Drug intelligence / Profile preview

3PO

Development stage
Preclinical
Modality
Small Molecules
Administration
Intraperitoneal
01

Overview

3PO is a research-stage small-molecule inhibitor of 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 (PFKFB3), a key regulatory enzyme controlling fructose-2,6-bisphosphate levels and glycolytic flux in proliferating cells.[1][3][4][7] By competitively inhibiting PFKFB3, 3PO reduces intracellular fructose-2,6-bisphosphate, diminishes glycolytic flux, decreases glucose uptake and lactate production, and exerts cytostatic and cytotoxic effects on transformed and highly glycolytic cells, leading to tumor growth suppression in xenograft models.[1][2][3][4][7] It has also been shown to modulate neutrophil function by blocking pathogenic reactive oxygen species and neutrophil extracellular trap formation, suggesting potential anti-inflammatory applications, although its specificity for PFKFB3 has been questioned in recent mechanistic studies.[5]

Other names
PFKFB3 inhibitor 3POPFKFB-3 inhibitor 3POPFKFB 3 inhibitor 3PO3-(3-pyridinyl)-1-(4-pyridinyl)-2-propen-1-one3-(3-pyridinyl)-1-(4-pyridyl)-2-propen-1-one6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 inhibitor 3PO
02

Targets

PFKFB3

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