NDI-091143 |
| Catalog No.GC38932 |
NDI-091143은 IC50이 2.1nM(ADP-Glo 분석), Ki가 7.0nM, Kd가 2.2nM인 강력하고 친화도가 높은 인간 ATP-시트레이트 리아제(ACLY) 억제제입니다. NDI-091143은 시트레이트의 결합 및 인식을 간접적으로 차단하는 시트레이트 도메인의 큰 형태 변화를 안정화함으로써 ACLY 촉매 작용을 알로스테릭하게 억제합니다.
Products are for research use only. Not for human use. We do not sell to patients.
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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