Catalog No.
Product Name
Application
Product Information
Citations
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PCSK9 Inhibitor
PCSK9-IN-24 is a potent inhibitor of PCSK9, a key regulator of LDL receptor degradation. By reducing PCSK9 levels, this compound facilitates increased LDL uptake by cells, making it valuable for investigations into cholesterol metabolism and atherosclerosis. Its application in research can enhance the understanding of lipid disorders and aid in the development of therapeutic strategies targeting cardiovascular diseases. -
PCSK9 Inhibitor
PCSK9 modulator-4 is a potent inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9), exhibiting an EC50 value of 0.15 nM. By targeting PCSK9, this compound plays a crucial role in reducing low-density lipoprotein cholesterol (LDL-C) levels. PCSK9 modulator-4 is particularly relevant for research focused on hyperlipidemia and related cardiovascular diseases. -
PCSK9 Inhibitor
PCSK9-IN-15 is a potent inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9), with a known dissociation constant (KD) of less than 200 nM. PCSK9 plays a critical role in cholesterol metabolism, primarily regulating low-density lipoprotein cholesterol (LDL-C) levels in the bloodstream. This compound is valuable for investigating cholesterol-lowering effects and the mechanisms underlying dyslipidemia. -
Ser/Thr Protease Inhibitor
PCSK9-IN-1 is a potent cyclic peptide inhibitor of Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) with a Ki value of 1.46 nM. This compound effectively inhibits the catalytic activity of PCSK9, leading to increased low-density lipoprotein receptor (LDLR) levels. PCSK9-IN-1 can be utilized in research focused on cholesterol metabolism, cardiovascular disease, and the development of therapeutics targeting dyslipidemia. -
PCSK9
Cepadacursen sodium is an antisense oligonucleotide (ASO) that targets and inhibits the synthesis of proprotein convertase subtilisin/kexin type 9 (PCSK9) in the liver. By reducing PCSK9 levels, it plays a critical role in regulating cholesterol metabolism. This reagent is particularly relevant for research focused on hypercholesterolemia and the prevention strategies for atherosclerotic cardiovascular disease (ASCVD). -
PCSK9 allosteric binder
PCSK9 allosteric binder-1 is a novel allosteric modulator of proprotein convertase subtilisin/kexin type 9 (PCSK9). This compound effectively modifies the interaction between PCSK9 and its receptor, leading to increased LDL receptor degradation. It holds significant potential for research applications in understanding and treating cardiovascular diseases, particularly those related to lipid metabolism and cholesterol homeostasis. -
PCSK9 Inhibitor
PCSK9-IN-20 is a potent PCSK9 inhibitor with an IC50 of 3.96 µM. This compound effectively reduces PCSK9 levels and upregulates LDL receptor (LDLR) expression in vitro. It serves as a valuable tool for research applications focused on cholesterol metabolism and cardiovascular disease mechanisms. -
PCSK9 siRNA
AZD8233 is an antisense oligonucleotide (ASO) that targets proprotein convertase subtilisin/kexin type 9 (PCSK9) to inhibit its protein synthesis. By reducing levels of PCSK9, AZD8233 enhances the availability of LDL receptors, which facilitates the clearance of low-density lipoprotein (LDL) from circulation and contributes to lowering LDL cholesterol (LDL-C) levels. This compound is applicable in research focused on lipid metabolism and cardiovascular disease. -
Mast Cell Activator
Compound 48/80 is a poly-p-methoxyphenethylmethylamine that serves as a selective mast cell activator. It functions at the mast cell membrane by stimulating trimeric G-proteins, leading to degranulation through the activation of phospholipase C and D pathways. This compound is frequently utilized in animal and tissue models for research on mast cell biology and immune responses. -
Histamine Releaser/Mast Cell Degranulator
Compound 48/80 trihydrochloride serves as a potent histamine releaser and mast cell degranulator. It is composed of condensation products from N-methyl-p-methoxyphenethylamine and formaldehyde. In addition to its degranulation activity, Compound 48/80 inhibits the activity of phosphatidylinositol-specific phospholipase C in human platelets, making it a valuable tool for studying mast cell function and signal transduction pathways in pharmacological research. -
cPLA2 Inhibitor
