| 规格 | 价格 | 库存 | 数量 | 操作 |
|---|---|---|---|---|
| 1mg | ¥1,350.00 | 现货 | 1 | |
| 5mg | ¥4,050.00 | 现货 | 1 | |
| 10mM (in 1mL DMSO) | ¥4,455.00 | 现货 | 1 |
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
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]. |
References: [1]. SUBSTITUTED 3-AZABICYCLO[3.1.0]HEXANES AS KETOHEXOKINASE INHIBITORS. US 20170183328 A1 |
