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. Author manuscript; available in PMC: 2011 Sep 15.
Published in final edited form as: Cancer Res. 2010 Sep 7;70(18):7232–7241. doi: 10.1158/0008-5472.CAN-10-0766

Figure 1.

Figure 1

In vitro assessment of PAC-1 and S-PAC-1. A, Structures of PAC-1 and S-PAC-1. B, The formation curve of the Zn2+:S-PAC-1 complex as determined by EGTA titration. S-PAC-1 binds zinc with a Kd of 46±5 nM. Error bars represent SEM (n=3). C, PAC-1 and S-PAC-1 induce rapid relief of zinc-mediated inhibition of procaspase-3 (D3A). Using a chromogenic Ac-DEVD-pNA substrate, the activity of procaspase-3 (7.5 µM) was assessed in the presence of inhibitory zinc (10 µM) and vehicle, PAC-1 or S-PAC-1 (50 µM). Maximal activity is observed after a 5-minute incubation with compound. Error bars represent the SEM (n=3). D, PAC-1 and S-PAC-1 both induce apoptotic cell death in U-937 cells as demonstrated by a population of annexin V positive, PI negative cells. Data shown is representative of three separate experiments.