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. 2012 May 24;122(6):2018–2031. doi: 10.1172/JCI46231

Figure 4. Sequence-dependent cytotoxicity of BIM SAHBA in hematologic cancer cells resistant to selective BCL-2/BCL-XL inhibition.

Figure 4

BIM SAHBA dose responsively reduces the viability of (A) OCI-AML3, (B) U937, (C) OPM-2, (D) Pfeiffer, and (E) K562 cancer cells, as measured at 24 hours by CellTiter-Glo assay (left column). R153D mutagenesis markedly impairs the cytotoxic activity of BIM SAHBA. Cells exposed to BIM SAHBA, but not its R153D mutant, exhibit dose-dependent annexin V binding at 6 hours after treatment, as monitored by FACS analysis (middle column). The negative effect of BIM SAHBA on cancer cell viability correlates with dose-responsive activation of caspase-3/7, as assessed by monitoring the cleavage of proluminescent caspase-3/7 substrate at 6 hours after treatment (right column). Data are mean ± SEM for experiments performed at least in triplicate. RLU, relative luminescence units.