DC-5163

DC-5163 is a potent glyceraldehyde-3-phosphate dehydrogenase (GAPDH) inhibitor with an IC50 of 176.3 nM and a Kd of 3.192 μM. DC-5163 can inhibit glycolysis pathway partially. DC-5163 also selectively inhibits cancer cell proliferation and induces apoptosis[1].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

IC50: 176.3 nM (Glyceraldehyde-3-phosphate dehydrogenase (GAPDH))[1] Kd: 3.192 μM (GAPDH)[1]

DC-5163 (100 μM; 48 hours; MDA-MB-231 cells) treatment clearly induces the apoptosis of MDA-MB-231 cells. DC-5163 also significantly reduces glucose uptake, lactate production, and 18F-FDG uptake rate compared to controls in MDA-MB-231cells[1]. DC-5163 treatment at 25 μM inhibits GAPDH activity in BT-549 cells, MCF7 cells, HCT116 cells, MDA-MB-231 cells and A549 cells after 48 hours[1]. DC-5163 inhibits MDA-MB-231 cell proliferation with an IC50 of 99.22 μM at 48 hours and 52.09 μM at 72 hours[1]. Apoptosis Analysis[1] Cell Line: MDA-MB-231 cells Concentration: 100 μM Incubation Time: 48 hours Result: Clearly induced the apoptosis of MDA-MB-231 cells.

[1]. Li T, et al. Discovery of novel glyceraldehyde-3-phosphate dehydrogenase inhibitor via docking-based virtual screening. Bioorg Chem. 2020 Mar;96:103620.