Acyltransferase Inhibitor

L-Penicillamine is an orally active serine palmitoyltransferase (SPT) inhibitor. L-Penicillamine inactivates the PLP cofactor by forming adducts, thereby inhibiting SPT activity and reducing sphingolipid biosynthesis. L-Penicillamine not only blocks tumor access to vitamin B6, but also stabilizes the human papillomavirus 16 E6 oncoprotein monomer and inhibits its polymerization, exhibiting a unique anticancer mechanism. L-Penicillamine effectively delays the growth of Sarcoma-180, induces tumor necrosis and prolongs survival (though long-term use may lead to Pyridoxine (HY-B1328) deficiency and weight loss).

ChAT IN-1 is a selective Choline Acetyltransferase (ChAT) inhibitor. It can be used to study mechanisms related to the overexpression of non-neuronal ChAT in cancers (e.g., colorectal and lung cancers) and Alzheimer’s disease (AD).

(Rac)-OSMI-1 is the racemate of OSMI-1. OSMI-1 is a cell-permeable O-GlcNAc transferase (OGT) inhibitor with an IC₅₀ value of 2.7 μM. OSMI-1 inhibits protein O-linked N-acetylglucosamine (O-GlcNAcylation) in several mammalian cell lines without qualitatively altering cell surface N- or O-linked glycans.

IONIS-DGAT 2Rx (ION-224) sodium is a DGAT2 inhibitor, which is promising for research of atherosclerosis.

AANAT-IN-1 is an arylalkylamine N-acetyltransferase (AANAT) inhibitor with a sheep AANAT IC₅₀ of 9.9 μM. AANAT-IN-1 binds to the active site of sheep AANAT, interacting with amino acid residues via hydrogen bonds, hydrophobic interactions, ionic interactions, and water bridges, inhibiting the enzyme's catalytic activity. AANAT-IN-1 can be used for the researches of circadian rhythm-associated neuropsychiatric conditions, seasonal affective disorder, and other diseases associated with abnormally elevated melatonin levels.

BMS-986172 is an orally active and selective Monoacylglycerol acyltransferase 2 (MGAT2) inhibitor with an IC₅₀ of 4.6 nM and 20 nM for hMGAT2 and mMGAT2, respectively. BMS-986172 reduces food intake and body weight. BMS-986172 can be used for the researches of metabolic diseases, such as obesity .

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

ST1060 is a Ceramide synthase 2 (CerS2) inhibitor. ST1060 reduces the levels of long-chain dihydroceramide (dhCer) produced by CerS2 catalysis, with IC₅₀ values of 63.6 μM and 61.3 μM for C24:0 and C24:1, respectively. ST1060 is applicable to the research of ceramide metabolism disorders and cervical cancer.

Yakuchinone B is an Acyl-CoA: cholesterol O-acyltransferase (ACAT) inhibitor with hypocholesterolemic activity, which is found in the seeds of Zingiberaceae. Yakuchinone B inhibits rat hepatic ACAT with an IC₅₀ value of 20.6 μM. Yakuchinone B is promising for research of hypercholesterolemia and atherosclerosis.

Hexadecyl-CoA is a non-hydrolyzable thioether analog of Palmitoyl-CoA. Hexadecyl-CoA competitively inhibits the acyl-CoA thioesterase activity of HNF-4α with a K_i of 0.3 μM, and inhibits DGAT2 activity with an IC₅₀ of approximately 2 μM. Hexadecyl-CoA also inhibits ATGL activity and serves as a reference inhibitor for DGAT2 LC/MS enzyme activity assays. Hexadecyl-CoA can be used in studies related to lipid metabolism, triglyceride synthesis and lipolysis.

ANAT inhibitor-2 is a ANAT inhibitor for canavan disease, with an IC₅₀ value of 20 μM.

Beauvericin-¹³C₄₅ is ¹³C labeled Beauvericin (HY-N6739). Beauvericin is a cyclohexapeptide Fusarium toxin with insecticidal, antibacterial, anticancer, antiviral and cytotoxic activities. Beauvericin causes cellular genotoxicity by producing DNA breaks, chromosomal aberrations and micronuclei, and inhibits the PI3K/AKT pathway to induce apoptosis, thereby inhibiting the growth of HCC. In addition, Beauvericin affects immune function by inhibiting lymphocyte proliferation and interfering with the differentiation process of human monocytes into macrophages.

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

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 .

Terpendole C, produced by Albophoma yamanashiensis, shows potent inhibitory activity against acyl-CoA: cholesterol acyltransferase (ACAT).

LDL-IN-1 (Compound 1) is an antioxidant, and is active against copper mediated LDL oxidation (IC₅₀ = 52 μM). LDL-IN-1 is also an Acyl-CoA:cholesterol acyltransferase-1 and -2 (ACAT-1/2) inhibitor, with IC₅₀s of 60 μM. LDL-IN-1 can be used for anti-atherosclerotic research.

Amidepsine A is a fungal metabolite isolated from the culture broth of Humicola sp. FO-2942 that inhibits Diacylglycerol acyltransferases (DGAT) activity.

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

TMP-153 is an orally active inhibitor of ACAT with an IC₅₀ value of approximately 5-10 nM against hepatic and intestinal ACAT in varicose animals. TMP-153 exhibits cholesterol-lowering effects and can be utilized in the research of atherosclerosis.

IWP-12 is a potent inhibitor of porcupine (PORCN) and inhibits cell-autonomous Wnt signaling with an IC₅₀ of 15 nM.