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.

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.

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.