Acyltransferases

Cat. No.

A11415

CAS No.

828934-41-4

Etomoxir (sodium salt)

Synonyms: (R)-(+)-Etomoxir

Etomoxir is an inhibitor of carnitine palmitoyltransferase A (CPT1), which is required for the oxidation of long-chain acyl CoA esters. Also a strong inhibitor of mitochondrial CPT1 and a candidate as an anti-diabetic drug.

Cat. No.

A11395

CAS No.

138046-43-2

YM 750

YM 750 is reported to act as a SOAT (acyl-CoA:cholesterol acyltransferase, ACAT) inhibitor.

Cat. No.

A12640

CAS No.

1808094-07-6

PF-06471553

PF-06471553 is a potent, selective and orally available monoacylglycerol acyltransferase 3 (MGAT3) inhibitor, with an IC50 of 92 nM.

Cat. No.

A14395

CAS No.

133825-80-6

Nevanimibe (ATR-101)

Synonyms: ATR 101; PD-132301

ATR-101 is in clinical development for the treatment of adrenocortical carcinoma (ACC).

Cat. No.

A16369

CAS No.

228544-65-8

VULM 1457

VULM 1457 is an Acyl-CoA: cholesterol acyltransferase (ACAT) or SOAT inhibitor. VULM 1457 decreases cholesterol levels in the liver and plasma.

Cat. No.

A16370

CAS No.

114289-47-3

CI 976

Synonyms: PD 128042

CI 976 is a trimethoxy fatty acid anilide inhibitor of liver and intestinal acyl coenzyme A cholesterol acyltransferase (ACAT) and sterol O-acyltransferase (SOAT). Cl 976 lowers non-high density lipoprotein (non-HDL) cholesterol and increases HDL-cholesterol concentrations.

Cat. No.

A16471

CAS No.

456-59-7

Cyclandelate

Synonyms: BS 572

Cyclandelate is an effective inhibitor of rat hepatic acycloenzyme A: cholesterol acyltransferase (ACAT) with IC50 of 80 μM.

Cat. No.

A16879

CAS No.

1452473-54-9

GOAT-IN-1

GOAT-IN-1 is an inhibitor of ghrelin O-acyltransferase (GOAT), which could be useful for the prophylaxis or treatment of obesity, diabetes, hyperlipidemia, metabolic, non-alcoholic fatty liver, steatohepatitis, sarcopenia, appetite control, alcohol/narcotic dependence, Alzheimer's disease, Parkinson's disease, cerebrovascular dementia, cerebral apoplexy, cerebral infarction, cardic disease, some kind of tumors.

Cat. No.

A18635

CAS No.

215589-63-2

FR-190809

Synonyms: FR190809.

FR-190809 is a potent, nonadrenotoxic, orally efficacious ACAT inhibitor.

Cat. No.

A19362

CAS No.

136609-26-2

RP 70676

RP 70676 is a potent inhibitor of ACAT, with IC50 of 25 and 44 nM for rat and rabbit ACAT.

Cat. No.

A19631

CAS No.

14417-88-0

Melinamide

Synonyms: AC 223; DL-N-(α-Methylbenzyl)linoleamide

Melinamide, an amide derivative of an unsaturated long-chain fatty acid, is an inhibitor of cholesterol absorption with an IC50 of 20.9 μM.

Cat. No.

A19983

CAS No.

1800025-30-2

TP-020 (MGAT2-IN-1)

Synonyms: MGAT2-IN-1

MGAT2-IN-1 is an orally active inhibitor of monoacylglycerol acyltransferase (MGAT2) with IC50 of 7.8 and 2.4 nM for human and mouse MGAT2, respectively.

Cat. No.

A20093

CAS No.

145961-79-1

ACAT-IN-1 cis isomer

ACAT-IN-1 cis isomer is a potent ACAT inhibitor with an IC50 of 100 nM.

Cat. No.

A20229

CAS No.

124900-72-7

YM17E

YM17E is an inhibitor of acyl CoA:cholesterol acyltransferase (ACAT), with IC50 of 44 nM in rabbit liver microsomes in vitro.

Cat. No.

A20330

CAS No.

136609-53-5

RP 73163 Racemate

Synonyms: RP73163

RP 73163 Racemate is the racemate of RP 73163. RP 73163 is a potent ACAT inhibitor, with cholesterol lowering activity.

