palmitoyltransferase

Etomoxir sodium salt ((R)-Etomoxir sodium salt) 是一种肉碱棕榈酰转移酶 1a (CPT-1a) 抑制剂，可以抑制脂肪酸氧化。Etomoxir sodium salt 具有抗肿瘤活性。

McN3716 是一种肉碱棕榈酰转移酶 I (CPT-1) 抑制剂，可用于研究代谢疾病。

Oxfenicine (4-Hydroxy-L-phenylglycine) 是具有口服活性的肉碱棕榈酰转移酶-1 抑制剂。它在缺血期间保护心脏免受坏死组织的损害。它可抑制心脏中脂肪酸的氧化。

CPT2 (Carnitine palmitoyltransferase 2) 是一种脂肪酸氧化过程中的酶，它在结直肠癌 (CRC) 预后评估中作为生物标志物。CPT2 通过过表达激活p-p53并增加p53蛋白水平，这有助于抑制肿瘤生长和促进细胞的凋亡。CPT2 缺乏是长链脂肪酸氧化障碍相关的常见遗传性疾病，并且CPT2 的表达降低与多种癌症的发展密切相关，因此，在癌症研究领域具有研究价值。

Myriocin (Thermozymocidin) 是一种从 Myriococcum albomyces 中得到的代谢产物，是一种丝氨酸-棕榈酰转移酶 (SPT) 抑制剂,具有潜在的抗肿瘤抗癌和抗寄生虫活性，通过 PI3K Akt mTOR 通路调节巨噬细胞极化和功能来抑制肿瘤生长。Myriocin 抑制 HCV 感染，可用于研究神经病变和真菌感染。

Etomoxir是一种不可逆的肉毒碱棕榈酰转移酶1a (CPT-1a) 抑制剂 (IC50=5-20 nM) 。Etomoxir通过抑制 CPT-1a 来抑制脂肪酸氧化，抑制棕榈酸酯的氧化，对腺嘌呤核苷酸转位酶有抑制作用，可通过破坏CoA稳态来抑制巨噬细胞极化。

Lipoxamycin hemisulfate (Lipoxamycin) 是一种丝氨酸棕榈酰转移酶抑制剂 (IC50 = 21 nM)，具有抗真菌活性。

Lipoxamycin HCl 是一种高效的丝氨酸棕榈酰转移酶 (serine palmitoyltransferase) 抑制剂，具有抗真菌活性，抑制丝氨酸棕榈酰转移酶活性。

GSK-7227是一种代表过氧化物酶体增殖物激活受体δ（PPARδ）的新型部分激动剂，通过上调骨骼肌细胞中PPARδ靶基因——特别是肉碱棕榈酰转移酶1a（CPT1a）和丙酮酸脱氢酶激酶4（PDK4）的表达，表现出强效的部分激动活性。GSK-7227在调节骨骼肌代谢与能量稳态方面具有潜在作用。

Teglicar（亦称为ST1326）是一种针对肝脏异构体的肉碱棕榈酰转移酶1（L-CPT1）的选择性可逆抑制剂。它降低了酮体生成和葡萄糖产生，减少了糖异生作用，并改善了葡萄糖稳态。

Cyano-myracrylamide 是一种抑制锌指 DHHC 结构域含量棕榈酰转移酶 20 (zDHHC20) 的化合物，IC50 为 1.35 µM。同时，它还能抑制 EGFR 和 CD36 的 S-酰化。在表达重组大肠杆菌 GobX、重组人 MyD88 或内源性 Ras 的 HEK293T 细胞中，Cyano-myracrylamide 抑制了大肠杆菌 E3 连接酶 GobX、MyD88 和 Ras 的 S-酰化，这些酶是 zDHHC20、zDHHC9 和 zDHHC6 的底物。

ALT-007 为一种口服有效的丝氨酸棕榈酰转移酶 (SPT) 抑制剂，是调控神经酰胺从头合成的关键限速酶。在年龄相关性肌肉减少症的小鼠模型中，该化合物能够有效恢复因年龄增长导致的肌肉质量和功能减退。ALT-007 可在秀丽隐杆线虫及与衰老和年龄相关疾病的小鼠模型中增强蛋白质稳态，展现神经酰胺抑制剂的特性。

9-Oxononanoic Acid是一种氧化脂肪酸，由亚油酸自氧化形成，它能提高磷脂酶 A2（PLA2）的活性，并增加离体人体血浆中血栓素 B2 的生成。9-Oxononanoic Acid 能减少肝脏新脂肪酸的合成，并提高大鼠肝脏肉碱棕榈酰转移酶（β-氧化的标志物）的活性。

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)) 是一种具有 12 个碳原子的鞘氨醇同系物，诱导丝氨酸棕榈酰转移酶活性以时间和浓度依赖性方式降低。

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是Nicotinamide的氘代标记化合物，可用于同位素示踪。Nicotinamide是一种维生素B3的衍生物，是SIRT1和SIRT2的抑制剂。

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.

Malonyl CoA是脂肪酸生物合成的重要底物，同时也担任脂肪酸氧化过程中的抑制剂角色。此外，Malonyl CoA亦作为线粒体肉碱棕榈酰转移酶1（CPT1）的可逆性抑制剂。