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MilliporeSigma™ Calbiochem™ PFKFB3 Inhibitor II, PFK15

Catalog No. 5310050001 Shop All MilliporeSigma Products
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53-100-50001 25 mg
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Description

A cell-permeable, bioavailable and more potent quinolinyl analog of PFKFB3 Inhibitor, 3PO (Cat

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 = 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 GI50 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.
TRUSTED_SUSTAINABILITY

Specifications

Color Light Beige
Description 97% by HPLC
Target Proteins PFKFB3
Molecular Formula C17H12N2O
Solubility DMSO
Content And Storage Protect from light
Form Solid
Quantity 25 mg
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