4,5-trisphosphate 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) .
Rendomab B4 (Rendomab-B49) is a monoclonal antibody targeting ETB. Rendomab B4 preferentially binds to ETB in the active conformational state and exhibits selectivity for ETB on melanoma cells. Rendomab B4 inhibits the G protein-dependent phospholipase C (PLC) pathway, blocks ET-3-induced Gαi/o-mediated inhibition of adenylate cyclase, and does not affect the activation of the ERK1/2 pathway. Rendomab B4 is applicable to melanoma-related research .
15:0 Lyso PC-d5 is deuterium labeled 15:0 Lyso PC (HY-W329357). 15:0 Lyso PC is a lysophosphatidylcholine (Lyso PC), a product of phospholipase A2 (PLA2) hydrolysis of phosphatidylcholine (PC) and is involved in cell membrane remodeling and inflammatory signaling. 15:0 Lyso PC demonstrates significant lipid metabolism disturbances in the serum of patients with ischemic heart disease (IHD) and ischemic cardiomyopathy (ICM). 15:0 Lyso PC can be used as a lipid biomarker for cardiovascular disease.
Glycerophospholipids and cephalins are a class of phospholipid compounds and important components of neural membranes. Glycerophospholipids and cephalins are hydrolysis substrates of phospholipase (such as PLA2, PLC, and PLD). After complete hydrolysis, they produce 1 mol of glycerol, phosphate, ethanolamine, and 2 mol of fatty acids, respectively. Glycerophospholipids and cephalins can maintain membrane structure, fluidity, and ion permeability, and serve as precursors of second messengers such as arachidonic acid and diacylglycerol. Glycerophospholipids and cephalins can regulate signal transduction, cell apoptosis, and membrane transport, and are used in the study of neurodegenerative diseases (such as Alzheimer's disease) .
Uridine-5'-O-(3-thiotriphosphate) (UTPγS) tetrasodium, a stable analogue of Uridine triphosphate (UTP) (HY-107372), is a potent agonist of the P2Y2 and P2Y4 receptors with increased metabolic stability. Uridine-5'-O-(3-thiotriphosphate) tetrasodium stimulates inositol phosphate formation in human 1321N1 astrocytoma cells stably expressing the phospholipase C-coupled human P2U-purinoceptor (EC50 = 240 nM) .
9-Oxononanoic acid (9-ONA) is an orally active acetyl-CoA carboxylase inhibitor. 9-Oxononanoic acid inhibits acetyl-CoA carboxylase via accumulation of long-chain acyl-CoA. 9-Oxononanoic acid increases carnitine palmitoyltransferase, isocitrate dehydrogenase and glucose 6-phosphate dehydrogenase activity to elevate β-oxidation and support NADPH (HY-113324) supplyactivity. 9-Oxononanoic acid stimulates phospholipase A2 activity via post-translational, non-transcriptional mechanisms. 9-Oxononanoic acid can be used for the research of atherothrombosis .
BAPTA tetrasodium (Standard) is the analytical standard of BAPTA tetrasodium. This product is intended for research and analytical applications. BAPTA tetrasodium is a selective and cell-impermeant 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 .
CL 118326 is a potent, selective, competitive inhibitor of mammalian pancreatic phospholipase A2 (PLA2) and a weak antagonist of platelet-activating factor receptor (PAF receptor). CL 118326 competitively inhibits mammalian pancreatic PLA2 (porcine: IC50 = 1.55 μg/mL), and shows no activity against snake venom or bee venom PLA2. CL 118326 inhibits PAF-induced and thrombin-induced platelet aggregation, as well as the release of leukotriene (LTC4) and histamine from basophil-enriched leukocytes. CL 118326 can be used for research on inflammation and allergic reactions .
2-Methoxybenzoic acid (NSC 3778; O-Methylsalicylic acid; Salicylic acid methyl ether) is a natural compound with potential salicylate-like effect. 2-Methoxybenzoic acid inhibits carbonic anhydrase activity, elevates intraplatelet cyclic guanosine monophosphate level, and suppresses cytosolic phospholipase A2 phosphorylation. 2-Methoxybenzoic acid suppresses platelet reactivity, including decreased spreading, retraction, and aggregation in platelets. 2-Methoxybenzoic acid ameliorates arterial thrombosis in a dose-dependent manner without affecting normal hemostasis in mice. 2-Methoxybenzoic acid can be used for the research of arterial thrombosis .
