palmitoyltransferase

Etomoxir sodium salt ((R)-Etomoxir sodium salt) is a carnitine palmitoyltransferase 1a (CPT-1a) inhibitor that inhibits fatty acid oxidation (FAO). Etomoxir sodium salt has antitumor activity.

McN3716 is a carnitine palmitoyltransferase I (CPT-1) inhibitor used for researching metabolic diseases.

Oxfenicine (4-Hydroxy-L-phenylglycine) is a carnitine palmitoyltransferase-1 inhibitor. Oxfenicine improves whole-body glucose tolerance and insulin sensitivity in high-fat diet-induced obese mouse with insulin resistance.

Carnitine palmitoyltransferase 2 (CPT2), an enzyme involved in fatty acid oxidation, serves as a prognostic biomarker for colorectal cancer (CRC). Overexpression of CPT2 activates phosphorylated p53, enhancing its expression, which in turn suppresses tumor growth and induces apoptosis. Conversely, a deficiency in CPT2 leads to the prevalent hereditary disorder of long-chain fatty acid oxidation in skeletal muscle. Additionally, the downregulation of CPT2 correlates strongly with the advancement of multiple cancers, highlighting its importance in cancer research [1] [2].

Myriocin (Thermozymocidin), a metabolite derived from Myriococcum albomyces, is a serine-palmitoyltransferase (SPT) inhibitor with potential antitumour, anticancer, and antiparasitic activities.Myriocin inhibits tumour growth by regulating macrophage polarisation and function through the PI3K/Akt/mTOR pathway.Myriocin inhibits HCV infection and can be used in the study of neurological diseases. Myriocin inhibits HCV infection and can be used to study neuropathy and fungal infections.

Etomoxir is an irreversible inhibitor of carnitine palmitoyltransferase 1a (CPT-1a) (IC50=5-20 nM). Etomoxir inhibits fatty acid oxidation by inhibiting CPT-1a, inhibits palmitate oxidation, has an inhibitory effect on adenine nucleotide translocase, and can inhibit macrophage polarization by disrupting CoA homeostasis.

Lipoxamycin hemisulfate (Lipoxamycin) is an inhibitor of serine palmitoyltransferase (IC50 = 21 nM) with antifungal activity.

Lipoxamycin HCl is a potent serine palmitoyltransferase inhibitor with antifungal activity and inhibits serine palmitoyltransferase activity.

GSK-7227, a novel compound representing a novel class of peroxisome proliferator-activated receptor delta (PPARδ) partial agonists, demonstrates potent partial agonistic activity by upregulating the expression of PPARδ target genes, specifically carnitine palmitoyltransferase 1a (CPT1a) and pyruvate dehydrogenase kinase 4 (PDK4), in cultured skeletal muscle cells, indicating its potential role in modulating skeletal muscle metabolism and energy homeostasis.

Teglicar (also known as ST1326) is a selective reversible inhibitor of carnitine palmitoyltransferase 1 (L-CPT1), the liver isoform. It reduces ketogenesis and glucose production, decreases gluconeogenesis, and enhances glucose homeostasis.

Cyano-myracrylamide is an inhibitor of zinc finger DHHC domain-containing palmitoyltransferase 20 (zDHHC20) with an IC50 value of 1.35 µM. It also inhibits the S-palmitoylation of EGFR and CD36. In HEK293T cells expressing recombinant E. coli GobX, recombinant human MyD88, or endogenous Ras, Cyano-myracrylamide inhibits the S-palmitoylation of E. coli E3 ligase GobX, MyD88, and Ras, which are substrates of zDHHC20, zDHHC9, and zDHHC6.

ALT-007 is an orally bioavailable inhibitor of serine palmitoyltransferase (SPT), the rate-limiting enzyme in de novo ceramide synthesis. In murine models of age-related sarcopenia, ALT-007 effectively restores muscle mass and function impaired by aging. Additionally, ALT-007 may enhance protein homeostasis in Caenorhabditis elegans and in mouse models of aging and age-associated diseases, acting as a ceramide inhibitor.

Hemiacetylcarnitinium chloride is a fatty acid metabolism inhibitor that specifically targets carnitine palmitoyltransferase I (CPT I). It disrupts the conversion of acyl-CoA to acylcarnitine, thereby blocking the subsequent oxidation of long-chain fatty acids and reducing ATP production required for energy-dependent cellular processes. Hemiacetylcarnitinium chloride is utilized in fatty acid metabolism research.

9-Oxononanoic Acid is an oxidized fatty acid, formed by the autoxidation of linoleic acid, which enhances phospholipase A2 (PLA2) activity and increases the production of thromboxane B2 in isolated human plasma.9-Oxononanoic Acid reduces hepatic neofatty acid synthesis and enhances the activity of rat hepatic carnitine palmitoyltransferase, a marker of β-oxidation. Activity.

Palmitoyl-D-carnitine is a long-chain acylcarnitine, an isomer of palmitoyl-L-carnitine , and the D enantiomer of palmitoyl-DL-carnitine . It inhibits carnitine palmitoyltransferase with a Ki value of 2.1 mM for 14C-palmitoylcarnitine synthesis by erythrocyte membranes.