AACOCF3, or Arachidonyl trifluoromethyl ketone, is a potent and selective inhibitor of cytosolic phospholipase A2 (cPLA2), exerting its effects through slow binding interactions. This compound is capable of blocking the production of both arachidonate and 12-hydroxyeicosatetraenoic acid in platelets stimulated by calcium ionophores. Additionally, AACOCF3 has been shown to inhibit glucose-induced insulin secretion from isolated rat islets, suggesting its potential utility in studying pathways related to cardiovascular disease and metabolic regulation. -
PLA2 Inhibitor
Pyrrophenone is a highly selective inhibitor of cytosolic phospholipase A2α (cPLA2α), exhibiting an IC50 value of 4.2 nM. This compound is valuable for research on phospholipid metabolism and inflammatory processes, as cPLA2α plays a critical role in the release of arachidonic acid and the production of inflammatory mediators. Pyrrophenone can be used to study the physiological effects of cPLA2α inhibition in various cellular and animal models. -
PGAM5 Inhibitor
LFHP-1c is a selective inhibitor of PGAM5, known for its neuroprotective properties in the context of brain ischemic stroke. This compound enhances the integrity of the blood-brain barrier by preventing ischemia-induced damage. LFHP-1c functions by binding to endothelial PGAM5, thereby inhibiting its phosphatase activity and disrupting its interaction with NRF2. It demonstrates protective effects both in vitro and in vivo, making it a valuable tool for research on ischemic conditions and related therapeutic strategies. -
N-SMase 2 Inhibitor
DPTIP is a selective inhibitor of neutral sphingomyelinase 2 (N-SMase 2), demonstrating a potent inhibitory activity with an IC50 of 30 nM. This compound effectively penetrates the blood-brain barrier, making it a valuable tool for studying the biological roles of N-SMase 2 in various neurobiological processes. Its application in research includes investigating exosome biogenesis and sphingolipid metabolism, providing insights into cellular signaling pathways in neurological disorders. -
NAPE-PLD Inhibitor
LEI-401 is a selective inhibitor of N-acylphosphatidylethanolamine phospholipase D (NAPE-PLD), exhibiting an IC50 of 27 nM. This CNS-active compound has been shown to modulate emotional behavior in mice, making it a valuable tool for research into neurochemistry and behavioral science. Its unique mechanism of action positions LEI-401 as a candidate for exploring therapeutic pathways in mood disorders and related conditions. -
Phospholipase Inhibitor
Bromoenol lactone is a selective and potent irreversible inhibitor of calcium-independent phospholipase A2 (iPLA2β), exhibiting an IC50 of approximately 7 μM. This compound effectively inhibits antigen-stimulated mast cell exocytosis without interfering with calcium influx. Bromoenol lactone is valuable for research applications aimed at understanding the roles of phospholipases in cellular processes and inflammatory responses. -
sPLA2 Inhibitor
Tris(2,4-di-tert-butylphenyl)phosphate is a potent inhibitor of secretory Phospholipase A2 (sPLA2), demonstrating significant anti-inflammatory activity. Isolated from the leaves of Vitex negundo L., this compound has been supported by molecular docking studies that confirm its inhibitory effects. It is particularly useful in research applications focused on inflammatory processes and lipid metabolism. -
PLC-γ Inhibitor
CCT129957 is a selective inhibitor of phospholipase C-γ (PLC-γ) with an IC50 of approximately 3 μM, demonstrating significant potency. This indole derivative effectively inhibits Ca2+ release in squamous carcinoma cells at a concentration of around 15 μM. CCT129957 is valuable for research applications targeting PLC-γ signaling pathways, providing insights into cellular function and disease mechanisms. -
Phospholipase Inhibitor
1-Naphthaleneacetic acid is an auxin that primarily acts as a phospholipase A2 (PLA2) inhibitor, exhibiting an IC50 of 13.16 μM. This compound is instrumental in promoting plant growth by modulating hormone levels and enhancing cell elongation. Additionally, its role in inhibiting PLA2 has made it a valuable tool in studying signaling pathways and inflammation in various biological systems. -
Phospholipase Inhibitor
MJ33 lithium salt is a competitive, reversible inhibitor targeting phospholipase A2 (PLA2). This compound specifically inhibits calcium-independent phospholipase A2 (iPLA2) activity of Prdx6, making it a valuable tool for researching phospholipid signaling pathways. MJ33 is utilized in studies focused on inflammation and cell signaling related to phospholipid metabolism. -
