Acyltransferases

Cat. No.

A69197

CAS No.

15573-67-8

4-Hydroxyphenylglyoxylate

Synonyms: 4-Hydroxyphenylglyoxylic acid; 4-HPGA

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.

Cat. No.

A69198

CAS No.

1113-41-3

L-Penicillamine

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.

Cat. No.

A69199

CAS No.

828934-40-3

(S)-(+)-Etomoxir

(S)-(+)-Etomoxir is the S enantiomer of Etomoxir, an irreversible inhibitor of carnitine palmitoyltransferase 1a (CPT-1a). This compound effectively inhibits fatty acid oxidation (FAO) by targeting CPT-1a, thereby reducing palmitate β-oxidation in human, rat, and guinea pig tissues. (S)-(+)-Etomoxir is widely used in research related to metabolism, obesity, and diabetes to explore the role of fatty acid metabolism in various physiological and pathological conditions.

Cat. No.

A69200

CAS No.

1809064-89-8

(R)-2-(3-(2-Ethoxyphenoxy)piperidin-1-yl)pyrimidine-5-carboxylic Acid

(R)-2-(3-(2-Ethoxyphenoxy)piperidin-1-yl)pyrimidine-5-carboxylic Acid serves as an important synthetic intermediate in the development of Ervogastat, a diacylglycerol acyltransferase 2 (DGAT-2) inhibitor. Its role in the synthesis of DGAT-2 inhibitors highlights its significance in studying lipid metabolism and potential therapeutic applications in managing metabolic disorders. Researchers can utilize this compound to further investigate the modulation of lipid synthesis pathways.

Cat. No.

A69201

CAS No.

1808258-99-2

BMS-986172

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.

Cat. No.

A69204

CAS No.

1048244-34-3

ANAT inhibitor-2

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.

Cat. No.

A69205

CAS No.

3055162-52-9

AANAT-IN-1

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.

Cat. No.

A69206

CAS No.

1060438-30-3

H2-003

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.

Cat. No.

A69207

CAS No.

119-47-1

GERI-BP002-A

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.

Cat. No.

A69208

CAS No.

156967-65-6

Terpendole C

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.

Cat. No.

A69209

CAS No.

81840-57-5

Yakuchinone B

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.

Cat. No.

A69210

CAS No.

615264-52-3

LDL-IN-1

LDL-IN-1 is a potent antioxidant that effectively inhibits copper-mediated LDL oxidation, with an IC50 of 52 µM. Additionally, it serves as an inhibitor of Acyl-CoA:cholesterol acyltransferase-1 and -2 (ACAT-1/2), exhibiting IC50 values of 60 µM. This compound is valuable for research into anti-atherosclerotic mechanisms and the modulation of cholesterol metabolism.

Cat. No.

A69211

CAS No.

128831-46-9

TMP-153

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.

Cat. No.

A69212

CAS No.

2267352-04-3

S-309309

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.

Cat. No.

A69213

CAS No.

6575-24-2

2,6-Dichlorophenylacetic acid

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.

Cat. No.

A69215

CAS No.

128427-86-1

C12-Sphingosine

C12-Sphingosine is a short-chain sphingosine homologue that primarily targets serine palmitoyltransferase. This reagent is known to inhibit the activity of this enzyme in primary cultured cerebellar cells, making it valuable for studying sphingolipid metabolism and its implications in neurobiology. Its applications extend to exploring cellular signaling pathways and understanding the role of sphingolipids in various physiological and pathological processes.

Cat. No.

A69218

CAS No.

331751-78-1

ANAT inhibitor-1

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.

Cat. No.

A69219

CAS No.

1402702-76-4

ST1060

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.

Cat. No.

A69220

CAS No.

179054-51-4

FR-182980

FR-182980 is a potent orally active inhibitor of acyl-CoA:cholesterol acyltransferase 1 (ACAT1), with an IC50 of 30 nM. This compound exhibits notable hypocholesterolemic activity, making it a valuable tool for the study of atherosclerosis and related lipid metabolism disorders. Researchers can utilize FR-182980 to investigate the role of ACAT1 in cholesterol homeostasis and its potential as a therapeutic target in cardiovascular diseases.

Cat. No.

A69222

CAS No.

55303-92-9

Penicillide

Synonyms: Vermixocin A

Penicillide, an acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor, is derived from the fungus Talaromyces derxii cultivated on rice. This compound exhibits significant inhibitory activity against ACAT, making it valuable for studies related to cholesterol metabolism and lipid disorders. Researchers can utilize Penicillide to explore its potential applications in understanding the regulation of cholesterol homeostasis and its implications in cardiovascular diseases.

Cat. No.

A69224

CAS No.

185539-34-8

SM-32504

SM-32504 is a potent inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT), exhibiting significant capability to lower serum cholesterol levels in mouse models subjected to high-fat and high-cholesterol diets. This compound serves as a valuable tool for studying hypercholesterolemia and atherosclerosis, providing insights into lipid metabolism and associated cardiovascular diseases.

Cat. No.

A69228

CAS No.

124884-99-7

YM-17E hydrochloride

YM-17E hydrochloride is a potent inhibitor of acyl CoA:cholesterol acyltransferase (ACAT), demonstrating an IC50 of 44 nM. This compound exhibits significant hypocholesterolemic effects, making it valuable for research in cholesterol metabolism and cardiovascular disease. Its application in studies on lipid regulation may advance understanding of lipid-related disorders.

Cat. No.

A69232

CAS No.

141993-70-6

Eldacimibe

Synonyms: WAY-ACA 147

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.

Cat. No.

A69233

CAS No.

96224-26-9

CL 277082

CL 277082 is a potent and selective inhibitor of acyl CoA:cholesterol acyltransferase (ACAT). It exhibits robust inhibitory activity with IC50 values of 0.14 μM in intestinal mucosal microsomes, 0.74 μM in liver microsomes, and 1.18 μM in rat adrenal microsomes. This compound effectively inhibits the ACAT-mediated cholesterol esterification process, making it a valuable tool for research into cholesterol absorption and metabolism.

Cat. No.

A69234

CAS No.

1710630-11-7

MGAT2-IN-2

MGAT2-IN-2 is a highly selective inhibitor of acyl CoA:monoacylglycerol acyltransferase 2 (MGAT2), demonstrating an IC50 of 3.4 nM. This compound is instrumental in studying lipid metabolism and associated metabolic disorders, making it valuable for research in obesity and diabetes. Its potent inhibitory activity offers potential avenues for therapeutic development targeting MGAT2.