PAC 1 is a procaspase-activating compound, which in turn produces caspase-3 (EC50 = 0.22 μM). PAC 1 also activates procaspase-7 in a less efficient manner (EC50 = 4.5 μM). This compound is a proapoptotic, inducing apoptosis in both cancerous and non-cancerous cell lines. The induction of apoptosis is dependent on the concentration of procaspase-3 (IC50 values anre 0.003-1.41 and 5.02=9.98 μM, respectively).
Putt et al (2006) Small-molecule activation of procaspase-3 to caspase-3 as a personalized anticancer strategy. Nat.Chem.Biol. 2 543.
Soluble in 1eq. HCl (75 nM), DMSO (100 mM), deionized water (≤2 mg/mL), water (0.25 mg/mL) at 25° C, ethanol (~5 mg/mL), DMSO:PBS(PH 7.2)(1:3), DMF (~30 mg/ml), and 1:3 solution of ethanol :PBS(PH 7.2) (~0.25 mg/ml).
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AzizAziz, G. et al. (PubMed 20638399) used PAC 1, a procaspase-activating compound, to validate that chicken cerebellar granule neurons function as a suitable model to study the mechanisms of interference with apoptosis of PAC 1 and similar compounds. PAC 1 successfully activated caspase-3-dependent cell death and was inhibited by the specific caspase-3-inhibitor Ac-DEVD-cmk. -SCBT Publication Review
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