khk-a

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

KHK-IN-2 is a selective inhibitor of ketohexokinase with an IC50 value of 0.45 μM.

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-1 hydrochloride is a selective, cell-permeable, and efficient hexokinase (KHK) inhibitor, useful for studying diabetes and obesity.

BI-9787 is a zwitterionic inhibitor of ketohexokinase (KHK), demonstrating IC50 values of 12 nM for hKHK-A and 12.8 nM for hKHK-C. It exhibits good metabolic stability in rat hepatocytes and favorable pharmacokinetic properties in vivo in rats.

KHK-IN-5 (Compound 18), a KHK inhibitor, is employed in the study of nonalcoholic fatty liver disease (NAFLD), nonalcoholic steatohepatitis (NASH), and type 2 diabetes (T2DM).

KHK-IN-6 (compound 33) acts as a KHK inhibitor with an IC50 of 0.6nM.

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].

KHK-2898 represents a highly specialized humanized monoclonal antibody specifically engineered to target the CD98 heavy chain (CD98hc/SLC3A2) with exceptional binding affinity to the human and monkey LAT1/CD98hc complex. It effectively facilitates the measurable blockade of amino acid transport and the induction of potent antibody-dependent cellular cytotoxicity (ADCC) across various preclinical experimental models to evaluate the disruption of tumor nutrient uptake and metabolic homeostasis during strictly monitored laboratory observation periods and functional cell viability assays.

KHK-2866 is a humanized monoclonal antibody targeting Heparin-Binding Epidermal Growth Factor-like Growth Factor (HB-EGF). By binding to HB-EGF, KHK-2866 blocks its interaction with EGFR and HER4 receptors, thereby inhibiting the proliferation and survival of tumor cells. HB-EGF is frequently overexpressed in various solid tumors, making it a key therapeutic target.