fih

1,4-DPCA is an inhibitor of prolyl-hydroxylase with an IC50 of 2.4 µM for collagen hydroxylation in human foreskin fibroblasts and 60 μM for factor inhibiting HIF (FIH).

IOX2 (IOX 2) is a selective inhibitor of the Hypoxia Inducible Factor (HIF) Prolyl-Hydroxylases (PHD); active in cells with the IC50 value of 21 nM for PHD2/ELGN-1 and no inhibition at FIH (20uM).

ZG-2305 is an effective, selective, and orally active inhibitor of FIH (factor inhibiting hypoxia-inducible factor (FIH)), with Ki values of 79.6 nM for FIH and 2786 nM for PHD2. This compound enhances the expression of the EGLN3 gene, reduces cellular triglyceride levels, and decreases lipid accumulation. ZG-2305 holds potential for research into obesity and fatty liver disease.

Vadadustat is a novel, titratable, oral hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor in development for the treatment of anemia.

DM-NOFD is a cell penetrant prodrug of NOFD, which is a potent and selective inhibitor of an asparaginyl hydroxylase FIH (factor-inhibiting HIF).

ZG-2291 is a selective inhibitor targeting FIH (hypoxia-inducible factor inhibitor) with oral activity. It selectively inhibits FIH by binding to it and inducing a conformational flip in a catalytically crucial tyrosine, without affecting other 2OG oxidases of the JmjC subfamily. ZG-2291 promotes thermogenesis and ameliorates obesity symptoms and metabolic dysfunctions in ob/ob mice. This compound holds promise for research in the field of obesity-related diseases.