FR054 是 HBO 酶 PGM3 的抑制剂，具有明显的抗乳腺癌活性。
货号:ajcx35972
CAS:35954-65-5
分子式:C14H19NO8
分子量：329.3
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

FR054 is an inhibitor of the HBP enzyme PGM3, with a remarkable anti-breast cancer effect[1].

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].

FR054 (1000 mg/kg, ip) suppresses cancer growth in MDA-MB-231 xenograft mice[1].

[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.