Cat. No.

A20707

CAS No.

141799-76-0

E-5324

E-5324 is potent inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT) with IC50s of 44 to 190 nM.

Cat. No.

A21108

CAS No.

135239-65-5

RP-64477

RP-64477 is a potent inhibitor of the cholesterol esterifying enzyme Acyl-coenzyme A:cholesterol O-acyltransferase (ACAT).

Cat. No.

A21767

CAS No.

133825-81-7

Nevanimibe hydrochloride

Synonyms: PD-132301 hydrochloride; PD132301; ATR101 hydrochloride; ATR 101

Nevanimibe hydrochloride (PD-132301 hydrochloride; ATR101 hydrochloride) is a selective and potent acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) inhibitor with an EC50 of 9 nM.

Cat. No.

A21773

CAS No.

217094-32-1

K-604 dihydrochloride

Synonyms: K604

K-604 dihydrochloride is a potent and selective acyl-CoA:cholesterol acyltransferase 1 (ACAT-1) inhibitor with an IC50 of 0.45±0.06 μM.

Cat. No.

A24136

CAS No.

19914-20-6

Enniatin B1

Enniatin B1 is a mycotoxin produced by Fusarium species, known for its diverse bioactivities. It functions as a moderate inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT), with an IC₅₀ of 73 μM in assays using rat liver microsomes, implicating a role in lipid metabolism modulation. Enniatin B1 is capable of crossing the blood-brain barrier, suggesting potential effects on central nervous system function. It also decreases the activation of ERK1/2 (p44/p42 MAPK) and moderately inhibits TNF-α-induced NF-κB activation, indicating anti-inflammatory and cell signaling modulatory properties.

Cat. No.

A24578

CAS No.

2748196-63-4

P053

P053 is a potent, non-competitive, and selective inhibitor of ceramide synthase 1 (CerS1), exhibiting an IC₅₀ of 0.5 μM. It functions as an endogenous regulator of mitochondrial fatty acid oxidation in skeletal muscle, influencing cellular energy metabolism. By modulating ceramide synthesis, P053 also acts as a systemic regulator of whole-body adiposity, making it a valuable compound for studying lipid metabolism, energy homeostasis, and metabolic disorders.

Cat. No.

A24596

CAS No.

11113-62-5

Enniatin complex

Enniatin complex is a mixture of cyclohexadepsipeptides isolated largely from Fusarium species of fungi, and has ionophoric, antibiotic, and in vitro hypolipidaemic properties. Enniatin complex inhibits enzymes like acyl-CoA: cholesterol acyl transferase and induces apoptosis in several cancer lines .

Cat. No.

A30897

CAS No.

1037837-27-6

ARN14494

ARN14494 is a selective inhibitor of serine palmitoyltransferase (SPT), exhibiting an IC50 of 27.3 nM. This compound demonstrates significant neuroprotective and anti-inflammatory effects, particularly in the context of Alzheimer's disease research. ARN14494 has been shown to safeguard neurons against β-amyloid 1-42-induced neurotoxicity through mechanisms such as antioxidant activity, anti-apoptotic effects, and the modulation of inflammatory responses. This makes ARN14494 a valuable tool for investigating therapeutic strategies for neurodegenerative disorders.

Cat. No.

A36083

CAS No.

242794-72-5

Ilekudinol B

Ilekudinol B is an inhibitor of ACAT and PTP1B, demonstrating an IC50 of 5.3 μM and a Ki of 11.6 μM against human PTP1B. This compound also inhibits the classical pathway of the complement system with an IC50 of 51 μM. Ilekudinol B is known to reduce TNF-α-induced IL-8 secretion and enhance glucose uptake in skeletal muscle myotubes, functioning as both an insulin mimetic and sensitizer. It is a valuable reagent for research focused on type 2 diabetes, obesity, and inflammatory diseases.

Cat. No.

A44216

CAS No.

688353-45-9

IWP-12

IWP-12 is a potent inhibitor of the acyltransferase porcupine (PORCN), significantly impacting cell-autonomous Wnt signaling pathways. With an IC50 value of 15 nM, IWP-12 effectively disrupts the Wnt signaling cascade, making it a valuable tool for studying the role of Wnt in various biological processes and diseases. This compound is particularly useful in cancer research and developmental biology applications.