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 .
Uridine-5'-O-(3-thiotriphosphate) (UTPγS), a stable analogue of Uridine triphosphate (UTP) (HY-107372), is a potent agonist of the P2Y2 and P2Y4 receptors with increased metabolic stability. Uridine-5'-O-(3-thiotriphosphate) stimulates inositol phosphate formation in human 1321N1 astrocytoma cells stably expressing the phospholipase C-coupled human P2U-purinoceptor (EC50 = 240 nM) .
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 .
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.
Myristinin B/C is a mixture of Myristinin B and Myristinin C. Myristinin B/C is a flavan compound found in Horsfieldia amygdaline and Myristica cinnamomea. Myristinin B/C can selectively inhibit COX-2 activity with an IC50 of 2.1 μg/mL. Myristinin B/C can reduce the production of prostaglandin E2 (PGE2) and inhibit phospholipase A2 (PLA2), thereby blocking the release of inflammatory mediators. Myristinin B/C can inhibit Candida albicans with an IC50 of 6 μg/mL. Myristinin B/C can be used for the research of inflammation and infection, such as rheumatoid arthritis .
BAPTA tetrapotassium (Standard) is the analytical standard of BAPTA tetrapotassium (HY-100168B). This product is intended for research and analytical applications. BAPTA tetrapotassium is a selective and cell-impermeant chelator for calcium. BAPTA tetrapotassium, 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 .
2-Methoxybenzoic acid (NSC 3778; O-Methylsalicylic acid; Salicylic acid methyl ether) (Standard) is the analytical standard of 2-Methoxybenzoic acid (HY-N1393). 2-Methoxybenzoic acid is a natural compound with potential salicylate-like effect. 2-Methoxybenzoic acid inhibits carbonic anhydrase activity, elevates intraplatelet cyclic guanosine monophosphate level, and suppresses cytosolic phospholipase A2 phosphorylation. 2-Methoxybenzoic acid suppresses platelet reactivity, including decreased spreading, retraction, and aggregation in platelets. 2-Methoxybenzoic acid ameliorates arterial thrombosis in a dose-dependent manner without affecting normal hemostasis in mice. 2-Methoxybenzoic acid can be used for the research of arterial thrombosis .
m-3M3FBS (Standard) is the analytical standard of m-3M3FBS. This product is intended for research and analytical applications. 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 .
Neomycin, an aminoglycoside antibiotic, exerts antibacterial activity through irreversible binding of the nuclear 30S ribosomal subunit, thereby blocking bacterial protein synthesis. Neomycin is a known phospholipase C (PLC) inhibitor. Neomycin potently inhibits both the nuclear translocation of angiogenin and angiogenin-induced cell proliferation and angiogenesis. Neomycin inhibits IP3-mediated Ca 2+ release, MgATP-dependent Ca 2+ uptake, and electrical excitation-evoked skeletal muscle Ca 2+ transients. Neomycin depletes gut microbiota in specific mouse models, causes hearing impairment, and kidney damage with prolonged exposure. Neomycin can be used for the research of cancer .
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 .
XEN445 is a potent, selective and orally active endothelial lipase (EL) inhibitor with an IC50 value of 0.237 μM. XEN445 selectively inhibits phospholipase enzymatic activity of LIPG. XEN445 raises plasma HDL and cholesterol levles. XEN445 induces G1cell cycle arrest, reduces cell viability, suppresses cancer stem cell self-renewal, and inhibits tumor formation in LIPG-expressing triple-negative breast cancer cells, while showing no inhibitory effect on invasiveness or cancer stem cell stemness in these cells. XEN445 can be used for the research of cancer and metabolic disease, such as triple-negative breast cancer .
