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Catalog No.
Product Name
Application
Product Information
Citations
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SPHK1 Inhibitor
CAY10621 is a selective inhibitor of sphingosine kinase 1 (SPHK1) with an IC50 value of 3.3 μM. This compound exhibits low cellular toxicity, making it suitable for biological studies. CAY10621 holds potential for research applications involving resistant cancer tumors, contributing to the understanding of therapeutic strategies targeting sphingosine metabolism. -
SphK2 Inhibitor
SphK2-IN-2 is a potent and selective inhibitor of sphingosine kinase 2 (SphK2) with an IC50 value of 0.23 μM. This compound demonstrates significant biological activity in regulating sphingolipid metabolism, making it a valuable tool for research applications related to cancer, neurodegenerative diseases, and inflammation. SphK2-IN-2 can aid in elucidating the role of SphK2 in various cellular pathways and the pathophysiology of related disorders. -
SphK2 Inhibitor
SLM6031434 is a selective inhibitor of sphingosine kinase 2 (SphK2) with an IC50 value of 0.4 μM. This compound promotes sphingosine accumulation and enhances Smad7 expression, leading to anti-fibrotic effects. SLM6031434 has demonstrated significant efficacy in reducing tubulointerstitial fibrosis in a mouse model of unilateral ureteral obstruction (UUO). It serves as a valuable tool for investigating proteinuric kidney diseases and chronic kidney disease (CKD). -
SphK1 Inhibitor
SLP7111228 is an inhibitor of sphingosine kinase 1 (SphK1), a key enzyme in sphingolipid metabolism. This compound effectively reduces lipopolysaccharide (LPS)-induced production of pro-inflammatory cytokines TNFα and IL-1β. SLP7111228 is valuable for research applications related to neuroinflammatory diseases, providing insights into the modulation of inflammatory responses. -
SphK2 Inhibitor
SLR080811 is a selective inhibitor of sphingosine kinase 2 (SphK2), with an inhibition constant (Ki) of 1.3 μM and approximately 10-fold selectivity over sphingosine kinase 1 (SphK1) with a Ki of 12 μM. This compound effectively reduces sphingosine 1-phosphate (S1P) levels in vitro, while also promoting a SphK1-dependent increase in S1P in in vivo mouse models. SLR080811 is suitable for research applications related to cancer and fibrosis, offering valuable insights into the role of sphingosine kinases in these disease processes. -
SphK2 Inhibitor
(R)-FTY720-OMe is a selective inhibitor of sphingosine kinase 2 (SphK2), exhibiting an IC50 of 16.5 μM. This compound is valuable in research applications related to cancer, fibrosis, Alzheimer's disease, and sickle cell disease. Its ability to modulate sphingolipid metabolism makes it an important tool for studying these pathological conditions and their underlying mechanisms. -
SphK2 Inhibitor
VT-ME6 is a selective inhibitor of sphingosine kinase 2 (SphK2), demonstrating a Ki value of 8 µM. This compound plays a pivotal role in the study of inflammatory diseases by modulating sphingolipid metabolism. Its specificity for SphK2 allows researchers to explore mechanisms underlying inflammation and related pathologies, making it a valuable tool for biochemical and pharmacological investigations. -
SphK Inhibitor
Opaganib hydrochloride is a selective, competitive inhibitor of sphingosine kinase 2 (SK2) with a Ki of 9.8 μM. This compound is valuable in studying sphingosine metabolism and signaling pathways. Its biological activities make it a potential therapeutic agent in various cancer models and inflammatory diseases. Researchers can utilize Opaganib hydrochloride to investigate the role of SK2 in disease progression and to explore novel treatment strategies. -
SPT Inhibitor
