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. Author manuscript; available in PMC: 2019 Dec 27.
Published in final edited form as: J Med Chem. 2019 Dec 5;62(24):11232–11259. doi: 10.1021/acs.jmedchem.9b01411

Figure 8.

Figure 8.

Compound target engagement in cell lysates. Levels of c-MYC and RBBP5 proteins in association with WDR5 were assessed after treatment with compound in lysates from WDR5-FLAG and c-MYC-HA co-overexpressing HEK293 cells. A fraction of the lysate before addition of compound is shown as a control lane. An α-FLAG immunoprecipitation was used to isolate WDR5, which is not detectable in the input due to the excess of WDR5 in the IP fraction. c-MYC and RBBP5 were blotted in independent experiments. Data are representative of minimum two independent biological repeats. α-FLAG immunoprecipitation from lysates treated with 50 μM compound from the A) acid subseries and B) amide subseries. C) A dose response treatment of compounds 6r and 7k from 6.25 to 50 μM, as compared to 50 μM treatment with respective inactive controls 6-NC and 7-NC and the vehicle control (VC). Control cells express c-MYC-HA and a GFP-FLAG construct. Panels D), E) and F) present quantification of two independent experiments, normalized to vehicle control.