2-Methoxybenzoic acid (NSC 3778; O-Methylsalicylic acid; Salicylic acid methyl ether)-d3 is deuterium-labeled 2-Methoxybenzoic acid (HY-N1393). 2-Methoxybenzoic acid is a natural compound with potential salicylate-like effect. 2-Methoxybenzoic acid inhibits carbonic anhydrase activity, elevates intraplatelet cyclic guanosine monophosphate level, and suppresses cytosolic phospholipase A2 phosphorylation. 2-Methoxybenzoic acid suppresses platelet reactivity, including decreased spreading, retraction, and aggregation in platelets. 2-Methoxybenzoic acid ameliorates arterial thrombosis in a dose-dependent manner without affecting normal hemostasis in mice. 2-Methoxybenzoic acid can be used for the research of arterial thrombosis .
Phosphatidylinositol 4,5-bisphosphate (L-alpha-Phosphatidylinositol-4,5-bisphosphate) is a plasma membrane lipid that is enriched in the cytoplasmic leaflet of the plasma membrane. Phosphatidylinositol 4,5-bisphosphate serves as a substrate for phospholipase C and class I PI3K, generating diacylglycerol, inositol (1,4,5)-trisphosphate, and phosphatidylinositol (3,4,5)-trisphosphate. Phosphatidylinositol 4,5-bisphosphate contributes to lamellipodial protrusion, directional cell migration, focal adhesion lipid generation, and trafficking of the GABAA receptor. Phosphatidylinositol 4,5-bisphosphate can be used in research related to acute lung injury and pulmonary edema .
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 (HY-W011051), Arachidonic acid (HY-109590) and eicosanoids in mouse peritoneal macrophages .
2-Methoxybenzoic acid (NSC 3778; O-Methylsalicylic acid; Salicylic acid methyl ether)- 13C6 is the 13C-labeled 2-Methoxybenzoic acid (HY-N1393). 2-Methoxybenzoic acid is a natural compound with potential salicylate-like effect. 2-Methoxybenzoic acid inhibits carbonic anhydrase activity, elevates intraplatelet cyclic guanosine monophosphate level, and suppresses cytosolic phospholipase A2 phosphorylation. 2-Methoxybenzoic acid suppresses platelet reactivity, including decreased spreading, retraction, and aggregation in platelets. 2-Methoxybenzoic acid ameliorates arterial thrombosis in a dose-dependent manner without affecting normal hemostasis in mice. 2-Methoxybenzoic acid can be used for the research of arterial thrombosis .
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 the nuclear translocation of angiogenin and angiogenin-induced cell proliferation and angiogenesis. Neomycin sulfate inhibits IP3-mediated Ca 2+ release, MgATP-dependent Ca 2+ uptake, and electrical excitation-evoked skeletal muscle Ca 2+ transients. Neomycin sulfate depletes gut microbiota in specific mouse models, causes hearing impairment, and kidney damage with prolonged exposure. Neomycin sulfate can be used for the research of cancer .
D-myo-Inositol-2,4,5-triphosphate (Ins(2,4,5)P3) (sodium salt) is a second messenger produced in cells by phospholipase C-mediated hydrolysis of phosphatidylinositol-4,5-biphosphate. D-myo-Inositol-2,4,5-triphosphate (sodium salt) can open calcium channels and increase intracellular calcium upon binding to its receptors on the endoplasmic reticulum. D-myo-Inositol-2,4,5-triphosphate (sodium salt) also acts as a partial agonist at rat hepatic IP3 receptors. D-myo-Inositol-2,4,5-triphosphate (sodium salt) can be studied in research on calcium ions signaling pathway .
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] .
MJ-33 is a competitive phospholipase A₂ (PLA₂) inhibitor with an IC50 of 0.3 μM. MJ-33 inhibits the activation of NOX2 by blocking the PLA₂ activity of Prdx6, thereby reducing the production of ROS. MJ-33 effectively inhibits the activity of acidic PLA₂ (pH 4.0), reduces the degradation of pulmonary surfactant phosphatidylcholine (PC), but has no effect on alkaline PLA₂ (pH 8.5). MJ-33 significantly alleviates lung oxidative damage induced by ischemia-reperfusion (I/R). MJ-33 significantly inhibits the invasive, migratory and adhesive abilities of prostate cancer cells by suppressing the MAPK, AKT, NF-κB and AP-1 signaling pathways. MJ-33 can be used to study ROS-related diseases and prostate cancer .