SPT-IN-2 is a potent inhibitor of serine palmitoyltransferase (SPT) with an IC50 of 0.71 nM against human SPT2. It effectively inhibits ceramide synthesis, leading to reduced intracellular ceramide and 3-ketodihydrosphingosine levels. This compound demonstrates anti-tumor activity in vivo and is characterized by favorable metabolic stability and cell membrane permeability, making it useful in cancer research. SPT-IN-2 is particularly relevant for studies involving lung adenocarcinoma, acute promyelocytic leukemia, and breast cancer. -
ACAT Inhibitor
447C88 is a potent acyl-coenzyme A cholesterol acyltransferase (ACAT) inhibitor with an IC50 value of 23 nM. It effectively reduces plasma cholesterol levels, making it valuable for research into endocrine and metabolic disorders, particularly hyperlipidemia. This compound can be utilized in studies aimed at understanding cholesterol metabolism and its implications in various diseases. -
GPAT Inhibitor
FSG67 is a potent glycerol 3-phosphate acyltransferase (GPAT) inhibitor, exhibiting an IC50 value of 24 μM. This compound is valuable for research into lipid metabolism, energy homeostasis, and related metabolic disorders. Its inhibitory action on GPAT makes it a useful tool for studying the roles of glycerolipid synthesis in various biological contexts. -
KAT8 Inhibitor
KAT8-IN-1 is an inhibitor of lysine acetyltransferase 8 (KAT8), with an IC50 of 141 μM against KAT8, alongside IC50 values of 221 μM for KAT2B and 106 μM for KAT3B. This selective inhibition of KAT8 impacts histone acetylation, making it relevant in the study of various biological processes associated with cancer and inflammatory diseases. KAT8-IN-1 is a valuable tool for researchers investigating the role of histone acetylation in gene regulation and its implications in disease mechanisms. -
SOAT2/ACAT2 Inhibitor
Pyripyropene A is a potent and selective inhibitor of sterol O-acyltransferase 2 (SOAT2) and acyl-coenzyme A:cholesterol acyltransferase 2 (ACAT2), exhibiting an IC50 of 0.07 µM. This compound effectively modulates cholesterol metabolism and has demonstrated the ability to reduce hypercholesterolemia and atherosclerosis in vivo. Pyripyropene A serves as a valuable tool for research into cholesterol-related diseases and therapeutic interventions targeting lipid metabolism. -
ACAT Inhibitor
Sandoz 58-035 is a competitive inhibitor of cholesterol acyltransferase (ACAT), demonstrating potent inhibition of cholesterol esterification in response to hormonal stimulation. This compound effectively achieves over 98% inhibition of ACAT activity in cellular models, making it valuable for research on lipid metabolism and related disorders. Sandoz 58-035 is particularly relevant for studies investigating the role of cholesterol acyltransferase in atherosclerosis and other metabolic conditions. -
zDHHC20 Inhibitor
Cyano-myracrylamide is a potent inhibitor of the zinc finger DHHC domain-containing palmitoyltransferase 20 (zDHHC20), with an IC50 value of 1.35 µM. This compound effectively inhibits S-acylation of various substrates, including EGFR, CD36, Legionella E3 ligase GobX, MyD88, and Ras, in HEK293T cells expressing recombinant variants or endogenous protein. Its ability to modulate the S-acylation process makes Cyano-myracrylamide a valuable tool for studying palmitoylation and its impact on cellular signaling pathways. -
OGT Inhibitor
ST045849 is a small-molecule inhibitor targeting O-GlcNAc transferase (OGT) with an IC50 of 30 μM against the soluble form of OGT (sOGT) and 53 μM against the nuclear/cytoplasmic form (ncOGT). This compound is valuable for studying the role of OGT in metabolism-related diseases, providing insights into regulatory mechanisms involving O-GlcNAcylation. Its application aids in understanding the biological implications of OGT inhibition in various pathological conditions. -
ACAT-1/2 Inhibitor
γ-Sanshool is a selective inhibitor of acyl-CoA cholesterol acyltransferase 1 (ACAT-1) and acyl-CoA cholesterol acyltransferase 2 (ACAT-2). This compound, derived from Zanthoxylum piperitum, exhibits inhibitory activity with IC50 values of 12.0 μM for ACAT-1 and 82.6 μM for ACAT-2. γ-Sanshool is valuable for research focused on cholesterol metabolism and cardiovascular diseases, offering insights into lipid regulation and potential therapeutic targets. -
