| Catalog | Description | Size | Price (USD) | Qty |
|---|---|---|---|---|
| GBM-2979-5MG | PAC-1 | 5mg | $63.00 | |
| GBM-2979-25MG | PAC-1 | 25mg | $200.00 |
| Bioassays Specification | |
| Bio-Activity | Procaspase-3 activator |
| Chemical Name | 4-(Phenylmethyl)-1-piperazineacetic acid [[2-hydroxy-3-(2-propenyl)phenyl]-methylene]hydrazide |
| Function / Pharmacology | PAC-1 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 |
| CAS# | 315183-21-2 |
| MW | 392.49 |
| Molecular Formula | C23H28N4O2 |
| Solubility | Soluble in DMSO (up to 35 mg/ml) or in Ethanol (up to 15 mg/ml) |
| Supplied | powder |
| Storage as supplied | -20°C |
| Ship temp | Ambient |
| References | 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 |
| Protein Specification | |
| Purity | >98% |
| Bioassays Specification | |
| Bio-Activity | Procaspase-3 activator |
| Chemical Name | 4-(Phenylmethyl)-1-piperazineacetic acid [[2-hydroxy-3-(2-propenyl)phenyl]-methylene]hydrazide |
| Function / Pharmacology | PAC-1 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 |
| CAS# | 315183-21-2 |
| MW | 392.49 |
| Molecular Formula | C23H28N4O2 |
| Solubility | Soluble in DMSO (up to 35 mg/ml) or in Ethanol (up to 15 mg/ml) |
| Supplied | powder |
| Storage as supplied | -20°C |
| Ship temp | Ambient |
| References | 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 |
| Protein Specification | |
| Purity | >98% |
