产品说明书
NDI-091143
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同义名 : | - |
| CAS号 : | 2375840-87-0 | |
| 货号 : | A1194991 | |
| 分子式 : | C20H14ClF2NO5S | |
| 纯度 : | 99%+ | |
| 分子量 : | 453.844 | |
| MDL号 : | N/A | |
| 存储条件： |
粉末 Keep in dark place,Inert atmosphere,Room temperature 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 105 mg/mL(231.36 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | ATP-citrate lyase (ACLY) connects glucose and lipid metabolism, converting a metabolite derived from glycolysis (citrate) to a substrate (acetyl-CoA) for the biosynthesis of fatty acids and cholesterol. Cancer cells that have high aerobic glycolysis are especially susceptible to ACLY inhibition, and ACLY is overexpressed and correlated with poor prognosis in several types of cancer. NDI-091143 is a potent human ACLY inhibitor[1]. It showed excellent nanomolar potency in the inhibition of human ACLY (IC50 values ranging from 2.1 to 4.8 nM depending on the enzymatic assay employed) and proved to be competitive with the substrate citrate (Ki value of 7.0 nM)[2]. | ||
| 作用机制 | NDI-091143 is located in an allosteric, mostly hydrophobic cavity next to the citrate-binding site, and requires extensive conformational changes in the enzyme that indirectly disrupt citrate binding[1]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.20mL 0.44mL 0.22mL |
11.02mL 2.20mL 1.10mL |
22.03mL 4.41mL 2.20mL |
| 参考文献 |
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[1]An allosteric mechanism for potent inhibition of human ATP-citrate lyase |