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. Author manuscript; available in PMC: 2023 Oct 19.
Published in final edited form as: J Am Chem Soc. 2022 Oct 6;144(41):18861–18875. doi: 10.1021/jacs.2c05030

Figure 2. Aza-SAHA derivative DKFZ-711 is a potent and selective HDAC10 binder.

Figure 2.

A. Molecules obtained from an “aza-scan” of the SAHA linker; B. Differential scanning fluorimetry thermal shift assay of aza-SAHA derivatives (500 μM) performed in duplicate with recombinant HDAC10 (4 μM); C. HDAC isozyme selectivity heatmap and pIC50 values of aza-SAHA derivatives reveal diverse inhibitory profiles depending on the nitrogen position. pIC50 values are the mean of two replicates, each determined by four-parameter non-linear regression analysis with eight dose levels in triplicate with HDAC Glo assaya or FRET assayb. c Mean of three individual experiments. d Curve fit was not convergent at 100 μM. For 95% confidence intervals, see Table S1.