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Adenosine triphosphate-citrate lyase (ACLY) links cellular carbon metabolism with lipid synthesis. The enzyme supplies cytosolic acetyl groups that contribute to biosynthesis and protein acetylation, connecting nutrient metabolism with gene regulation. This category includes BMS303141, SB 204990 and NDI-091143, each annotated as an ACLY inhibitor. These compounds represent different chemical approaches to studying the same enzyme. The selection is relevant to investigations of metabolic flux, lipid-associated pathways and the relationship between intermediary metabolism and chromatin regulation.
BMS303141 is a potent inhibitor of ATP citrate lyase (ACL). BMS303141 inhibits lipid synthesis in HepG2 cells with an IC50 of 8 μM, and lowers plasma triglycerides in a murine hyperlipdemia model.
Synonyms: ESP-55016
ETC-1002 is a novel, first-in-class, orally available, once-daily LDL-C lowering small molecule; activator of hepatic AMP-activated protein kinase (AMPK); also has potent inhibitory activity against hepatic ATP-citrate lyase(IC50=29 uM).
SB 204990 is a potent and specific inhibitor of ATP citrate lyase (ACLY) enzyme.
NDI-091143 is a potent and high-affinity human ATP-citrate lyase (ACLY) inhibitor with an IC50 of 2.1 nM (ADP-Glo assay), a Ki of 7.0 nM and a Kd of 2.2 nM.
EVT0185 is an orally active inhibitor of ATP citrate lyase (ACLY). Through conversion to a CoA thioester by SLC27A2 in the liver, EVT0185 exhibits its inhibitory effects by binding to the CoA-binding site of ACLY, achieving an IC50 of 2.5 μM. This compound mimics the immune and antitumor effects associated with genetic ACLY deletion, enhancing tumor-infiltrating B cells and increasing levels of chemokine CXCL13. EVT0185 is relevant for research into various cancers, particularly hepatocellular carcinoma (HCC).
ACLY-IN-1 is a potent inhibitor of ATP citrate lyase (ACLY), with an IC50 of 8.3 nM and a binding affinity (KD) of 72.0 nM. This compound exhibits favorable pharmacokinetic properties and shows significant hypolipidemic effects in vivo. ACLY-IN-1 serves as a valuable tool for research focused on metabolic disorders and lipid metabolism.
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