Journal: Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie
Article Title: Breaking boundaries: Pan BETi disrupt 3D chromatin structure, BD2-selective BETi are strictly epigenetic transcriptional regulators.
doi: 10.1016/j.biopha.2022.113230
Figure Lengend Snippet: Fig. 5. Pan-BETi, not BD2-selective BETi, inhibit THP-1 proliferation and induce apoptosis. (A)THP-1 cells were treated for 72 hrs and proliferation was measured with Cell Titre Fluor (Promega), n = 5. (B) Pan-BETi, not BD2-BETi, induce apoptosis in THP-1 cells. THP-1 cells were treated with indicated compounds for 4 days after which cells were harvested and live stained via AnnexinV-FITC Apoptosis kit (BD Biosciences) and FACs was performed. (C) Pan-BETi, not BD2-BETi, induce apoptosis in THP-1 cells. Quantitation of triplicate flow cytometry data. n = 3. Apa5 (apabetalone 5 µM); Apa20 (apabetalone 20 µM); RVX2157 (10 µM); ABBV744 (40 nM); JQ1 (1 µM); IBET762 (0.5 µM); OTX015 (0.5 µM); Paclitaxel (100 nM). Bar graph statistics: One way ANOVA followed by Dunnet’s multiple comparison test; * , p < 0.05; * *, p < 0.01; * ** , p < 0.001.
Article Snippet: All compounds used in the study are commercially available Apabetalone (Selleck Chemicals S7295); ABBV744 (Selleck Chemicals S8723); JQ1 (Selleck Chemicals S7110); IBET762 (Selleck Chemicals S7189); OTX015 (Tocris 6181); MZ1 (Tocris 6154); Paclitaxel (Selleck Chemicals S1150) with the exception of RVX2157 which was prepared as previously described [55].
Techniques: Staining, Quantitation Assay, Flow Cytometry, Comparison