DGAT2 Inhibitor
JNJ-DGAT2-A is a selective inhibitor of diacylglycerol acyltransferase 2 (DGAT2), demonstrating an IC50 value of 0.14 μM in human DGAT2-expressing Sf9 insect cell membranes. This compound is instrumental in studying triglyceride synthesis and its regulation, making it valuable for research focused on lipid metabolism and related metabolic disorders. Its specificity for DGAT2 allows for targeted investigations into pathways influencing energy storage and fat accumulation. -
DGAT2 Inhibitor
PF-07202954 is a potent and selective inhibitor of DGAT2, with an IC50 of 10 nM for human and 17 nM for rat DGAT2. This compound effectively reduces triglyceride synthesis, diminishes hepatic triglyceride accumulation, and lowers plasma triglyceride levels. Additionally, PF-07202954 inhibits de novo lipogenesis and suppresses the hepatic SREBP signaling pathway along with the expression of SREBP target genes. It is relevant for research on non-alcoholic steatohepatitis and related metabolic disorders. -
GPAT Inhibitor
GPAT-IN-1 is a selective inhibitor of glycerol-3-phosphate acyltransferase (GPAT), exhibiting an IC50 value of 8.9 μM. This compound effectively disrupts lipid metabolism and may play a crucial role in obesity research by influencing fatty acid synthesis and storage. Its applications extend to studies investigating metabolic disorders and exploring therapeutic strategies targeting GPAT activity. -
MGAT2 Inhibitor
BMS-963272 is a selective inhibitor of MGAT2, exhibiting an IC50 of 7.1 nM. This compound is primarily utilized in research focused on metabolic disorders and inflammatory diseases, contributing to valuable insights into underlying biochemical pathways. Its oral bioavailability enables convenient in vivo studies, enhancing its utility in preclinical models. -
Acyltransferase Inhibitor
Glabrol is a potent non-competitive inhibitor of acyl-coenzyme A: cholesterol acyltransferase (ACAT), with an IC50 value of 24.6 μM for rat liver microsomal ACAT activity. This isoprenyl flavonoid is derived from the ethanol extract of licorice roots. Glabrol is primarily utilized in research focused on lipid metabolism and cholesterol homeostasis, providing valuable insights into acyltransferase activity in various biological systems. -
ACAT1/2 Inhibitor
Pactimibe is a dual inhibitor of acyl-CoA:cholesterol acyltransferase 1 and 2 (ACAT1/2), exhibiting IC50 values of 4.9 µM and 3.0 µM, respectively. It effectively inhibits ACAT activity in liver, macrophages, and THP-1 cells with IC50s of 2.0 µM, 2.7 µM, and 4.7 µM. Additionally, Pactimibe noncompetitively inhibits oleoyl-CoA with a Ki of 5.6 µM and reduces cholesteryl ester formation with an IC50 of 6.7 µM. This compound demonstrates significant anti-atherosclerotic potential by lowering plasma cholesterol levels, making it valuable for research in cardiovascular diseases and lipid metabolism. -
OGT Inhibitor
OSMI-2 is a selective inhibitor of O-linked N-acetylglucosamine transferase (OGT), designed for cellular permeability. This compound has been shown to enhance the splicing of retained introns in various cell types, making it a valuable tool for studying the regulation of alternative splicing and OGT's role in cellular processes. OSMI-2 is applicable in various research fields, including cancer biology and neurodegenerative disorders, where OGT activity is implicated. -
Acyltransferase Inhibitor
SD-066-4 is an orally active inhibitor of acyltransferases, enzymes involved in the transfer of acyl groups across various biological processes. This compound demonstrates significant potential in cancer research by modulating lipid metabolism and cellular signaling pathways associated with tumor growth and progression. Its application in studies of cancer biology may help elucidate the role of acyltransferases in oncogenesis and therapeutic resistance. -
ACAT Inhibitor
