PAC-1 (315183-21-2) is a procaspase-activating compound, directly activating procaspase-3, producing caspase-3, EC50=0.22 μM.1 It is less potent at activating procaspase-7, EC50=4.5 μM. It induces apoptosis in a variety of cancer cell lines. The mechanism of activation involves sequestering inhibitory zinc ions thus allowing procaspase-3 to autoactivate.2?? Sensitizes cancer cells to various chemotherapeutic agents.3
PAC-1 is a potent procaspase-3 activator with EC50 of 0.22 μM.
Procaspase-activating compound; activates procaspase-3 to produce caspase-3 (EC 50 = 0.22 μ M). Also activates procaspase-7 in a less efficient manner (EC 50 = 4.5 μ M). Pro-apoptotic; induces apoptosis in both cancerous and non-cancerous cells dependent on procaspase-3 concentration (IC 50 values are 0.003-1.41 and 5.02-9.98 μ M respectively).
1) Putt et al. (2006), Small-molecule activation of procaspase-3 to caspase-3 as a personalized anticancer strategy; Nat. Chem. Biol., 2 543
2) Peterson et al. (2009), PAC-1 activates procaspase-3 in vitro through relief of zinc-mediated inhibition; J. Mol. Biol., 388 144
3) Bolham et al. (2016), Small-Molecule Procaspase-3 Activation Sensitizes Cancer to Treatment with diverse Chemotherapeutics; ACS Cent. Sci., 2 545
