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. Author manuscript; available in PMC: 2015 Dec 22.
Published in final edited form as: Nat Chem Biol. 2014 Sep 7;10(10):853–860. doi: 10.1038/nchembio.1629

Figure 4. Slow kinetics of SCH772984 both in vitro and in cell based systems.

Figure 4

a) ITC binding isotherms for the interactions of SCH772984 with ERK2 and haspin. Shown are raw titration heats (insets) as well as normalized binding heats. b) BLI data showing the association and dissociation sensograms at different inhibitor concentrations for the interaction of SCH772984 with ERK2 and haspin and ERK2 with VTX-11e. c) Comparison of cellular activities of the ERK inhibitors in MDA-MB 231 cells. Cells were treated with 100nM inhibitors for 4 hours and lysates were analysed using Western blotting before and after inhibitor wash out. Western blots band intensities were quantified and normalized relative to DMSO-treated cells. Quantification of Western blot signals for indicated phospho-proteins relative to loading controls is shown in the extrapolated recovery curves (lower panels) and reflects the recovery rates of MAPK pathway specific phosphorylation events. Western Blots show representative experiments of two repeats.