MJ-33 lithium salt is a competitive phospholipase A2 (PLA2) inhibitor with an IC50 of 0.3 μM. MJ-33 lithium salt inhibits NOX2 activation and reduces ROS production by blocking the PLA2 activity of Prdx6. MJ-33 lithium salt effectively inhibits the activity of acidic PLA2 (pH 4.0) and reduces the degradation of alveolar surfactant phosphatidylcholine (PC), but exerts no effect on alkaline PLA2 (pH 8.5). MJ-33 lithium salt significantly alleviates lung oxidative injury induced by ischemia-reperfusion (I/R). MJ-33 lithium salt significantly inhibits the invasion, migration and adhesion abilities of prostate cancer cells by suppressing the MAPK, AKT, NF-κB and AP-1 signaling pathways. MJ-33 lithium salt can be used for the research of ROS-related diseases and prostate cancer .
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.
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.
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 .
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.
BAPTA is a selective and cell-impermeant chelator for calcium. BAPTA has high selectivity against magnesium and calcium. BAPTA can also inhibit phospholipase C activity independently of their role as Ca 2+ chelators .
Glycerophospholipids and cephalins are a class of phospholipid compounds and important components of neural membranes. Glycerophospholipids and cephalins are hydrolysis substrates of phospholipase (such as PLA2, PLC, and PLD). After complete hydrolysis, they produce 1 mol of glycerol, phosphate, ethanolamine, and 2 mol of fatty acids, respectively. Glycerophospholipids and cephalins can maintain membrane structure, fluidity, and ion permeability, and serve as precursors of second messengers such as arachidonic acid and diacylglycerol. Glycerophospholipids and cephalins can regulate signal transduction, cell apoptosis, and membrane transport, and are used in the study of neurodegenerative diseases (such as Alzheimer's disease) .
BAPTA tetrapotassium is a selective and cell-impermeant chelator for calcium. BAPTA has high selectivity against magnesium and calcium. BAPTA tetrapotassium can also inhibit phospholipase C activity independently of their role as Ca 2+ chelators .
Choline tosylate (Choline p-toluenesulfonate) is an intermediate and also a substrate of choline acetyltransferase (CHAT). Choline tosylate inhibits phospholipase A2 and phospholipase C .
15:0 Lyso PC is a lysophosphatidylcholine (Lyso PC), a product of phospholipase A2 (PLA2) hydrolysis of phosphatidylcholine (PC) and is involved in cell membrane remodeling and inflammatory signaling. 15:0 Lyso PC demonstrates significant lipid metabolism disturbances in the serum with ischemic heart disease (IHD) and ischemic cardiomyopathy (ICM). 15:0 Lyso PC can be used as a lipid biomarker for cardiovascular disease .
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.
BAPTA (Standard) is the analytical standard of BAPTA. This product is intended for research and analytical applications. BBAPTA is a selective and cell-impermeant 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 .
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.
BAPTA tetrapotassium (Standard) is the analytical standard of BAPTA tetrapotassium (HY-100168B). This product is intended for research and analytical applications. BAPTA tetrapotassium is a selective and cell-impermeant chelator for calcium. BAPTA tetrapotassium, 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 .
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 Ca 2+ 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 .
Plipastatin A1 (Fengycin IX; SNA-60-367-3) is a lipopeptide with phospholipase A2 inhibitory activity. Plipastatin A1 inhibits conidial germination of Botrytis cinerea in vitro and reduces the incidence of gray mold on tomato leaves. Plipastatin A1 is applicable to research related to gray mold [1][2].
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 .
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 .
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 .
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) .
Ranakinin is a NK1R agonist. Ranakinin inhibits the binding of selective NK1 radioligands to NK1 receptors. Ranakinin activates phospholipase C (Phospholipase C), thereby enhancing polyphosphoinositide hydrolysis. Ranakinin stimulates inositol phosphate production and reduces membrane polyphosphoinositide levels. Ranakinin stimulates corticosterone and aldosterone secretion .
