yGsy2p-IN-H23是一种有效的酵母糖原合酶2(yGsy2p)抑制剂，对人糖原合酶1(hGYS1)的IC50为875µM。yGsy2p-IN-H23结合在yGsy2p的尿苷二磷酸葡萄糖结合口袋内。yGsy2p-IN-H23用于糖原储存疾病(GSDs)的相关研究。
yGsy2p-IN-H23 is a potent and first-in-class inhibitor for yeast glycogen synthase 2 (yGsy2p) with an IC50 of 875 µM for human glycogen synthase 1 (hGYS1). yGsy2p-IN-H23 bounds within the uridine diphosphate glucose binding pocket of yGsy2p. yGsy2p-IN-H23 is used for the research of glycogen storage diseases (GSDs)[1].
yGsy2p-IN-H23 (compound H23) has IC50 values against either hGYS1δ634S8,11N or wild-type hGYS1 were 161 μM and 875 µM, respectively. yGsy2p-IN-H23 exhibits IC50 values of 280 µM and 263 µM in the absence and presence of G6P for yGsy2p against yeast and human glycogen synthase (GS), respectively. yGsy2p-IN-H23 is not in direct competition with G6P[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.
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