CP-113818 is a potent inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT), targeting cholesterol metabolism. This compound is utilized in research focusing on Alzheimer's disease, where it may help elucidate the role of cholesterol in neurodegeneration and amyloid plaque formation. Its ability to modulate lipid metabolism makes it a valuable tool for investigating therapeutic strategies in neurodegenerative disorders. -
SPT Inhibitor
ALT-007 is a selective serine palmitoyltransferase (SPT) inhibitor that effectively reduces the accumulation of toxic very-long-chain deoxysphingolipids, promoting protein homeostasis. This compound has demonstrated the ability to restore age-related muscle mass loss in mouse models of sarcopenia, and enhances protein homeostasis in both murine and C. elegans models related to aging and disease. ALT-007 is a valuable tool for research focused on age-related neuromuscular disorders. -
DGAT-1 Inhibitor
DGAT1-IN-3 is a selective inhibitor of diacylglycerol O-acyltransferase 1 (DGAT-1), demonstrating potent inhibition with IC50 values of 38 nM for human DGAT-1 and 120 nM for rat DGAT-1. This compound is useful for investigating biochemical pathways related to obesity, dyslipidemia, and metabolic syndrome, offering insights into lipid metabolism and energy homeostasis. Its oral bioavailability supports in vivo studies, making it a valuable tool for researchers examining metabolic disorders. -
Ceramide Synthase Inhibitor
Fumonisin B2 is a selective inhibitor of ceramide synthase that disrupts de novo sphingolipid biosynthesis. By blocking the amide bond formation between fatty acids and dihydrosphingosine, it leads to significant intracellular accumulation of free dihydrosphingosine and altered sphingosine levels, which inhibit cell proliferation and induce cell death. Fumonisin B2 is utilized in research to study the pathogenesis of diseases linked to Fusarium verticillioides contamination, such as equine leukoencephalomalacia, porcine pulmonary edema syndrome, human esophageal cancer, and rat hepatocellular carcinoma. -
Acyl-CoA Synthetase Inhibitor
2-Fluoropalmitic acid is an acyl-CoA synthetase inhibitor that demonstrates potential as an anti-glioma agent. This compound effectively reduces the viability and stem-like characteristics of glioma stem cells (GSCs) while also inhibiting the proliferation and invasion of glioma cell lines. Its ability to target cancer cell metabolism makes it a valuable tool in glioma research and therapeutics. -
ACAT1/2 Inhibitor
Pactimibe sulfate is a dual inhibitor of acyl-CoA:cholesterol acyltransferase 1 and 2 (ACAT1/2) with IC50 values of 4.9 μM and 3.0 μM, respectively. It effectively inhibits ACAT activity in liver, macrophages, and THP-1 cells, demonstrating IC50s of 2.0 μM, 2.7 μM, and 4.7 μM, respectively. Pactimibe sulfate also noncompetitively inhibits oleoyl-CoA with a Ki value of 5.6 μM and significantly inhibits cholesteryl ester formation with an IC50 of 6.7 μM. Additionally, it exhibits anti-atherosclerotic properties by reducing plasma cholesterol levels, making it valuable for research in lipid metabolism and cardiovascular disease. -
ACAT Inhibitor
Eflucimibe is an acyl-coenzyme A cholesterol O-acyltransferase (ACAT) inhibitor that specifically targets the enzyme involved in cholesteryl ester synthesis. This compound exhibits significant biological activity in the modulation of lipid metabolism and is primarily utilized in research related to atherosclerosis and cardiovascular disease. Eflucimibe may provide insights into therapeutic strategies for managing hyperlipidemia and associated disorders. -
CPT I Inhibitor
4-Hydroxyphenylglyoxylate is a selective inhibitor of carnitine palmitoyltransferase I (CPT I), a key enzyme in fatty acid metabolism. This compound is instrumental in investigating the modulation of CPT I activity in liver mitochondria and examining the impact on fatty acid oxidation in isolated hepatocytes. Its ability to inhibit fatty acid oxidation makes it a valuable tool in metabolic research and studies related to energy homeostasis. -
