2102501-84-6
2102501-84-6 structure
- Name: Ketohexokinase inhibitor 1
- Chemical Name: Ketohexokinase inhibitor 1
- CAS Number: 2102501-84-6
- Molecular Formula: C16H19F3N4O2
- Molecular Weight: 356.34
- Catalog: Research Areas Metabolic Disease
- Create Date: 2018-05-09 07:03:00
- Modify Date: 2025-08-25 11:11:42
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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.
| Name | Ketohexokinase inhibitor 1 |
|---|
| Description | 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. |
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| Related Catalog | |
| Target |
IC50: 8.4 nM (KHK-C), 66 nM (KHK-A)[1] |
| In Vitro | 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]. |
| Kinase Assay | 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 |
| Molecular Formula | C16H19F3N4O2 |
|---|---|
| Molecular Weight | 356.34 |