Figure 5 | British Journal of Cancer

Figure 5

From: Selective AKR1C3 inhibitors do not recapitulate the anti-leukaemic activities of the pan-AKR1C inhibitor medroxyprogesterone acetate

Figure 5

Identification of AKR1C3-selective inhibitors from the NCI Diversity Set. (A) NCI compounds were screened against recombinant AKR1C proteins using the AKR1C-diaphorase assay (see Materials and Methods) and % inhibition of activity measured. IC50s of selected compounds against all four AKR1C isoforms, shown below the bar chart, were calculated using dose titrations of each compound against recombinant AKR1C protein in the NADPH assay. (B) Cumulative cell counts for HL60, K562 and KG1a after 7 days treatment with either solvent control, 5 μ M MPA, or the selected compounds at 10 times the IC50 concentration, without (top three panels) or with 0.5 mM BEZ (bottom three panels). Data shown is mean of a minimum of N=3 experiments±s.e.m. *P<0.01.

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