SPT Inhibitor
L-Penicillamine is an orally active inhibitor of serine palmitoyltransferase (SPT), targeting the PLP cofactor to form adducts that inhibit SPT activity and subsequently reduce sphingolipid biosynthesis. This compound not only restricts tumor access to vitamin B6 but also stabilizes the human papillomavirus 16 E6 oncoprotein monomer, inhibiting its polymerization and demonstrating a distinct anticancer mechanism. In preclinical studies, L-Penicillamine has been shown to delay the growth of Sarcoma-180, induce tumor necrosis, and extend survival. Caution is advised for long-term use due to potential risks of Pyridoxine deficiency and weight loss. -
MGAT2 Inhibitor
BMS-986172 is a selective inhibitor of Monoacylglycerol acyltransferase 2 (MGAT2), demonstrating an IC50 of 4.6 nM for human MGAT2 and 20 nM for mouse MGAT2. This orally active compound has been shown to reduce food intake and body weight, making it a valuable tool for researching metabolic disorders, particularly obesity. Its efficacy in modulating MGAT2 activity supports its potential in addressing various metabolic diseases. -
ANAT inhibitor
ANAT inhibitor-2 is a selective inhibitor of the enzyme arylacetamide deacetylase (ANAT), which plays a role in the metabolism of various substrates. With an IC50 value of 20 μM, this compound demonstrates significant inhibitory activity, making it an important tool for studying canavan disease and its underlying biochemical pathways. Research applications include investigations into metabolic disorders and the development of therapeutic strategies for genetic conditions associated with ANAT dysfunction. -
AANAT Inhibitor
AANAT-IN-1 is a potent inhibitor of aralkylamine N-acetyltransferase (AANAT), demonstrating an IC50 value of 10μM. AANAT plays a critical role in the synthesis of melatonin, a hormone implicated in various disorders, including seasonal affective disorder (SAD), characterized by dysregulated melatonin levels. This compound serves as a valuable research tool for studying the mechanisms of melatonin synthesis and its impact on seasonal mood fluctuations. -
DGAT2 Inhibitor
H2-003 is a selective inhibitor of human diacylglycerol O-acyltransferase 2 (DGAT2), targeting triglyceride biosynthesis. This compound demonstrates effectiveness in inhibiting lipid droplet formation in 3T3-L1 adipocytes, making it a valuable tool for studying DGAT2 function. H2-003 is applicable in research focusing on DGAT2 and metabolic disorders associated with triglyceride accumulation. -
ACAT Inhibitor
GERI-BP002-A is an acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor derived from Aspergillus fumigatus F93. This compound is primarily utilized in cancer research, where it plays a crucial role in studying lipid metabolism and its impact on tumor progression. By inhibiting ACAT, GERI-BP002-A contributes to the alteration of cholesterol esters, facilitating investigations into lipid-related pathways in various cancer models. -
ACAT Inhibitor
Terpendole C is a potent acyl-CoA: cholesterol acyltransferase (ACAT) inhibitor derived from Albophoma yamanashiensis. This compound exhibits significant biological activity in modulating lipid metabolism by inhibiting the conversion of cholesterol to cholesteryl esters. Terpendole C is widely utilized in research focusing on cholesterol-related disorders and lipid metabolism studies. -
ACAT Inhibitor
Yakuchinone B is an Acyl-CoA: cholesterol O-acyltransferase (ACAT) inhibitor that exhibits hypocholesterolemic activity. Isolated from the seeds of Zingiberaceae, it specifically inhibits rat hepatic ACAT with an IC50 value of 20.6 μM. This compound holds potential for research applications related to hypercholesterolemia and atherosclerosis, contributing to the understanding of cholesterol metabolism and cardiovascular health. -
ACAT Inhibitor
