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. 2021 Jul 13;64(14):10102–10123. doi: 10.1021/acs.jmedchem.1c00348

Figure 10.

Figure 10

Inhibition of CREBBP/EP300 with 2 reduces c-Myc levels and acetylation of H3K18 in HCT116 cells (human colorectal cancer cell line) and stabilizes HIF-1α in hypoxia. (A) HCT116 cells were exposed to 2 (10 μM) for the times shown. Western blots were then carried out for the proteins indicated. β-Actin is included as a loading control. (B) HCT116 cells were exposed to 2 (10 μM) for the times indicated followed by mRNA preparation. Q-PCR was then carried out to determine c-Myc mRNA levels compared to the 18S. Data were analyzed using one-way ANOVA. *P < 0.05, **P < 0.01, ***P < 0.001. (C) The inactive compound 3 does not reduce levels of c-Myc. (D) HCT116 cells were exposed to compound 2 (10 μM) in hypoxia for the times shown. c-Myc was reduced in hypoxia, which is a known phenomenon. The stabilization of HIF-1α above the level observed in hypoxia alone was observed. (E) HCT116 cells were exposed to 2 (10 μM) or I-CBP112 for the times indicated. Treatment with both compounds resulted in a decrease in H3K27Ac and c-Myc. A decrease in H3K18Ac was observed upon treatment with 2 but not I-CBP112.