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Fig. 6 | Epigenetics & Chromatin

Fig. 6

From: Development of novel cellular histone-binding and chromatin-displacement assays for bromodomain drug discovery

Fig. 6

Pharmacological cross-validation of cellular histone and chromatin-binding assays with the TRIM24 biochemical AlphaScreen assay. a Merged IF images of two-color staining of OV90 cells following in situ cell extraction showing TRIM24 inhibitor-mediated displacement of endogenous TRIM24 (green) from chromatin while leaving histone H3 (red) protein levels unchanged (IACS-6558, 10 µM, 2 h). b Dose–response curves for a dozen TRIM24 inhibitors (1 h, no SAHA treatment) in OV90 cells using in situ cell extraction and IF detection/quantification. c EC50 values calculated from the above drug titration studies in OV90 cells (percent inhibition relative to DMSO control wells) were correlated with values obtained from the biochemical AlphaScreen and the cellular AlphaLISA assays

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