NG 52

NG 52 is a potent, cell-permeable, selective, ATP-compatible and orally active Cdc28p and Pho85p kinase inhibitor with IC₅₀s of 7 μM and 2 μM, respectively. NG 52 also inhibits the activity of phosphoglycerate kinase 1 (PGK1) with an IC₅₀ of 2.5 μM. NG 52 is inactive against yeast kinases Kin28p, Srb10, and Cak1p^[1][2]. In Vitro: NG 52 (Compound 52) inhibits growth in a drug-sensitized yeast strain (S. cerevisiae) with a GI₅₀ of 30 μM. NG 52 is active against cdc2-cyclin B with an IC₅₀ value of 340 nM^[1].
NG 52 dose-dependently inhibits the proliferation of glioma U87 and U251 cell lines with GI₅₀ values of 7.8 μM and 5.2 μM, respectively, meanwhile it potently inhibits the proliferation of primary glioma cells^[2].
NG 52 (12.5-50 μM) effectively inhibits the phosphorylation of PDHK1 at Thr338 site and the phosphorylation of PDH at Ser293 site in U87 and U251 cells, resulting in more pyruvic acid entering the Krebs cycle with increased production of ATP and ROS^[2].
NG 52 can reverse the Warburg effect by enhancing the activity of pyruvate dehydrogenase (PDH) through inhibiting the activity of PGK1, and switched cellular glucose metabolism from anaerobic mode to aerobic mode^[2]. In Vivo: NG 52 (50-150 mg/kg; oral administration; daily; for 13 days) treatment dose-dependently suppresses the growth of glioma xenograft^[2].