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. Author manuscript; available in PMC: 2012 Oct 15.
Published in final edited form as: Chem Biol Interact. 2011 Aug 16;194(1):58–68. doi: 10.1016/j.cbi.2011.08.005

Figure 3. Doses of analogs that cause equipotent proteasome inhibition are similarly cytotoxic.

Figure 3

A. Higher doses of non-LG analogs are required to cause decreases in viability of Jurkat cells as measured by trypan blue exclusion. B. Non-LG analogs have IC50 values in the micromolar range, compared to the LG analogs with have IC50s in the nanomolar range. IC50 doses were determined from the viability readings in (3A). C. Equipotent concentrations were identified to induce DNA fragmentation. Jurkat cells were treated with increasing concentrations of marizomib, NPI-2078 and NPI-2104 for 24 h. DNA fragmentation was assessed by propidium iodide staining followed by flow cytometry. Shown are effects of concentrations identified to induce DNA fragmentation in 50% of the cell population. D. Analysis of CT-L activity with equipotent concentrations. Jurkat cells were treated with equipotent concentrations identified in (C) of NPI-2078, NPI-2104 and marizomib. Samples were analyzed for CT-L activity after 1 and 12 h of exposure to analogs. Control cells treated with DMSO were defined as exhibiting 100% of CT-L activity. * P < 0.05 control cells compared to treatment (two way ANOVA and post-hoc analysis with Bonferroni’s test). LG: leaving group, Non-LG: non-leaving group.