Métabolisme

IDO1-IN-22 (Compound 3) is an inhibitor of IDO1, demonstrating potent activity with biochemical hIDO1 IC50 of 67.4 nM and HeLa hIDO1 IC50 of 17.6 nM.

SH1573 is an orally active inhibitor of mutant isocitrate dehydrogenase 2 (mIDH2). It selectively targets the mIDH2 R140Q protein with a potent inhibitory effect (IC50=4.78 nmol/L), significantly reducing the production of the oncogenic metabolite 2-hydroxyglutarate (2-HG) in animal models, cell lines, serum, and tumors. SH1573 is utilized in the study of acute myeloid leukemia (AML).

CC15009 is a potent inhibitor of xanthine oxidoreductase (XOR), demonstrating an IC50 value of 0.237 nM. It effectively inhibits the oxidative subtype of XOR, thereby reducing the generation of the byproduct ROS and exhibiting antioxidant activity. CC15009 has shown a favorable dose-dependent uric acid-lowering effect in two different XOR substrate-induced hyperuricemia mouse models.