Biological Activity
Procaspase-activating compound; activates procaspase-3 to produce caspase-3 (EC50 = 0.22 μM). Also activates procaspase-7 in a less efficient manner (EC50 = 4.5 μM). Pro-apoptotic; induces apoptosis in both cancerous and non-cancerous cells dependent on procaspase-3 concentration (IC50 values are 0.003 - 1.41 and 5.02 - 9.98 μM respectively).
Compound Libraries
PAC 1 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 392.5 |
| Formula | C23H28N4O2 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 315183-21-2 |
| PubChem ID | 9675990 |
| InChI Key | YQNRVGJCPCNMKT-LFVJCYFKSA-N |
| Smiles | O=C(N/N=C/C3=CC=CC(CC=C)=C3O)CN(CC2)CCN2CC1=CC=CC=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| 1eq. HCl | 29.44 | 75 | |
| DMSO | 39.25 | 100 | |
| ethanol | 19.63 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 392.5. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.55 mL | 12.74 mL | 25.48 mL |
| 5 mM | 0.51 mL | 2.55 mL | 5.1 mL |
| 10 mM | 0.25 mL | 1.27 mL | 2.55 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.51 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Putt et al (2006) Small-molecule activation of procaspase-3 to caspase-3 as a personalized anticancer strategy. Nat.Chem.Biol. 2 543 PMID: 16936720
Peterson et al (2009) Procaspase-3 activation as an anti-cancer strategy: structure-activity relationship of procaspase-activating compound 1 (PAC-1) and its cellular co-localization with caspase-3. J.Med.Chem. 52 5721 PMID: 19708658
Keywords: PAC 1, supplier, activators, procaspase-3, proapoptotic, Caspases, Proteinases, Proteases, PAC1, Caspases, Enzyme, Substrates, /, Activators, Caspases, Tocris Bioscience