TMP-153 is a potent inhibitor of Acyl-CoA:cholesterol acyltransferase (ACAT) with an IC50 value ranging from 5-10 nM for hepatic and intestinal ACAT, demonstrated in preclinical studies. This compound effectively reduces cholesterol levels and is primarily utilized in research related to atherosclerosis and lipid metabolism. TMP-153's mechanism of action makes it a valuable tool for studying cholesterol-related disorders and their potential therapeutic interventions. -
MGAT2 Inhibitor
S-309309 is a selective inhibitor of MGAT2, an enzyme involved in glycan biosynthesis. This compound demonstrates oral bioactivity and has potential applications in metabolism-related research, particularly in the study of lipid metabolism and its implications in metabolic disorders. S-309309 may serve as a valuable tool for investigating the role of MGAT2 in cellular pathways and metabolic regulation. -
IPNS/Acyl-CoA: 6-APA Acyltransferase Inhibitor
2,6-Dichlorophenylacetic acid acts as an inhibitor of isopenicillin N synthase (IPNS) and acyl-CoA: 6-APA acyltransferase. This compound exhibits notable cytostatic activity against tumor cells, making it a valuable tool in cancer research. Its role in modulating bacterial cell wall biosynthesis positions it as a relevant agent for studying antibiotic mechanisms and drug development. -
OGT Inhibitor
OSMI-3 is a selective inhibitor of O-linked N-acetylglucosamine transferase (OGT), characterized by its potent and cell-permeable properties. This compound effectively modulates OGT activity, leading to the enhancement of retained intron splicing in cellular contexts. OSMI-3 is valuable in research investigating the role of OGT in cellular processes and its implications in various disease states. -
ANAT Inhibitor
ANAT inhibitor-1 is a selective inhibitor of human aspartate N-acetyltransferase (ANAT), specifically developed for research into canavan disease. By inhibiting ANAT, this compound plays a crucial role in studying the biochemical pathways disrupted in this disorder. Its application extends to elucidating the mechanisms underlying neurodegenerative conditions and developing potential therapeutic strategies. -
CerS2 Inhibitor
ST1060 is a selective ceramide synthase 2 (CerS2) inhibitor. It effectively reduces the levels of long-chain dihydroceramide (dhCer) with IC50 values of 63.6 μM and 61.3 μM for C24:0 and C24:1, respectively. This compound is valuable for research applications involving lipid metabolism, cellular stress responses, and potential therapeutic strategies targeting sphingolipid pathways. -
ACAT2 Inhibitor
Eldacimibe is an inhibitor of acyl-CoA:cholesterol acyltransferase 2 (ACAT2), which plays a crucial role in cholesterol metabolism. This compound effectively reduces plasma cholesterol levels by inhibiting cholesterol absorption and preventing the transformation of macrophages into foam cells. Eldacimibe is applicable in research focused on cardiovascular diseases such as atherosclerosis, as well as endocrine and metabolic disorders, particularly hypercholesterolemia. -
GGTI Inhibitor
GGTI-2147 is a potent inhibitor of geranylgeranyl transferase I (GGTase I). It effectively blocks the geranyl-geranylation of the small GTPase Rap1A, leading to a reduction in Rac1 activity and mitigation of OGD/R-induced neuronal apoptosis. This compound is valuable for research into neurodevelopmental disorders, including autism, depression, and schizophrenia. -
GPase Inhibitor
CP-316819 is a potent inhibitor of glycogen phosphorylase (GPase), demonstrating significant antihyperglycemic activity with IC50 values of 17 nM and 34 nM against human skeletal muscle glycogen phosphorylase (huSMGPa) and liver glycogen phosphorylase (huLGPa), respectively. This compound promotes glycogen accumulation under normoglycemic conditions while allowing glycogen utilization during low glucose availability. Additionally, CP-316819 has been shown to prevent neuronal cell death and sustain brain electrical activity, making it a valuable tool for research into metabolic regulation and neuroprotection.
