| Description | KHK-IN-1 (KHK-IN-8) is a selective and cell membrane permeable inhibitor of ketohexokinase (KHK, IC50=12 nM; F=34%). KHK-IN-1 inhibits F1P production in HepG2 cell lysates with IC50 of 400 nM. KHK-IN-1 has potential for the study of obesity and diabetes. |
| Target activity | KHK:12 nM |
| Synonyms | KHK-IN-8, Ketohexokinase inhibitor 8 |
| molecular weight | 422.55 |
| Molecular formula | C21H26N8S |
| CAS | 1303469-70-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: Insoluble |
| References | 1. Maryanoff BE, et al. Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site. ACS Med Chem Lett. 2011 Apr 18;2(7):538-43. 2. Wu KL, Hung CY, Chan JY, Wu CW. An increase in adenosine-5'-triphosphate (ATP) content in rostral ventrolateral medulla is engaged in the high fructose diet-induced hypertension. J Biomed Sci. 2014 Jan 27;21:8. 3. Maryanoff BE, et al. Pyrimidinopyrimidine inhibitors of ketohexokinase: exploring the ring C2 group that interacts with Asp-27B in the ligand binding pocket. Bioorg Med Chem Lett. 2012 Aug 15;22(16):5326-9. |