atp citrate lyase

SB 204990 is an effective and specific ATP citrate lyase enzyme inhibitor.

Hydroxycitric acid tripotassium hydrate (Potassium citrate monohydrate) is the major active ingredient of Garcinia cambogia and a derivative of citric acid, which effectively inhibits stone formation and HIF, and has antioxidation, anti-inflammation, and anti-tumor effects. It also competitively inhibits ATP citrate lyase, offering weight loss benefits.

2-Furoic acid (Furan-2-carboxylic acid) reduces serum cholesterol and triglyceride levels and exhibits anti-lipidemic effects.

MEDICA16 is a selective agonist for GPR40 as well as a partial agonist for GPR120. MEDICA16, an ATP-citrate lyase inhibitor, significantly reduces intracellular TG content in gastrocnemius muscle with an increase in insulin sensitivity.

BMS-303141 is a potent ATP-citrate lyase (ACL) inhibitor (IC50: 0.13 uM, human recombinant ACL).

Forrestiacid K, a terpenoid derived from Pseudotsuga forrestii, functions as an inhibitor of ATP-citrate lyase (ACL) [1].

NDI-091143 is a potent, high-affinity human ATP-citrate lyase (ACLY) inhibitor with an IC50 of 2.1 nM (ADP-Glo assay), indirectly disrupting citrate binding via an unexpected mechanism of inhibition.

Bempedoic acid (ETC1002) is an orally available, once-daily LDL-C lowering small molecule designed to lower elevated levels of LDL-C and to avoid side effects associated with existing LDL-C lowering therapies. Bempedoic acid(ETC1002) is absorbed rapidly in the small intestine and enters the liver through cell surface receptors different from those transporters that selectively take up statins. Bempedoic acid(ETC1002) is a regulator of lipid and carbohydrate metabolism.

(-)-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.

(-)-Hydroxycitric acid lactone (Garcinia lactone) is an anti-obesity agent and a potent inhibitor of ATP citrate lyase, an enzyme that catalyzes the extramitochondrial cleavage of citrate to oxaloacetate and acetyl-CoA.

Forrestiacid J is an inhibitor of ATP-citrate lyase (ACL), exhibiting an IC50 value of 2.6 μM [1].

Citric acid trilithium salt tetrahydrate (Lithium citrate tribasic tetrahydrate) , the active component of Lithium, is a medicine used in the therapy of psychiatric disease. It has shown the effects of signaling pathways and metabolic in the brain based on the particular disease and clinical condition model. According to the reports, Citric acid trilithium salt tetrahydrate was used as a mood stabilizer when treating bipolar mood disorders (BD) and lower the risk of self-harm in BD patient. In addition,Citric acid trilithium salt tetrahydrate has been the choice drug in the therapy of acute manic episodes.Citric acid trilithium salt tetrahydrate also could dissolve uric acid crystals in urine achieved from patients with gout. Besides,Citric acid trilithium salt tetrahydrate have some dose-dependent side-effects. The the main side-effects of Lithium Citrate is the tendency to inhibit the prostatic acid phosphatase enzyme (PAP), which result in the accumulation of PAP.

Antimycin A4 is an active component of the antimycin A antibiotic complex that is more polar than antimycin A1 , antimycin A2 , and antimycin A3 . Antimycin A4 inhibits ATP-citrate lyase with a Ki value of 64.8 μM. The antimycin A complex is a mixture of antimycins A1, A2, A3, and A4 that demonstrates antifungal, insecticidal, nematocidal, and piscicidal properties. It blocks mitochondrial respiration and can deplete cellular levels of ATP via inhibition of complex III of the mitochondrial electron transport chain (ETC). Antimycin A prevents the transfer of electrons between the b-cytochromes and ubiquinone at the Q(inner) site of complex III. This results in the stabilization of the ubisemiquinone radical at the Q(outer) site of complex III, leading to increased production of superoxide. Antimycin A is widely used in research to shunt electron flow through the ETC to study the chemical details of oxygen respiration. Additionally, antimycin A has been shown to inhibit Bcl-2 and Bcl-xL proteins, inducing apoptosis.

SB-201076 is a potent ATP citrate-lyase inhibitor. SB-204990 is the prodrug of SB-201076.

Palmitoleic acid, an ω-7 monounsaturated fatty acid found in macadamia and sea buckthorn oils, enhances both basal and insulin-stimulated glucose uptake, as well as Glut4 protein levels in 3T3-L1 adipocytes at a 200 µM concentration. Ex vivo, at a dosage of 300 mg/kg per day, it significantly increases glucose uptake and both aerobic and anaerobic glycolysis, while decreasing de novo fatty acid synthesis and the activity of lipogenic enzymes, specifically ATP citrate lyase (ACL) and glucose-6-phosphate dehydrogenase (G6PDH), in isolated murine adipocytes. Furthermore, the dietary administration of palmitoleic acid at 300 mg/kg mitigates high-fat diet-induced insulin resistance and liver inflammation in mice.

Nicodicosapent is a fatty acid niacin conjugate and an inhibitor of the sterol regulatory element-binding protein (SREBP), which is a key regulator of cholesterol metabolism proteins such as PCSK9, HMG-CoA reductase, ATP citrate lyase, and NPC1L1.

(-)-Hydroxycitric acid (HCA) can inhibit fat synthesis and reduces food intake, the primary mechanism of action of HCA appears to be related to its ability to act as a competitive inhibitor of the enzyme ATP-citrate lyase, which catalyzes the conversion of citrate and coenzyme A to oxaloacetate and acetyl coenzyme A (acetyl-CoA), primary building blocks of fatty acid and cholesterol synthesis.

Gnetuhainin I (Compound 5), a lignin sourced from Pouzolzia zeylanica, exhibits potent inhibition of ATP citrate lyase (ACLY) with an IC50 value of 2.63 μM [1].