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CAS No.: 2375840-87-0

NDI-091143 Catalog No. CSN24799

NDI-091143 is a small-molecule inhibitor of human ACLY. It 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.

规格	价格	促销价格	库存	数量

400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

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 (K_i 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].
参考文献

[1] An allosteric mechanism for potent inhibition of human ATP-citrate lyase
[2] Granchi C. Discovery of Allosteric Inhibition of Human ATP-Citrate Lyase. Trends Pharmacol Sci. 2019;40(6):364-366.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2034 mL
- 11.0170 mL
- 22.0340 mL
- 5 mM
- 0.4407 mL
- 2.2034 mL
- 4.4068 mL
- 10 mM
- 0.2203 mL
- 1.1017 mL
- 2.2034 mL

技术信息

CAS号

2375840-87-0

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H14ClF2NO5S

运输

蓝冰

分子量

453.84

别名

溶解度

DMSO	100.0 mg/mL (220.3 mM)
Water	insoluble

动物实验配方

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