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Overview
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Background
First procaspase-activating compound (PAC-1) is a small-molecule activator of procaspase-3 that directly catalyzes the maturation of procaspase-3 to the active caspase-3 by inducing the cleavage of procaspase-3 in a time-dependent manner. As a result of the direct and immediate activation of procaspase-3, PAC-1 potently induces apoptosis in cancer cell lines. The PAC-1 induced apoptosis has been observed to be proportional to the concentrations of procaspase-3 inside the cells of primary colon cancer isolates. Study results have demonstrated that PAC-1 is able to induce cell death in both primary cancerous cells and adjacent normal tissues with 50% inhibition concentration IC50 values ranging from 0.003 to 1.41 μM and 5.02 to 9.98 μM respectively.
Reference:
Putt KS, Chen GW, Pearson JM, Sandhorst JS, Hoagland MS, Kwon JT, Hwang SK, Jin H, Churchwell MI, Cho MH, Doerge DR, Helferich WG, Hergenrother PJ. Small-molecule activation of procaspase-3 to caspase-3 as a personalized anticancer strategy. Nat Chem Biol. 2006 Oct;2(10):543-50. Epub 2006 Aug 27.
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- Properties
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Overview