NDI-091143 |
| Katalog-Nr.GC38932 |
NDI-091143 ist ein potenter und hochaffiner Inhibitor der humanen ATP-Citrat-Lyase (ACLY) mit einem IC50-Wert von 2,1 nM (ADP-Glo-Test), einem Ki-Wert von 7,0 nM und einem Kd-Wert von 2,2 nM. NDI-091143 hemmt die ACLY-Katalyse allosterisch, indem es große KonformationsÄnderungen in der CitratdomÄne stabilisiert, die indirekt die Bindung und Erkennung von Citrat blockieren.
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Cas No.: 2375840-87-0
Sample solution is provided at 25 µL, 10mM.
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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. 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].
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].
[1]. Wei J, et al. An allosteric mechanism for potent inhibition of human ATP-citrate lyase. Nature. 2019 Apr;568(7753):566-570.
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