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. Author manuscript; available in PMC: 2014 Mar 15.
Published in final edited form as: ACS Chem Biol. 2012 Dec 26;8(3):626–635. doi: 10.1021/cb300604u

Figure 4. KG-548 disrupts in vitro ARNT/TACC3 interactions.

Figure 4

a. Titration of KG-548 into an in vitro pulldown assay of minimal ARNT PAS-B and TACC3-CT interacting fragments shows a dose-dependent reduction in ARNT/TACC3 complex formation. b. Quantification of KG-548 potency for disrupting the ARNT PAS-B/TACC3-CT interaction as provided by AlphaScreen, showing an apparent IC50 of 25 µM. c. Co-immunoprecipitation assays of full length ARNT and TACC3 proteins in HEK293T cell lysates show that KG-548 weakens the ARNT/TACC3 interaction as demonstrated by the dose-dependent decrease in the intensity of the ARNT protein band (quantitated with % remaining compared to DMSO control) associated with immunoprecipitated TACC3 protein.