产品
编 号:F287227
分子式:C20H14ClF2NO5S
分子量:453.84
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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100mg
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生物活性:
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.

体外研究:
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.
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