Fig. 4.

1 inhibits CDKs in human cells, inducing cell cycle arrest. (A) Inhibition of luciferase-CDK2/cyclin E1 nanoBRET signal with BGC HX1012/HX1035-derived metabolites. Data represent the average ± the SD of the mean, n = 6. ND = not determined; inhibition did not exceed 50% at the highest concentration tested (50 µM). DIN, dinaciclib. (B) Cell cycle distribution measured by DAPI after 24 h treatment with 25 µM 1 compared to dimethyl sulfoxide (DMSO) in synchronized HCT116 cells (means ± SD; n = 6). ****P < 0.0001, two-way ANOVA with Sidak post hoc test. (C) EdU and pHH3 incorporation measured by flow cytometry with varied concentrations of 1 in synchronized HCT116 cells (means ± SD; n = 6).