Ketohexokinase inhibitor 1
Ketohexokinaseinhibitor1是一种己酮糖激酶(ketohexokinase(KHK))抑制剂，对KHK-C和KHK-A的IC50值分别为8.4nM和66nM，摘自专利US20170183328A1，example4。
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包装价格促销价数量
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5mg￥6950.005560.00- +
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10mg￥12712.0010170.00- +
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25mg￥27550.0022040.00- +
- 货号: ajce47042
- CAS: 2102501-84-6
- 别名:
- 分子式: C16H19F3N4O2
- 分子量: 356.34
- 纯度: ＞98%
- 溶解度: DMS : ≥ 125 mg/mL (350.79 mM)
- 储存: Store at -20°C
- 库存: 现货
Background
Ketohexokinase inhibitor 1 is an inhibitor of ketohexokinase (KHK), with IC50s of 8.4 nM and 66 nM for KHK-C and KHK-A, respectively, extracted from patent US 20170183328 A1, example 4.
Ketohexokinase inhibitor 1 (Example 4) is an inhibitor of ketohexokinase (KHK), with IC50s of 8.4 nM and 66 nM for KHK-C and KHK-A, sepctively[1].
[1]. SUBSTITUTED 3-AZABICYCLO[3.1.0]HEXANES AS KETOHEXOKINASE INHIBITORS. US 20170183328 A1
Protocol
Kinase experiment: | A 384-well format on a assay plate is used in the assay and monitored by UV-vis spectroscopy in continuous mode at room temperature (rt). Compounds (Ketohexokinase inhibitor 1) are prepared in DMSO as 4 mM stocks, diluted using an 11-point half-log scheme on a Biomek FX, and incubated at rt for 30 minutes with the reaction mixture containing 50 mM HEPES, pH 7.4, 140 mM KCl, 3.5 mM MgCl2, 0.8 mM fructose, 2 mM TCEP, 0.8 mM PEP, 0.7 mM NADH, 0.01% Triton X-100, 30 U/mL pyruvate kinase-lactate dehydrogenase, and 10 nM purified KHK-C. The compound concentration in each well ranged from 1 nM to 100 μM. The reaction is initiated with the addition of 0.2 mM ATP. The absorbance is measured for 30 minutes on a SpectraMax reader after ATP is added. The concentrations provided are based on the final mixture volume of 40 μL[1]. |
参考文献: [1]. SUBSTITUTED 3-AZABICYCLO[3.1.0]HEXANES AS KETOHEXOKINASE INHIBITORS. US 20170183328 A1 | |
