DC-5163 is a potent inhibitor of glyceraldehyde 3-phosphate dehydrogenase (GAPDH) with IC50 of 176.3 nM and Kd of 3.192 μM. DC-5163 selectively inhibits cancer cell proliferation and induces apoptosis, and partially inhibits the glycolysis pathway.

GAPDH:176.3 nM , GAPDH:(kd)3.192 μM

DC-5163 (100 μM; 48 hours; MDA-MB-231 cells) treatment can obviously induce apoptosis of MDA-MB-231 cells. DC-5163 inhibited the proliferation of MDA-MB-231 cells with an IC50 of 49.22 μM at 48 hours and 52.09 μM at 72 hours. Compared with the experimental control, DC-5163 also significantly reduced glucose uptake, lactic acid production and 18F-FDG uptake rate. After treatment with 25μM DC-5163 for 48 hours, it can inhibit the GAPDH activity of BT-549 cells, MCF7 cells, HCT116 cells, MDA-MB-231 cells and A549 cells.