ketohexokinase inhibitor 1

Ketohexokinase inhibitor 1 is a ketohexokinase inhibitor (IC50s: 8.4 nM and 66 nM for KHK-C and KHK-A, respectively).

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.

KHK-IN-4 (compound 14) is a potent inhibitor of ketohexokinase (KHK), suitable for researching fructose metabolism diseases [1].

KHK-IN-3 (Example 1), a ketohexokinase (KHK) inhibitor, plays a crucial role in the study of various diseases including kidney disease, nonalcoholic steatohepatitis (NASH), diabetes, and heart failure. KHK, a pivotal rate-limiting enzyme and fructokinase, facilitates the metabolism of fructose by catalyzing the transformation of fructose into fructose-1-phosphate (FIP) utilizing ATP. This process lacks feedback inhibition, leading to the buildup of metabolites involved in lipogenesis, gluconeogenesis, and oxidative phosphorylation [1].