NDI-091143

2375840-87-0

453.84

DMSO : 125 mg/mL (275.43 mM; Need ultrasonic)

Metabolic Enzyme/Protease

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 K_i of 7.0 nM and a K_d of 2.2 nM. NDI-091143 inhibits ACLY catalysis allosterically, by stabilizing large conformational changes in the citrate domain that indirectly block the binding and recognition of citrate^[1]. IC50 & Target: IC50: 2.1 nM (human ATP-citrate lyase); Ki: 7.0 nM (human ATP-citrate lyase); Kd: 2.2 nM (human ATP-citrate lyase)^[1] In Vitro: Thermal shift assays shows that NDI-091143 gives rise to considerable stabilization of both full-length ACLY and the N-terminal segment. The thermal shift data are consistent with limited proteolysis experiments using full-length ACLY, in which NDI-091143 together with Mg-ATP provided the greatest protection against digestion by chymotrypsin^[1].