iGP-1 is a cell-permeable, selective mixed inhibitor of mitochondrial sn-glycerol-3-phosphate dehydrogenase ( mGPDH ), with IC 50 s of 6.3 μM and 13.6 μM for rat mGPDH activity and H 2 O 2 production, respectively. iGP-1 specifically blocks the mitochondrial component of the glycerophosphate shuttle without affecting cytosolic GPDH. iGP-1 not only inhibits cell proliferation and glutaminolysis, and enhances glycolysis , but also significantly alters key cellular physiological processes such as apoptosis , ROS production, HIF-1α stability and mitochondrial membrane potential. iGP-1 remains active in neutrophil cultures under both normoxic and hypoxic conditions, and serves as an ideal probe for glycerol-3-phosphate metabolic mechanisms. iGP-1 has been applied to studies on prostate cancer and related metabolic pathways.
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