1-Deoxysphingosine (m18:1(4E)) is an atypical sphingolipid that contains a double bond at the 4E native position and is formed when serine palmitoyltransferase condenses palmitoyl-CoA with alanine instead of serine during sphingolipid synthesis.1,2 Plasma levels of 1-deoxysphingosine (m18:1(4E)) are increased in patients with chronic idiopathic axonal neuropathy (CIAP) and diabetic distal symmetrical polyneuropathy (DSPN).3 |1. Steiner, R., Saied, E.M., Othman, A., et al. Elucidating the chemical structure of native 1-deoxysphingosine. J. Lipid Res. 57(7), 1194-1203 (2016).|2. Alecu, I., Othman, A., Penno, A., et al. Cytotoxic 1-deoxysphingolipids are metabolized by a cytochrome P450-dependent pathway. J. Lipid Res. 58(1), 60-71 (2017).|3. Hube, L., Dohrn, M.F., Karsai, G., et al. Metabolic syndrome, neurotoxic 1-deoxysphingolipids and nervous tissue inflammation in chronic idiopathic axonal polyneuropathy (CIAP). PLoS One 12(1):e0170583, (2017).

C22 dihydro 1-Deoxyceramide (m18:0/22:0) is a very long-chain atypical ceramide containing a 1-deoxysphinganine backbone. 1-Deoxysphingolipids are formed when serine palmitoyltransferase condenses palmitoyl-CoA with alanine instead of serine during sphingolipid synthesis.1,2 C22 dihydro 1-Deoxyceramide (m18:0/22:0) has been found in mouse embryonic fibroblasts (MEFs) following application of 1-deoxysphinganine alkyne or 1-deoxysphinganine-d3.3 It has also been found as the most prevalent dihydro deoxyceramide species in mouse brain, spinal cord, and sciatic nerve at one, three, and six months of age.4 |1. Steiner, R., Saied, E.M., Othman, A., et al. Elucidating the chemical structure of native 1-deoxysphingosine. J. Lipid Res. 57(7), 1194-1203 (2016).|2. Alecu, I., Othman, A., Penno, A., et al. Cytotoxic 1-deoxysphingolipids are metabolized by a cytochrome P450-dependent pathway. J. Lipid Res. 58(1), 60-71 (2017).|3. Alecu, I., Tedeschi, A., Behler, N., et al. Localization of 1-deoxysphingolipids to mitochondria induces mitochondrial dysfunction. J. Lipid. Res. 58(1), 42-59 (2017).|4. Schwartz, N.U., Mileva, I., Gurevich, M., et al. Quantifying 1-deoxydihydroceramides and 1-deoxyceramides in mouse nervous system tissue. Prostaglandins Other Lipid Mediat. 141, 40-48 (2019).

C24 dihydro 1-Deoxyceramide (m18:0/24:0) is a very long-chain atypical ceramide containing a 1-deoxysphinganine backbone. 1-Deoxysphingolipids are formed when serine palmitoyltransferase condenses palmitoyl-CoA with alanine instead of serine during sphingolipid synthesis.1,2 C24 dihydro 1-Deoxyceramide (m18:0/24:0) has been found in mouse embryonic fibroblasts (MEFs) following application of 1-deoxysphinganine alkyne or 1-deoxysphinganine-d3.3 It has also been found in mouse brain, spinal cord, and sciatic nerve at one, three, and six months of age.4 |1. Steiner, R., Saied, E.M., Othman, A., et al. Elucidating the chemical structure of native 1-deoxysphingosine. J. Lipid Res. 57(7), 1194-1203 (2016).|2. Alecu, I., Othman, A., Penno, A., et al. Cytotoxic 1-deoxysphingolipids are metabolized by a cytochrome P450-dependent pathway. J. Lipid Res. 58(1), 60-71 (2017).|3. Alecu, I., Tedeschi, A., Behler, N., et al. Localization of 1-deoxysphingolipids to mitochondria induces mitochondrial dysfunction. J. Lipid. Res. 58(1), 42-59 (2017).|4. Schwartz, N.U., Mileva, I., Gurevich, M., et al. Quantifying 1-deoxydihydroceramides and 1-deoxyceramides in mouse nervous system tissue. Prostaglandins Other Lipid Mediat. 141, 40-48 (2019).

C12-Sphingosine (Sphingosine (d12:1)) is a sphingosine congener with 12 carbon atoms, inducing serine palmitoyltransferase activity in a time- and concentration-dependent manner.

Aminocarnitine is an inhibitor of fatty acid oxidation that acts as a hypoglycemic and antiketogenic compound. It alters lipidic metabolism by inhibiting carnitine acetyltransferase (CAT) and carnitine palmitoyltransferase (CPT).

Clomoxir is a carnitine palmitoyltransferase I inhibitor that was under development as an antiarrhythmic and antidiabetic.

S-(-)-Etomoxir is an inhibitor of carnitine palmitoyltransferase A (CPT1) -- a molecule required for the oxidation of long-chain acyl CoA esters.

Nicotinamide-D4 is a deuterium-labelled compound of Nicotinamide (TMSM-1731) for isotope tracing. Nicotinamide, a vitamin B3 derivative, inhibits SIRT1 and SIRT2.

ARN 14494 is a potent serine palmitoyltransferase inhibitor (SPT; IC50 = 27.3 nM). ARN 14494 inhibits synthesis of long chain ceramides and dihydroceramides in an in vitro model of Alzheimer's diease. The compound prevents the synthesis of proinflammatory cytokines and the oxidative stress-related enzymes iNOS and COX-2 in mouse primary cortical astrocytes. ARN 14494 is neuroprotective against β-amyloid 1-42 induced neurotoxicity in primary cortical neurons co-cultured with astrocytes.