Skip to main content
. 2016 Jul 20;44(19):9206–9217. doi: 10.1093/nar/gkw621

Figure 5.

Figure 5.

Pharmacological inhibition of Set7 methyltransferase activity attenuates the expression of SM-associated genes. (A) Chemical structure of the Set7 inhibitor, (R)-PFI-2. (B) Inhibition of SRF and H3K4 methylation by the (R)-PFI-2 compound. A total of 5 μM of (R)-PFI-2 was added in each reaction and the activity assessed. Flag-Set7 activity is presented as fold-change normalized to DMSO control. A total of 2 nmol of H3K4 peptide was used as a control substrate. (C) Set7 inhibitor (R)-PFI-2 attenuates expression of SM-associated genes. Sca1+ cells (upper panel) and mouse aortic SMCs (lower panel) were incubated with 20 μM (R)-PFI-2 for 2 days. DMSO was used as a vehicle control. mRNA levels of histone modifiers and SM-associated markers were assessed by qRT-PCR using Gapdh as the internal control. Gene expression was normalized against DMSO control. Error bars represent the standard error of the mean of at least three independent experiments. *P < 0.05, **P < 0.01 and ***P < 0.001.