PTDSS1 Inhibitor
DS55980254 is an orally active inhibitor of phosphatidylserine synthase 1 (PTDSS1), effectively blocking the synthesis of intracellular phosphatidylserine. Inhibition of PTDSS1 disrupts the balance of cell membrane phospholipid components, which can subsequently activate B cell receptor (BCR) signaling pathways. This compound is valuable for research focused on phospholipid metabolism and its implications in B cell signaling and immune responses. -
SMS1 Inhibitor
SMS1-IN-1 is a potent sphingomyelin synthase 1 (SMS1) inhibitor with an IC50 of 2.1 μM. This compound demonstrates significant biological activity relevant to lipid metabolism and cellular signaling pathways. SMS1-IN-1 is primarily utilized in research focused on atherosclerosis, offering insights into its molecular mechanisms and potential therapeutic strategies. -
CalciumChelator
BAPTA tetrasodium is a selective, cell-impermeant calcium chelator that effectively targets calcium ions. With high selectivity for calcium over magnesium, it serves as an intracellular buffer to explore the dynamics of Ca2+ release from intracellular stores and its influx through Ca2+-permeable channels in plasma membranes. Additionally, BAPTA tetrasodium can inhibit phospholipase C activity, functioning independently of its chelation role, making it valuable in various biochemical and physiological research applications. -
PLA2 Inhibitor
ONO-RS-082 is a selective inhibitor of phospholipase A2 (PLA2), demonstrating an IC50 of 1.0 μM. This compound uniquely lacks activity against phospholipase C (PLC), even at concentrations up to 100 μM. ONO-RS-082 is applicable for research involving the modulation of PLA2 activity and can facilitate studies related to inflammatory processes and cell membrane dynamics. -
PLD2 Inhibitor
VU0364739 is a selective inhibitor of phospholipase D2 (PLD2) with an IC50 of 22 nM. This compound has been shown to decrease cancer cell proliferation, making it a valuable tool for studying the role of PLD2 in tumor biology. Its application in cancer research allows for further exploration of the molecular mechanisms underlying cell growth and proliferation. -
sPLA2 Inhibitor
KH064 is a potent inhibitor of secretory phospholipase A2 (sPLA2), specifically targeting human nonpancreatic secretory PLA2 isoform IIa (hnpsPLA2-IIa) with an IC50 of 29 nM. This D-tyrosine derivative exhibits significant anti-inflammatory activity, making it suitable for research applications in inflammation and related disease models. Its oral bioavailability further enhances its potential for in vivo studies in pharmacological and toxicological research. -
ASM Inhibitor
ASM-IN-1 is a potent inhibitor of acid sphingomyelinase (ASM) with an IC50 value of 1.5 µM. It exhibits significant bioactivity by reducing lipid plaques in the aortic arch and aorta, as well as decreasing plasma ceramide concentration and oxidized low-density lipoprotein (Ox-LDL) levels. ASM-IN-1 demonstrates antiatherosclerotic and anti-inflammatory properties, making it valuable for research in cardiovascular diseases and lipid metabolism. -
Phospholipase A2 Inhibitor
PACOCF3 (Palmityltrifluoromethylketone) is a selective inhibitor of phospholipase A2, demonstrating an IC50 of 3.8 μM. This compound effectively modulates Ca2+ signaling within renal tubular cells, making it a valuable tool for studying phospholipase A2-related pathways and their implications in renal physiology and pathology. Researchers can utilize PACOCF3 to explore therapeutic interventions in conditions mediated by altered phospholipid metabolism. -
Lp-PLA2 Inhibitor
GSK2647544 is an orally available, selective inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2). This enzyme is a calcium-independent phospholipase A2 involved in proinflammatory processes, primarily secreted by monocyte-derived macrophages. GSK2647544 demonstrates potential for modulation of inflammatory pathways and is applicable in research focusing on cardiovascular diseases and inflammatory disorders. -
Serine Hydrolases Inhibitor
ABC47 is a potent inhibitor of serine hydrolases, specifically targeting ABHD4 and ABHD3, with IC50 values of 0.03 μM and 0.1 μM, respectively. This compound plays a significant role in research related to infantile neuronal ceroid lipofuscinosis, making it a valuable tool for studying the mechanisms and treatment of this neurodegenerative disorder. Its specificity and potency facilitate investigations into serine hydrolase functions and their implications in various biological processes. -
