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.

Etomoxir is a carnitine palmitoyltransferase 1a (CPT-1a) inhibitor that inhibits fatty acid oxidation by inhibiting CPT-1a and inhibits palmitate oxidation in humans, rats, and guinea pigs. Etomoxir has an inhibitory effect on adenine nucleotide translocase and can inhibit macrophage polarization by disrupting CoA homeostasis.

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

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

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).

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

Nicotinamide-d4 is intended for use as an internal standard for the quantification of nicotinamide by GC- or LC-MS. Nicotinamide is an amide form of niacin, which is also known as vitamin B3, that can be biosynthesized in vivo or obtained through the diet. It is a precursor in the synthesis of the metabolic cofactor NAD+ and an inhibitor of sirtuin 1 (SIRT1; IC50 = <50 µM). Nicotinamide (10 µM) increases the activity of serine palmitoyltransferase (SPT) and the biosynthesis of ceramide, glucosylceramide, sphingomyelin, free fatty acids, and cholesterol in primary human keratinocytes. Nicotinamide (40 µM) induces apoptosis in SNU-398, SNU-739, and HepG2 hepatocellular carcinoma (HCC) cells, and it prevents the formation of neoplastic lesions in a diethylnitrosamine-induced mouse model of HCC. Unlike niacin, nicotinamide does not reduce plasma lipid levels or induce flushing.

Malonyl CoA tetralithium (Malonyl coenzyme A), serves as a substrate in fatty acid biosynthesis and functions as an inhibitor of fatty acid oxidation. Additionally, it acts as a reversible inhibitor of mitochondrial carnitine palmitoyltransferase (CPT) 1 [1] [2].

Sphingosine (d16:1), an unconventional sphingolipid, is synthesized through enzymatic reactions starting with the condensation of myristoyl-CoA and serine by serine palmitoyltransferase long-chain base subunit 3 (SPTLC3), which shows a preference for myristoyl-CoA. This compound is found in minute quantities in its free form in human plasma and as a component of various plasma sphingolipids, such as sphingosine-1-phosphate, ceramides, sphingomyelins, and in brain cerebrosides, albeit at lower concentrations than the more common d18:1 sphingoid base. Sphingosine (d16:1) acts as an inhibitor of PKC in mixed micelle assays and diminishes superoxide production triggered by phorbol 12-myristate 13-acetate in isolated human neutrophils, as well as inhibiting the growth of CHO cells with IC50 values of 1 and 3.2 µM, respectively. Additionally, the concentration of sphingolipids containing sphingosine (d16:1) in the plasma is linked to the dietary consumption of saturated fatty acids and protein among ethnic Chinese populations.

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).

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.

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

Malonyl CoA serves as a substrate in fatty acid biosynthesis while inhibiting fatty acid oxidation. It also acts as a reversible inhibitor of mitochondrial carnitine palmitoyltransferase (CPT) 1 [1] [2].

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).

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(14Z)) is an unconventional sphingolipid featuring a (14Z) double bond at the n-4 position, synthesized when serine palmitoyltransferase combines palmitoyl-CoA with alanine, not serine, during sphingolipid production. Unlike typical sphingolipids, it lacks the essential C1-hydroxyl group for standard degradation but undergoes metabolism by cytochrome P450 (CYP) subfamilies CYP4A and CYP4F in MEF cells.

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.

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].

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.

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.

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.

4-Hydroxyphenylglyoxylic acid, an active metabolite of the prodrug oxfenicine, functions as an inhibitor of carnitine palmitoyltransferase 1 (CPT1). It effectively inhibits CPT1 in isolated rat liver mitochondria at concentrations of 200 to 1,000 µM and restricts oleate oxidation in isolated rat hepatocytes.