3PO inhibits recombinant PFKFB3 activity with IC50 of 25 μM, suppresses glucose uptake, and decreases the intracellular concentration of Fru-2,6-BP, lactate, ATP, NAD+, and NADH in vitro.

PFK-158 is a potent and selective inhibitor of PFKFB3 that is currently being investigated in a phase I study in patients with advanced solid malignancies.

YZ9 is a PFKFB3 inhibitor with IC50 of 0.183 μM, also inhibits F-6-P with Ki of 0.094 μM.

PFK-015 is an effective inhibitor of PFKFB3 with IC50 of 110 nM (recombinant PFKFB3) and inhibits PFKFB3 activity in cancer cells with IC50 of 20 nM.

AZ PFKFB3 26 is a potent and selective PFKFB3 inhibitor with IC50 of 0.023 μM.

AZ PFKFB3 67 is a potent and selective PFKFB3 inhibitor with IC50 of 11 nM.