Fig. 2: Structure-activity relationships of T-448 analogs. | Nature Communications

Fig. 2: Structure-activity relationships of T-448 analogs.

From: Covalent adduct Grob fragmentation underlies LSD1 demethylase-specific inhibitor mechanism of action and resistance

Fig. 2: Structure-activity relationships of T-448 analogs.

a Table summarizing enzyme inhibition (IC50) and fragmentation activity of T-488 (2) analogs where the % of each FAD species is reported along with the relative % N-formyl-FAD formed. IC50 values are reported as mean ± s.d. of n = 3 biological replicates (see Fig. S1b and S2c for full inhibition curves). b Binding curves showing fluorescence polarization (y-axis) for increasing concentrations of LSD1-CoREST (x-axis) in the presence of a labelled SNAG(2-10) peptide after treatment with vehicle or LSD1 inhibitor (n = 3 biological replicates). c Co-IP of FLAG-LSD1 with GFI1B after vehicle or LSD1 inhibitor treatment (500 nM, 48 h) in transiently transfected HEK 293T cells. * denotes skipped lane. Data in (a–c) are representative of two independent experiments. Data in (a) are provided in Supplementary Data 1. Source data are provided as a Source Data file for (b, c).

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