G6PD Activator AG1

G6PD activator AG1 is an activator of glucose-6-phosphate dehydrogenase (G6PDH; EC₅₀ = 3.4 µM for G6PDH^R459L).¹ It selectively induces the dimerization of G6PDH^R459L over 6-phosphogluconate dehydrogenase (6PGD), GAPDH, aldehyde dehydrogenase 2 (ALDH2), and ALDH3A1. G6PD activator AG1 decreases the levels of reactive oxygen species (ROS) in, and increases the viability of, primary human lymphocytes isolated from a patient carrying the G6PDH^R459L mutation. It inhibits hemolysis induced by chloroquine (Item No. 14194) or diamide in isolated human erythrocytes when used at a concentration of 5 µM. G6PD activator AG1 (1 µM) decreases chloroquine-induced pericardial edema in zebrafish embryos. It decreases tumor volume and weight and increases survival in an NCI H226 lung mesothelioma mouse xenograft model when administered at a dose of 40 mg/kg.²

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1. Hwang, S., Mruk, K., Rahighi, S., et al. Correcting glucose-6-phosphate dehydrogenase deficiency with a small-molecule activator. Nat. Commun. 9(1), 4045 (2018).

2. Lu, C., Yang, D., Klement, J.D., et al. H3K9me3 represses G6PD expression to suppress the pentose phosphate pathway and ROS production to promote human mesothelioma growth. Oncogene 41(18), 2651-2662 (2022).