PGMI-004A is a specific small molecule inhibitor of glycolytic enzyme phosphoglycerate mutase 1 (PGAM1) with IC50 of 13.1 uM, Ki of 3.91 uM.
PGMI-004A directly binds to the protein with KD of 9.4 uM.
PGMI-004A treatment results in decreased 2-PG and increased 3-PG levels in H1299 cells, which could be rescued by treatment with methyl-2-PG.
PGMI-004A treatment results in decreased oxidative PPP flux and NADPH/NADP+ ratio as well as reduced biosynthesis of lipids and RNA and cell proliferation in H1299 cells.
PGMI-004A treatment inhibits cancer cell proliferation and tumor growth, and alters 3-PG and 2-PG levels in primary leukemia cells from human patients, leading to attenuated leukemia cell proliferation.
