Abstract: Aspects of the present disclosure include G6PD-modulating agents and methods for modulating a glucose-6-phosphate dehydrogenase (G6PD) in a sample using such agents. A G6PD-modulating agent can be dimeric and include two terminal carbocyclic or heterocyclic groups connected via a linker. In some instances, the agent includes a diamino-containing linker. In certain cases, the agent includes two amino substituents. Also provided are methods for treating a subject for a G6PD deficiency-associated condition, that include administering to a subject an effective amount of a G6PD-modulating agent to selectively activate a mutant G6PD and treat the subject. Kits and compositions for practicing the subject methods are also provided.