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EZH2 inhibition synergies with CDK9 inhibition
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Figure 1. Efficiency of CDKI-73 on diffuse large B-cell lymphoma cells. (A) The IC50 values of diffuse large B-cell lymphoma (DLBCL) cell lines after exposure to CDKI- 73/Flavopiridol for 72 hours (h). (B) Cellular CDK9 inhibition [2 h for detection of RNA polymerase II (RNA Pol II) (ser2)] and the level of apoptosis-related proteins (24 h) influenced by CDKI-73/Flavopiridol. (C) Apoptosis caused by CDKI-73/Flavopiridol. (D) The relative mRNA expression of MCL1 and XIAP after treated with CDKI- 73/Flavopiridol for 6 h. (E) Comet assay. Cells were treated with CDKI-73/Flavopiridol for 24 h (scale bar, 25 μm). Quantified results of the average DNA contents and the length of the comet tails using CometScor software. (F) γ-H2AX level in Pfeiffer and SU-DHL-4 cells treated with indicated time or dose of CDKI- 73/Flavopiridol. (G) Tumor growth curve graphs RTV over time in each treatment group in Pfeiffer xenografts. Data are expressed as the mean + standard error of the mean (SEM). All data are representative of at least three independent experiments. ***P<0.001, **P<0.01, *P<0.05 compared with the control group. Mut: mutant; wt: wild-type.
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