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. Author manuscript; available in PMC: 2020 Jul 19.
Published in final edited form as: ACS Chem Biol. 2019 Jul 2;14(7):1393–1397. doi: 10.1021/acschembio.9b00292

Figure 2.

Figure 2.

In vitro assay with HDAC11 inhibitors. (A) Optimization of HDAC11 inhibitors based on SIS4. Optimization of HDAC11 inhibitors based on SIS4. IC50 values were obtained by using myristoyl-H3K9 peptide as the substrate except values shown in parentheses for SIS7 and SIS17, which are measured using myristoyl-SHMT2 peptide as the substrate. Some of the IC50 curves are shown in Supplementary Figure 1. (B) Comparing SIS7 and SIS17 to FT895 on HDAC11 inhibition using myristoyl-H3K9. IC50 values using myristoyl-H3K9 derived from GraphPad Prism are presented as mean values from three independent experiments. (C) In vitro IC50 values against different HDACs and sirtuins with acyl-H3K9 peptides. [a] acyl-H3K9 peptides used. [b] FT895 inhibited 50% of HDAC4 activity at 25 μM but inhibition with higher concentration did not increase inhibition rate. [c] Deacetylation activity of enzyme tested. [d] Detrifluoroacetylation activity of enzyme tested. [e] Demyristoylation activity of enzyme tested. [f] Both deacetylation and demyristoylation activities of enzyme tested.