KHK-IN-1 

KHK-IN-1 (compound 8) is a selective and cell membrane permeable ketohexokinase (KHK) inhibitor (IC₅₀=12 nM; F=34%). KHK-IN-1 inhibits the production of F1P in HepG2 cell lysates (IC>sub>50=400 nM). KHK-IN-1 has potential for the study of diabetes and obesity^[1].

IC50=12 nM (KHK)^[1].

KHK-IN-1 stable in human and rat liver microsome preparations (88 and 72% remaining at 10 min) and do not significantly inhibit cytochrome P450s from human liver microsomes (1A2, 2C19, 2D6, 2C9, and 3A4)^[1].
KHK-IN-1 (0-10 µM; incubate 30 min, then add to 15 mM fructose and incubate for another 3 h) inhibits production of F1P in HepG2 cell lysates with an IC₅₀ value of 400 nM^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

KHK-IN-1 (10 mg/kg; p.o.; single) shows oral bioavailability of 34% in rats^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

422.55

C₂₁H₂₆N₈S

1303469-70-6

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]