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FR054

Chemical Structure : FR054

CAS No.: 10378-06-0

FR054 (FR-054, (6R)-FR054 )

Catalog No.: PC-49557Not For Human Use, Lab Use Only.

FR054 (FR-054) is a specific small molecule inhibitor of hexosamine biosynthetic pathway (HBP) enzyme N-Acetylglucosamine-phosphate Mutase (PGM3), shows a remarkable anti-breast cancer effect.

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Biological Activity

FR054 (FR-054) is a specific small molecule inhibitor of hexosamine biosynthetic pathway (HBP) enzyme N-Acetylglucosamine-phosphate Mutase (PGM3), shows a remarkable anti-breast cancer effect.
FR054 enhanced the stability of PGM3 protein in a dose-dependent manner and with a more potent binding than the natural substrate GlcNAc-6-P.
FR054 induced an early proliferation arrest followed by a marked cell death increase in breast cancer cells.
FR054 (250 μM, 24 h) treatment efficiently affected both N- and O-glycosylation levels in MDA-MB-231 cells.
FR054 reduced MDA-MB-231 cell adhesion, migration, and integrin β1 membrane localization, induced ER stress and a ROS-dependent apoptotic cell death.
FR054 (1000 mg/kg, 10% DMSO) administered in single dose reduced tumor growth in nude mice xenograft model of TNBC cells MDA-MB-231.

Physicochemical Properties

M.Wt 329.30
Formula C14H19NO8
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-Methyl-(3,4,6-tri-O-acetyl-1,2-dideoxy-α-d-glucopyrano)-[2,1-d]-2-oxazoline

References

1. Ricciardiello F, et al. Cell Death Dis. 2018 Mar 7;9(3):377.

2. Ricciardiello F, et al. Oncogene. 2020 May;39(20):4103-4117.

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