| Bioactivity | FR054 is an inhibitor of the HBP enzyme PGM3, with a remarkable anti-breast cancer effect[1]. | ||||||||||||
| Invitro | 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[1].FR054 (250 μM, 24 h) treatment efficiently affects both N- and O-glycosylation levels in MDA-MB-231 cells[1].FR054 induces endoplasmic reticulum (ER) stress and a ROS-dependent apoptotic cell death[1]. Cell Viability Assay[1] Cell Line: | ||||||||||||
| In Vivo | FR054 (1000 mg/kg, ip) suppresses cancer growth in MDA-MB-231 xenograft mice[1]. Animal Model: | ||||||||||||
| Name | FR054 | ||||||||||||
| CAS | 35954-65-5 | ||||||||||||
| Formula | C14H19NO8 | ||||||||||||
| Molar Mass | 329.30 | ||||||||||||
| Appearance | Oil | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
|
||||||||||||
| Reference | [1]. Francesca Ricciardiello, et al. Inhibition of the Hexosamine Biosynthetic Pathway by targeting PGM3 causes breast cancer growth arrest and apoptosis. Cell Death Dis. 2018 Mar 7;9(3):377. |