cPLA2 Inhibitor
Giripladib is an indole-based inhibitor of cytosolic phospholipase A2 (cPLA2). It demonstrates potent inhibitory activity against cPLA2, making it a valuable tool for investigating inflammatory processes. Giripladib is applicable in research focused on osteoarthritis and breast cancer, facilitating studies on the role of phospholipase A2 in these conditions. -
cPLA2α Inhibitor
CAY10502 is a potent inhibitor of calcium-dependent cytosolic phospholipase A2 α (cPLA2α), exhibiting an IC50 of 4.3 nM in isolated enzyme assays. This compound is valuable for research into retinopathy and inflammatory diseases, highlighting its potential role in modulating lipid metabolism and inflammation pathways. Its specificity and efficacy provide a useful tool for elucidating cPLA2α's involvement in various pathological processes. -
Lp-PLA2 Inhibitor
SB-435495 is a potent and selective inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2), exhibiting reversible and non-covalent binding with an IC50 of 0.06 nM. This compound demonstrates significant anti-inflammatory properties and is utilized in research related to cardiovascular diseases and atherosclerosis. Its oral bioavailability makes it a valuable tool for studying Lp-PLA2's role in various disease models. -
Phospholipase Inhibitor
1-Naphthaleneacetic acid potassium salt is a synthetic auxin that primarily inhibits phospholipase A2 (PLA2) with an IC50 of 13.16 μM. This compound is utilized in plant biology to promote growth and development, as well as in biochemical studies to explore the role of PLA2 in cellular processes. Its ability to modulate enzymatic activity makes it a valuable tool in both agricultural research and molecular biology investigations. -
sPLA2 Inhibitor
Varespladib sodium is a highly selective inhibitor of group IIA secretory phospholipase A2 (sPLA2), exhibiting an IC50 of 9 nM. This compound demonstrates significant inhibition of sPLA2 activity in serum from multiple species, including rat, rabbit, guinea pig, and human, with reported IC50 values of 8.1 nM, 5.0 nM, 3.2 nM, and 6.2 nM, respectively. Varespladib sodium is instrumental in studying inflammatory processes and lipid metabolism, making it valuable for research applications related to cardiovascular diseases and other sPLA2-mediated conditions. -
nSMase2 Inhibitor
nSMase2-IN-1 is an orally active inhibitor of Neutral sphingomyelinase 2 (nSMase2), exhibiting an IC50 value of 0.13 ± 0.06 μM. This compound demonstrates metabolic stability in liver microsomes and possesses a favorable brain-to-plasma ratio, making it suitable for studies involving central nervous system diseases. nSMase2-IN-1 is a valuable reagent for research applications focused on elucidating the role of sphingolipid metabolism in neurological disorders. -
Phospholipase Inhibitor
Aristolochic acid C is a potent inhibitor of phospholipase A2 (PLA2), a key enzyme involved in various inflammatory processes. This compound has demonstrated the ability to disrupt cortical microtubule arrays, thereby influencing cellular structure and root growth in Arabidopsis. Its applications extend to studies in plant biology and the investigation of signaling pathways mediated by phospholipase activity. -
NAPE-PLD Activator
VU533 is a potent NAPE-PLD activator, with an EC50 value of 0.30 µM. This compound enhances NAPE-PLD activity and promotes efferocytosis in macrophages, making it valuable for investigating mechanisms underlying cardiometabolic diseases. VU533 serves as an important tool for researchers exploring the role of NAPE-PLD in cellular activities and disease progression. -
Choline tosylate
Choline tosylate is a nucleophilic compound that serves as an inhibitor of phospholipase A2 and phospholipase C. It demonstrates notable anti-tumor activity by impeding the formation of diacylglycerol (DAG), thereby inhibiting tumor growth in murine models. This reagent is valuable for research in cancer biology and studies focused on lipid signaling pathways. -
sPLA2 Inhibitor
LY-311727 is a potent inhibitor of secretory non-pancreatic phospholipase A2 (sPLA2), demonstrating an IC50 of less than 1 μM for group IIA sPLA2. This compound functions by blocking the enzymatic activity of sPLA2, which plays a critical role in proinflammatory processes. LY-311727 is valuable for research focused on the modulation of inflammation and the investigation of sPLA2-related biological pathways. -
