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FR054 is an inhibitor of the HBP enzyme PGM3, with a remarkable anti-breast cancer effect.

FR054 (0.5-1 mM, 24-48 h) induces an early proliferation arrest followed by a marked cell death increase in breast cancer cells and induces apoptosis. The effect of FR054 occurs through PGM3 inhibition instead of other off-target effects.
FR054 (250 μM, 24 h) treatment efficiently affects both N- and O-glycosylation levels in MDA-MB-231 cells.
FR054 induces endoplasmic reticulum (ER) stress and a ROS-dependent apoptotic cell death.

FR054 (1000 mg/kg, ip) suppresses cancer growth in MDA-MB-231 xenograft mice.

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