Rendomab B4 (Rendomab-B49) is a monoclonal antibody targeting ETB. Rendomab B4 preferentially binds to ETB in the active conformational state and exhibits selectivity for ETB on melanoma cells. Rendomab B4 inhibits the G protein-dependent phospholipase C (PLC) pathway, blocks ET-3-induced Gαi/o-mediated inhibition of adenylate cyclase, and does not affect the activation of the ERK1/2 pathway. Rendomab B4 is applicable to melanoma-related research .
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 the nuclear translocation of angiogenin and angiogenin-induced cell proliferation and angiogenesis. Neomycin sulfate inhibits IP3-mediated Ca 2+ release, MgATP-dependent Ca 2+ uptake, and electrical excitation-evoked skeletal muscle Ca 2+ transients. Neomycin sulfate depletes gut microbiota in specific mouse models, causes hearing impairment, and kidney damage with prolonged exposure. Neomycin sulfate can be used for the research of cancer .
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 .
Rhamnetin is a quercetin derivative found in Coriandrum sativum, inhibits secretory phospholipase A2 and histone deacetylase 2 (HDAC2). Rhamnetin exhibits antitumor, antioxidant and anti-inflammatory activity .
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 .
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 .
2-Methoxybenzoic acid (NSC 3778; O-Methylsalicylic acid; Salicylic acid methyl ether) is a natural compound with potential salicylate-like effect. 2-Methoxybenzoic acid inhibits carbonic anhydrase activity, elevates intraplatelet cyclic guanosine monophosphate level, and suppresses cytosolic phospholipase A2 phosphorylation. 2-Methoxybenzoic acid suppresses platelet reactivity, including decreased spreading, retraction, and aggregation in platelets. 2-Methoxybenzoic acid ameliorates arterial thrombosis in a dose-dependent manner without affecting normal hemostasis in mice. 2-Methoxybenzoic acid can be used for the research of arterial thrombosis .
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 .
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 .
Phosphatidylinositol 4,5-bisphosphate (L-alpha-Phosphatidylinositol-4,5-bisphosphate) is a plasma membrane lipid that is enriched in the cytoplasmic leaflet of the plasma membrane. Phosphatidylinositol 4,5-bisphosphate serves as a substrate for phospholipase C and class I PI3K, generating diacylglycerol, inositol (1,4,5)-trisphosphate, and phosphatidylinositol (3,4,5)-trisphosphate. Phosphatidylinositol 4,5-bisphosphate contributes to lamellipodial protrusion, directional cell migration, focal adhesion lipid generation, and trafficking of the GABAA receptor. Phosphatidylinositol 4,5-bisphosphate can be used in research related to acute lung injury and pulmonary edema .
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 .
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 .
9-Oxononanoic acid (9-ONA) is an orally active acetyl-CoA carboxylase inhibitor. 9-Oxononanoic acid inhibits acetyl-CoA carboxylase via accumulation of long-chain acyl-CoA. 9-Oxononanoic acid increases carnitine palmitoyltransferase, isocitrate dehydrogenase and glucose 6-phosphate dehydrogenase activity to elevate β-oxidation and support NADPH (HY-113324) supplyactivity. 9-Oxononanoic acid stimulates phospholipase A2 activity via post-translational, non-transcriptional mechanisms. 9-Oxononanoic acid can be used for the research of atherothrombosis .
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 .
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 .
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 .
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 .
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 .
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 and histone deacetylase 2 (HDAC2). Rhamnetin exhibits antitumor, antioxidant and anti-inflammatory activity .
trans-Benzylideneacetone (Standard) is the analytical standard of trans-Benzylideneacetone. This product is intended for research and analytical applications. 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[1].
Parameritannin A-1 is a tetrameric proanthocyanidin (PAC) that can be isolated from the bark of Parameria laevigata Moldenke (Apocynaceae). Parameritannin A-1 is a COX-2 inhibitor. Parameritannin A-1 also inhibits the activity of phospholipase A2 (PLA2) .
Benzylideneacetone (Standard) is the analytical standard of Benzylideneacetone. This product is intended for research and analytical applications. 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 .