Phospholipase Inhibitor
(S)-Bromoenol lactone is an irreversible inhibitor targeting calcium-independent phospholipase A2β (iPLA2β). It effectively reduces the vasopressin-induced release of arachidonate from cultured rat aortic smooth muscle (A10) cells, demonstrating an IC50 of 2 µM. This compound serves as a valuable tool for studying phospholipase activity and its role in various cellular processes. -
Secreted Phospholipases A2 Inhibitor
N-Palmitoyl-l-leucine is an inhibitor of secreted phospholipases A2, targeting the hydrolysis of membrane phospholipids. This compound exhibits significant anti-inflammatory properties and is valuable in research applications related to inflammatory diseases and conditions associated with phospholipase activity. Its ability to modulate inflammatory responses makes it a useful tool for studying mechanisms of inflammation and potential therapeutic interventions. -
Phospholipase Inhibitor
A3373 is a novel inhibitor of Phospholipase D1 (PLD1) and Phospholipase D2 (PLD2), exhibiting IC50 values of 325 nM and 15.15 μM, respectively. This compound effectively inhibits lipopolysaccharide (LPS)-induced immune responses, making it valuable for research in autoimmune arthritis, bone demineralization, and osteoclastogenesis. Its action on phospholipase pathways underscores its potential for studying related inflammatory and osteological disorders. -
Lp-PLA2 Inhibitor
Lp-PLA2-IN-13 is a selective inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2). This compound exhibits strong inhibitory activity, making it a valuable tool for investigating neurodegenerative diseases. It serves as a potential therapeutic candidate for research focused on the modulation of inflammatory processes associated with neurodegeneration. -
aSMase Inhibitor
C10 Bisphosphonate is a potent inhibitor of acid sphingomyelinase (aSMase) with an IC50 value of 0.02 μM in rat models. This compound demonstrates significant effectiveness in preventing Dexamethasone-induced apoptosis and mitigating platelet-activating factor (PAF)-induced pulmonary edema. C10 Bisphosphonate serves as a valuable tool for research focused on pulmonary edema and related cellular mechanisms. -
Phospholipase Inhibitor
Lp-PLA2-IN-3 is a powerful inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2), exhibiting an IC50 of 14 nM against recombinant human Lp-PLA2 (rhLpPLA2). This compound demonstrates significant biological activity in modulating inflammation and atherosclerosis-associated pathways. It is applicable in research focused on cardiovascular diseases and other conditions linked to phospholipid metabolism. -
Phospholipase Inhibitor
PDDC is a selective phospholipase inhibitor, specifically targeting neutral sphingomyelinase 2 (nSMase2). This compound effectively reduces tau-induced nSMase2 activity and mitigates ceramide elevation, thereby slowing tau propagation in mouse models. PDDC is utilized in research related to Alzheimer's disease, providing insights into the modulation of neurodegenerative pathways. -
rPLA/cPLA Inhibitor
EA4 is a quinone derivative that acts as an inhibitor of both secretory and cytosolic phospholipase A2 (rPLA and cPLA). It exhibits rPLA2 inhibition with a Ki value of 130 μM, making it a valuable tool for investigating the mechanisms of hemostasis, thrombosis, and erythropoiesis. This compound aids in the study of lipid metabolism and its implications in various physiological and pathological processes. -
PLCδ1 Inhibitor
N-Stearoylsphingomyelin is a sphingolipid that acts as an inhibitor of Phospholipase Cδ1 (PLCδ1). This compound plays a significant role in modulating cellular signaling pathways and is valuable in studying the physiological effects of PLCδ1 inhibition. Its applications include research in cell biology, signal transduction, and neurobiology, making it a useful reagent for investigating various biological processes. -
Phospholipase C
Phospholipase C (PLC) is an enzyme that hydrolyzes membrane phospholipids, producing diacylglycerol (DAG) and inositol triphosphate (IP3). This enzymatic activity is crucial for cellular signaling and regulation, facilitating the activation of multiple downstream signaling pathways involved in processes such as immune responses and cell growth. PLC is widely utilized in research to investigate cellular signaling mechanisms and the role of lipid mediators in health and disease.
