FIGURE 1:
Synthesis and characterization of FX12 as a dislocation inhibitor. (A) Chemistry optimization through SAR studies of Stattic. (B) drGFP assay. HeLa cells stably expressing NHK-drGFP reporter plasmids were treated with DMSO (background control), proteasome inhibitor BTZ (50 nM) alone (positive control), or BTZ in combination with series concentrations of the indicated compounds for 4 h before GFP intensities were measured in a microplate reader. GFP intensities were normalized to the positive control (set as 100%) after background subtraction. Error bars = SD for n = 3 biological replicates. (C) Cytotoxicity assay. HepG2 cells were treated with increasing concentrations of FX12 or its analogues for 24 h followed by measuring cell viability with WST-1. Cells treated with DMSO was used as control (set as 100%). Error bars = SD for n = 5 biological replicates. (D) IC50s derived from C.