lipogenesis

MT 63-78 is a specific and effective direct AMPK activator (EC50: 25 μM) that blocks prostate cancer growth by inhibiting the lipogenesis and mTORC1 pathways. It has antitumor effects and induces cell mitotic arrest and apoptosis.

INT-767 is a potent farnesoid X receptor (FXR) TGR5 dual agonist that prevents NASH and promotes visceral adipose brown lipogenesis and mitochondrial function for the study of non-alcoholic steatohepatitis.

L-(+)-Arabinose selectively inhibits intestinal sucrase in a non-competitive manner, thereby preventing glucose elevation induced by sucrose intake.

(-)-Hydroxycitric acid (Garcinia acid) is the principal acid found in the fruit rinds of Garcinia cambogia. It acts as a potent and competitive inhibitor of ATP citrate lyase, suppressing fatty acid synthesis, food intake, lipogenesis, and inducing weight loss.

SR9243, an LXR inverse agonist, can induce LXR-corepressor interaction; shows anticancer activity and selectively targets the lipogenesis and Warburg effect.

HDAC11-IN-2 (compound B6) is a highly selective inhibitor of Histone Deacetylase 11 (HDAC11). It demonstrates IC50 values of 51.1 ×10^-3 μM for HDAC11 and 5 μM for HDAC8. HDAC11-IN-2 reduces de novo lipogenesis (DNL) and enhances fatty acid oxidation, which alleviates hepatic lipid accumulation and pathological symptoms in MASLD mice. By inhibiting HDAC11, HDAC11-IN-2 enhances the phosphorylation of AMPKα1 at the Thr172 site, thereby modulating de novo lipogenesis and fatty acid oxidation in the liver.

AMPK activator17 (Compound 10g) is an orally bioavailable AMPK activator. It significantly inhibits lipogenesis (IC50: 3.4 μM) and improves dyslipidemia. By activating the AMPK pathway, AMPK activator17 suppresses early adipocyte differentiation (mitotic clonal expansion) and enhances mitochondrial function and fatty acid oxidation in mature adipocytes. It improves dyslipidemia through promoting cholesterol reverse transport. AMPK activator17 is applicable in research on obesity and associated metabolic disorders, such as type 2 diabetes and cardiovascular diseases.

Pinolenic Acid (PNLA) is an omega-6 polyunsaturated fatty acid extracted from pine nuts, with anti-inflammatory, anticancer, and lipid-lowering activities, improving oleic acid-induced lipogenesis and oxidative stress in HepG2 cells, useful in breast cancer research.

Neomangiferin (Mangiferin 7-glucoside) has beneficial effects on high fat diet-induced nonalcoholic fatty liver disease in rats. Neomangiferin and mangiferin inhibit tartrate-resistant acid phosphatase, a biochemical marker of osteoclast function and bone resorption.

CTL-06, a Fatty Acid Synthase (FASN) inhibitor with an IC50 of 3 μM, induces apoptosis, while CTL-12 impedes cell cycle progression in the Sub-G1 S phase and modulates apoptotic and anti-apoptotic markers by upregulating caspase-9 and Bax and downregulating Bcl-xL. Additionally, CTL-12 suppresses de novo lipogenesis, curtailing the metabolic needs of tumor cells, with utilization in breast and colorectal cancer studies [1].

CTL-12, a fatty acid synthase (FASN) inhibitor (IC50: 2.5 μM), induces apoptosis and disrupts the cell cycle at the Sub-G1 S phase. It upregulates caspase-9 and the apoptosis marker Bax, while downregulating the anti-apoptotic marker Bcl-xL. By inhibiting de novo lipogenesis, CTL-12 thwarts tumor cells' metabolic requirements and is frequently employed in breast and colorectal cancer studies [1].

Haloxyfop-P-methyl, an aryloxyphenoxypropionate herbicide, is absorbed through both foliage and roots, where it inhibits lipogenesis and induces oxidative stress in susceptible plant species [1].

KHK-IN-3 (Example 1), a ketohexokinase (KHK) inhibitor, plays a crucial role in the study of various diseases including kidney disease, nonalcoholic steatohepatitis (NASH), diabetes, and heart failure. KHK, a pivotal rate-limiting enzyme and fructokinase, facilitates the metabolism of fructose by catalyzing the transformation of fructose into fructose-1-phosphate (FIP) utilizing ATP. This process lacks feedback inhibition, leading to the buildup of metabolites involved in lipogenesis, gluconeogenesis, and oxidative phosphorylation [1].

NNMTi (5-Amino-1-methylquinolinium) is a substrate site-targeting, selective nicotinamide N-methyltransferase (NNMT) inhibitor (IC50 = 1.2 μM; 50 μM SAM, 100 μM NCA) that reduces 3T3-L1 lipogenesis (EC50 = 30μM) and adipocytes 1-methylnicotinamide level (EC50 = 2.3 μM) without affecting related methyltransferases & enzymes in the NAD+ salvage pathway

Erycibelline has antiobesity activity, it may be a useful therapeutic agent for body weight control by downregulating adipogenesis and lipogenesis.

Neobyakangelicol has anti-lipolytic hormones effects, it can strongly inhibit insulin- stimulated lipogenesis.

Tachioside has antiobesity, antioxidant and α-glucosidase inhibitory activities, it decreases lipid content in 3T3-L1 adipocytes by inhibiting lipogenesis, shows antiobesity activities. Tachioside can inhibit nitric oxide production in lipopolysaccharides-stimulated RAW 264.7 cells with IC50 value of 12.14 μM.