MilliporeSigma™ Calbiochem™ PFKFB3 Inhibitor II, PFK15

Description

• 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 (IC 50 = 207nM compared to 22.9μM 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 ∽10μM) nor PFK-1, hexokinase, phosphoglucoisomerase, or PFKFB4 even at 100μM
• Induces apoptosis and reduces proliferation in transformed cells (mean GI 50 of ∽3μM 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 (∽25mg/kg, i.p
• administered every 3rd day)
• Please note that the molecular weight for this compound is batch-specific due to variable water content.