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. Author manuscript; available in PMC: 2017 Apr 24.
Published in final edited form as: Nat Chem Biol. 2016 Oct 24;12(12):1089–1096. doi: 10.1038/nchembio.2209

Figure 3. Biochemical and biophysical properties of bivalent inhibitors.

Figure 3

(a) (6S+2S)-PEG1, (6R+2R)-PEG1 or JQ1 were incubated with BRD4(1) and complex formation was assayed by size exclusion chromatography. (b) Stoichiometry of (6S+2S)-PEG1 or JQ1 binding to BRD4(1) as analyzed by Isothermal titration calorimetry. (c) Immunoblot for BRD4, MYC, and actin after treatment of MV4;11 cells with (6S+2S)-PEG1 or JQ1 at the indicated concentrations for 2 hours. (d) Immunoblot for BRD4, MYC, HEXIM1, and actin after treatment of MV4;11 cells with (6S+2S)-PEG1 at 10 nM at the indicated time points. Full blots can be found in Supplementary Figure 15.