Fig. 5. SGC3027 inhibits HSP70 methylation in cells and its active component SGC8158 methylation in vitro.

a SGC8158 inhibits PRMT7 methylation of HSPA8 in vitro. SGC8158 IC₅₀ = 294 ± 26 nM (2 biological replicates, each with technical n = 3, mean ± SEM), SGC8158N IC₅₀ > 100 µM (n = three technical replicates). The methylation assay was performed in the presence of ATP (n = 3 technical replicates). b SGC3027 is a prodrug cellular inhibitor of PRMT7 as illustrated by the prodrug conversion to the active component in cells. c SGC3027 inhibits PRMT7-dependent HSP70 monomethylation in C2C12 cells. Cells were treated with the compound for 2 days. The experiment was repeated four times with similar results. d Quantification of SGC3027 and SGC3027N effects on HSP70 monomethylation in C2C12 cells. The graphs represent non-linear fits of Rme1 signal intensities normalized to intensities of HSP70. SGC3027: n = 11, four separate experiments, IC₅₀ = 2.4 ± 0.1 µM; SGC3027N: n = 4 technical replicates, IC₅₀ > 40 µM (mean ± SEM). e A representative blot for SGC3027N effects on HSP70 methylation. Rme1—arginine monomethylation. The experiment with 3 and 10 µM SGC3027N concentration was repeated three times with similar results. Source data are provided as a Source Data file.