G6PDi-1 is a non-steroidal, potent cell active small molecule inhibitor of glucose-6-phosphate dehydrogenase (G6PD) with IC50 of 70 nM (hG6PD).
G6PDi-1 binds to G6PD reversibly and non-competitively, binds to G6PD at an allosteric site and inhibits enzyme catalytic activity.
G6PDi-1 dose-dependently decreases 6-PG levels in HepG2 cells with IC50 of 13 uM, decreases 2H transfer from [1-2H]-glucose to NADPH's active hydride in treated HCT116 cells (IC50=31 uM).
G6PDi-1 dose-dependently increases NADP+/NADPH ratio in T cells, suppresses T cell cytokine production while having a minimal effect on initial activation or proliferation, suppresses oxidative burst in bone marrow derived macrophages.
