YZ9

• CAT Number: R063926
• CAS Number: 6093-71-6
• Molecular Formula: C12H10O5
• Molecular Weight: 234.207
• Purity: ≥95%
• Storage: -20°C
• IUPAC Name: ethyl 7-hydroxy-2-oxochromene-3-carboxylate
• InChI: InChI=1S/C12H10O5/c1-2-16-11(14)9-5-7-3-4-8(13)6-10(7)17-12(9)15/h3-6,13H,2H2,1H3
• InChIKey: IETDBZQIWIJQJG-UHFFFAOYSA-N
• SMILES: CCOC(=O)C1=CC2=C(C=C(C=C2)O)OC1=O

Cells that are rapidly proliferating or hypoxic emphasize glycolysis over oxidative phosphorylation to meet energy needs. During glycolysis, fructose 6-phosphate (F6P) is phosphorylated by 6-phosphofructo-2-kinases (PFKs) to generate fructose 2,6-bisphosphate. As PFK family members also mediate the reverse reaction as fructose 2,6-bisphosphatases, these enzymes are known as PFKFB family members. Notably, PFKFB3 is overexpressed in a wide variety of cancer cell lines. YZ9 is a potent inhibitor of PFKFB3, with an IC50 value of 183 nM in vitro. It avidly competes with F6P at PFKFB3 (Ki = 94 nM). YZ9 is also cell permeable, inhibiting the growth of HeLa cells with a GI50 value of 2.7 µM.