G6PD activator AG1

G6PD activator AG1 is a potent and selective glucose-6-phosphate dehydrogenase (G6PD) activator with an EC₅₀ of 3 μΜ^[1]. G6PD activator AG1 reduces hemolysis of human erythrocytes^[2]. IC50 & Target:IC50: 3 μΜ (G6PD)^[1] In Vitro:AG1 (50, 100, 250, 500, 750, 1000 nM) of 1 μM increases the viability by 20% and the proteolytic stability of Canton G6PD in SH-SY5Y cells. AG1 has no effect when G6PD was knocked down by siRNA, supporting the specificity of AG1 toward G6PD^[2].
AG1 (1-5 μΜ; pre-incubated overnight) reduces the extent of hemolysis with 5 μΜ in human erythrocytes suspension (5%) exposed to either 1 mM chloroquine (CQ; 4 hours) or diamide (a GSH oxidant; 4 hours). AG1 increases GSH levels and reduced ROS levels together with increased G6PD activity under these drug-induced oxidative stress^[2].
AG1 has no effect on the dimerization or activity of several other NAD- or NADP+-dependent dimeric or tetrameric enzymes, including 6-phosphogluconate dehydrogenase (6PGD), glyceraldehyde 3-phosphate dehydrogenase (GAPDH), aldehyde dehydrogenase 2 (ALDH2), and aldehyde dehydrogenase 3A1 (ALDH3A1)^[2].