2-Methoxybenzoic acid (NSC 3778; O-Methylsalicylic acid; Salicylic acid methyl ether) (Standard) is the analytical standard of 2-Methoxybenzoic acid (HY-N1393). 2-Methoxybenzoic acid is a natural compound with potential salicylate-like effect. 2-Methoxybenzoic acid inhibits carbonic anhydrase activity, elevates intraplatelet cyclic guanosine monophosphate level, and suppresses cytosolic phospholipase A2 phosphorylation. 2-Methoxybenzoic acid suppresses platelet reactivity, including decreased spreading, retraction, and aggregation in platelets. 2-Methoxybenzoic acid ameliorates arterial thrombosis in a dose-dependent manner without affecting normal hemostasis in mice. 2-Methoxybenzoic acid can be used for the research of arterial thrombosis .
Myristinin A (YM 26567-1) is a trans-isomer flavan compound found in Horsfieldia amygdaline and Myristica cinnamomea. Myristinin A can selectively inhibit COX-2 activity with an IC50 of 16.9 μg/mL. Myristinin A can reduce the production of prostaglandin E2 (PGE2) and inhibit phospholipase A2 (PLA2), thereby blocking the release of inflammatory mediators. Myristinin A can inhibit Candida albicans with an IC50 of 8.8 μg/mL. Myristinin A can be used for the research of inflammation and infection, such as rheumatoid arthritis .
Myristinin B/C is a mixture of Myristinin B and Myristinin C. Myristinin B/C is a flavan compound found in Horsfieldia amygdaline and Myristica cinnamomea. Myristinin B/C can selectively inhibit COX-2 activity with an IC50 of 2.1 μg/mL. Myristinin B/C can reduce the production of prostaglandin E2 (PGE2) and inhibit phospholipase A2 (PLA2), thereby blocking the release of inflammatory mediators. Myristinin B/C can inhibit Candida albicans with an IC50 of 6 μg/mL. Myristinin B/C can be used for the research of inflammation and infection, such as rheumatoid arthritis .
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.
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.
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 .
(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 .
15:0 Lyso PC-d5 is deuterium labeled 15:0 Lyso PC (HY-W329357). 15:0 Lyso PC is a lysophosphatidylcholine (Lyso PC), a product of phospholipase A2 (PLA2) hydrolysis of phosphatidylcholine (PC) and is involved in cell membrane remodeling and inflammatory signaling. 15:0 Lyso PC demonstrates significant lipid metabolism disturbances in the serum of patients with ischemic heart disease (IHD) and ischemic cardiomyopathy (ICM). 15:0 Lyso PC can be used as a lipid biomarker for cardiovascular disease.
2-Methoxybenzoic acid (NSC 3778; O-Methylsalicylic acid; Salicylic acid methyl ether)- 13C6 is the 13C-labeled 2-Methoxybenzoic acid (HY-N1393). 2-Methoxybenzoic acid is a natural compound with potential salicylate-like effect. 2-Methoxybenzoic acid inhibits carbonic anhydrase activity, elevates intraplatelet cyclic guanosine monophosphate level, and suppresses cytosolic phospholipase A2 phosphorylation. 2-Methoxybenzoic acid suppresses platelet reactivity, including decreased spreading, retraction, and aggregation in platelets. 2-Methoxybenzoic acid ameliorates arterial thrombosis in a dose-dependent manner without affecting normal hemostasis in mice. 2-Methoxybenzoic acid can be used for the research of arterial thrombosis .
2-Methoxybenzoic acid (NSC 3778; O-Methylsalicylic acid; Salicylic acid methyl ether)-d3 is deuterium-labeled 2-Methoxybenzoic acid (HY-N1393). 2-Methoxybenzoic acid is a natural compound with potential salicylate-like effect. 2-Methoxybenzoic acid inhibits carbonic anhydrase activity, elevates intraplatelet cyclic guanosine monophosphate level, and suppresses cytosolic phospholipase A2 phosphorylation. 2-Methoxybenzoic acid suppresses platelet reactivity, including decreased spreading, retraction, and aggregation in platelets. 2-Methoxybenzoic acid ameliorates arterial thrombosis in a dose-dependent manner without affecting normal hemostasis in mice. 2-Methoxybenzoic acid can be used for the research of arterial thrombosis .
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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Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
MedchemExpress Validation 03
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
MedchemExpress Validation 04
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
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