PF-06835919 | Ketohexokinase inhibitor

PF-06835919 chemical structure

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PF-06835919 (2102501-84-6) is a potent (IC50 = 10 nM KHK-C; 170 nM KHK-A) inhibitor of ketohexokinase (KHK), the first enzyme in the fructose metabolic cascade.1 It displayed high selectivity against other sugar kinases. PF-06835919 prevented hyperinsulinemia, hypertriglyceridemia, and hepatic steatosis in fructose-fed rats.2 The increased tumor proliferation effect of fructose in CaSki cells was inhibited by PF-06835919.3 An interesting new tool to study metabolic and fatty liver diseases.

References/Citations:

  1. Futatsugi et al. (2020), Discovery of PF-06835919: A Potent Inhibitor of Ketohexokinase (KHK) for the Treatment of Metabolic Disorders Driven by the Overconsumption of Fructose; J. Med. Chem. 63 13546
  2. Gutierrez et al. (2021), Pharmacologic inhibition of ketohexokinase prevents fructose-induced metabolic dysfunction; Mol. Metab. 48 101196
  3. Fowle-Girder et al. (2024), Dietary fructose enhances tumour growth indirectly via interorgan lipid transfer; Nature 636 737
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Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

PF-06835919 (2102501-84-6) is a potent (IC50 = 10 nM KHK-C; 170 nM KHK-A) inhibitor of ketohexokinase (KHK), the first enzyme in the fructose metabolic cascade.1 It displayed high selectivity against other sugar kinases. PF-06835919 prevented hyperinsulinemia, hypertriglyceridemia, and hepatic steatosis in fructose-fed rats.2 The increased tumor proliferation effect of fructose in CaSki cells was inhibited by PF-06835919.3 An interesting new tool to study metabolic and fatty liver diseases.

References/Citations:

  1. Futatsugi et al. (2020), Discovery of PF-06835919: A Potent Inhibitor of Ketohexokinase (KHK) for the Treatment of Metabolic Disorders Driven by the Overconsumption of Fructose; J. Med. Chem. 63 13546
  2. Gutierrez et al. (2021), Pharmacologic inhibition of ketohexokinase prevents fructose-induced metabolic dysfunction; Mol. Metab. 48 101196
  3. Fowle-Girder et al. (2024), Dietary fructose enhances tumour growth indirectly via interorgan lipid transfer; Nature 636 737