yGsy2p-IN-1 is a potent inhibitor for yeast glycogen synthase 2 (yGsy2p). yGsy2p-IN-1 is a competitive human glycogen synthase 1 (hGYS1) inhibitor with an IC50 of 2.75 µM and a Ki of 1.31 µM for wild-type hGYS1. yGsy2p-IN-H23 a pyrazole inhibitor, is used for glycogen storage diseases (GSDs)[1].
yGsy2p-IN-1 (compound 23; 0.1, 1, 10, 100, 1000 µM) has IC50s of 7.89 μM and 33.6 μM for yGsy2p-WT and yGsy2p-Y513L[1]. yGsy2p-IN-1 (100 μM) exhibits almost complete inhibition of synthase activity in both HEK293-PTG and Rat-1 cell lysates[1].
[1]. Buyun Tang, et al. Discovery and Development of Small-Molecule Inhibitors of Glycogen Synthase. J Med Chem. 2020 Apr 9;63(7):3538-3551.