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NDI-091143
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
NDI-091143图片
CAS NO:2375840-87-0
包装与价格：
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
NDI-091143 是一种有效的高亲和力人 ATP 柠檬酸裂解酶 (ACLY) 抑制剂，IC50 为 2.1 nM (ADP-Glo分析)，Ki 为 7.0 nM，Kd 为 2.2 nM。NDI-091143 通过稳定柠檬酸盐域中的大构象变化来间接抑制柠檬酸的结合和识别，从而抑制了 ACLY 催化变构反应。
Cas No.2375840-87-0
Canonical SMILESO=C(OC)C1=CC(S(=O)(NC2=CC(C3=CC=CC=C3)=C(F)C=C2F)=O)=C(O)C(Cl)=C1
分子式C20H14ClF2NO5S
分子量453.84
溶解度DMSO: 125 mg/mL (275.43 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.