NDI-091143
目录号: PL02884 纯度: ≥99%
CAS No. :2375840-87-0
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中文名称
NDI-091143
英文名称
NDI-091143
英文别名
methyl 3-chloro-5-[(4,6-difluoro[1,1'-biphenyl]-3-yl)sulfamoyl]-4-hydroxybenzoate;s8878;Methyl 3-chloro-5-(N-(4,6-difluoro-[1,1'-biphenyl]-3-yl)sulfamoyl)-4-hydroxybenzoate;LBG;Methyl 3-chloro-5-[(2,4-difluoro-5-phenylphenyl)sulfamoyl]-4-hydroxybenzoate;NDI-091143
Cas No.
2375840-87-0
分子式
C20H14ClF2NO5S
分子量
453.84
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
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。
生物活性
NDI-091143 is a potent and high-affinity human ATP-citrate lyase (ACLY) inhibitor with an IC 50 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.
性状
Solid
IC50 & Target[1][2]
IC50: 2.1 nM (human ATP-citrate lyase); Ki: 7.0 nM (human ATP-citrate lyase); Kd: 2.2 nM (human ATP-citrate lyase)
体外研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Wei J, et al. An allosteric mechanism for potent inhibition of human ATP-citrate lyase. Nature. 2019 Apr;568(7753):566-570.
溶解度数据
In Vitro: DMSO : 100 mg/mL (220.34 mM; ultrasonic and warming and heat to 60°C)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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