3PO is a small-molecule inhibitor of PFKFB3 with an IC50 of 22.9 μM for recombinant human PFKFB3 protein and does not inhibit PFK-1 activity. It suppresses glucose uptake, and decreases the intracellular concentration of Fru-2,6-BP, lactate, ATP, NAD+, and NADH.

＞98%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

3-(3-pyridinyl)-1-(4-pyridinyl)-2-propen-1-one

white to beige powder

DMSO ：42 mg/mL (199.78 mM)

Ethanol ：42 mg/mL (199.78 mM)

PFKFB3

3PO is an inhibitor of the PFKFB3 isozyme primarily through competition with Fru-6-P and does not inhibit purified PFK-1 activity. 3PO markedly attenuates the proliferation of several human malignant hematopoietic and adenocarcinoma cell lines (IC50, 1.4-24 μmol/L) and is selectively cytostatic to ras-transformed human bronchial epithelial cells relative to normal human bronchial epithelial cells. 3PO can cause G2-M phase arrest.

i.p. administration of 3PO (0.07 mg/g) to tumor-bearing mice markedly reduces the intracellular concentration of Fru-2,6-BP, glucose uptake, and growth of established tumors in vivo. It suppresses tumorigenic growth of breast adenocarcinoma, leukemia, and lung adenocarcinoma cells in vivo[1]. The PK properties of 3PO are examined in C57Bl/6 mice intravenously administered 3PO: clearance CL=2312 mL/min/kg, T1/2=0.3 hr, Cmax=113 ng/ml, AUC0-inf=36 ng/hr/ml. 3PO is reported to have potent activity against a highly relevant mouse model of leukemia.

[1]. Clem B, et al. Small-molecule inhibition of 6-phosphofructo-2-kinase activity suppresses glycolytic flux and tumor growth. Mol Cancer Ther. 2008 Jan;7(1):110-20.

[2]. Schoors S, et al. Partial and transient reduction of glycolysis by PFKFB3 blockade reduces pathological angiogenesis. Cell Metab. 2014 Jan 7;19(1):37-48.

[3]. Lea MA, Inhibition of Growth of Bladder Cancer Cells by 3-(3-Pyridinyl)-1-(4-pyridinyl)-2-propen-1-one in Combination with Other Compounds Affecting Glucose Metabolism. Anticancer Res. 2015 Nov;35(11):5889-99.