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PAC-1 is a procaspase-activating compound; activates procaspase-3 to produce caspase-3 (EC50 = 0.22 μM). PAC-1 enhances the activity of procaspase-3 in vitro and induces apoptotic death in cancer cells in culture and in mouse xenograft models. Signaling through the neuropeptide GPCR PAC(1) induces neuritogenesis via a single linear cAMP- and ERK-dependent pathway using a novel cAMP sensor. The data presented herein further bolster the hypothesis that PAC-1 induces apoptosis in cancer cells through the direct activation of procaspase-3, has implications for the design and discovery of next-generation procaspase-3 activating compounds, and sheds light on the anti-apoptotic role of cellular zinc.
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Source | Exp Hematol (2015). Figure 2.PAC-1 |
| Method | flow cytometry | |
| Cell Lines | MM cell lines | |
| Concentrations | 3 and 10 μmol/L | |
| Incubation Time | 24 hours | |
| Results | Both MM.1S and U266 cells demonstrated a time-dependent decrease in cell viability. |
| Cell Experiment | |
|---|---|
| Cell lines | U-937, HL-60, CRL-1872, ACHN, NCI-H226, Hs888Lu, Hs578Bst, MCF-10A, SK-MEL-5, BT-20, MDA-MB-231, UACC-62, SK-N-SH, B16-F10 , Hs 578t and PC-12 |
| Preparation method | Determination of IC50 values in various cell lines. Various concentrations of etoposide or PAC-1 were added to cells and incubated for 24 h and 72 h for etoposide and PAC-1, respectively. Cell death was quantified by the addition of MTS/PMS CellTiter 96 Cell Proliferation Assay reagent (Promega). The plates were incubated at 37 1C for approximately 1 h (until the colored product formed), and the absorbance was measured at 490 nm. |
| Concentrations | 0~20 µM |
| Incubation time | 24 h and 72 h |
| Animal Experiment | |
|---|---|
| Animal models | nude mice bearing NCI-H226 xenograft model |
| Formulation | mixture of 24:1 vegetable oil/DMSO |
| Dosages | 50 and 100 mg/kg once a day for 21 d |
| Administration | oral gavage |
| Molecular Weight | 392.5 |
| Formula | C23H28N4O2 |
| CAS Number | 315183-21-2 |
| Solubility (25°C) | DMSO 48 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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| VMY-1-103
VMY-1-103 is an inhibitor for cyclin/Cdk complex, that arrests the cell cycle at G1 phase. |
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