PFKFB3 Inhibitor II, PFK15

A cell-permeable, bioavailable and more potent quinolinyl analog of PFKFB3 Inhibitor, 3PO (Cat. No. 525330) that inhibits the activity of 6-Phosphofructo-2-kinase (PFKFB3) by reversibly docking to its substrate binding domain (IC50 = 207 nM compared to 22.9 µM for 3PO). Shown to effectively reduce fructose 2,6-bisphosphate, glucose uptake, and intracellular ATP levels. Does neither affect the activity of 96 other kinases in any significant manner (at ~10 µM) nor PFK-1, hexokinase, phosphoglucoisomerase, or PFKFB4 even at 100 µM. Induces apoptosis and reduces proliferation in transformed cells (mean GI50 of ~3 µM in the NCI-60 cancer cell panel). Displays adequate pharmacokinetic properties to suppress glucose uptake and the growth of Lewis lung carcinoma is syngenic mice and block the growth of human tumor xenografts in athymic mice (~25 mg/kg, i.p. administered every 3rd day).

Cell permeable: yes

Primary Target
PFKFB3

Reversible: yes

Target IC₅₀: 207 nM for hrPFKFP3

Packaged under inert gas

Following reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 6 months at -70°C.

Use only fresh DMSO for reconstitution.

Clem, B. F., et al. 2013. Mol. Cancer Ther.12, 1461.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Standard Handling (A)