| Molecular Formula | C17H13NO3 |
| Molar Mass | 279.29 |
| Solubility | Soluble in DMSO (up to 40 mg/ml). |
| Appearance | solid |
| Color | Off-white |
| Storage Condition | Store at RT |
| Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months. |
| Use | UPF 1069 is a PARP inhibitor with IC50 values of 8 and 0.3 μM for PARP-1 and PARP-2, respectively. |
| In vitro study | UPF 1069 is a selective inhibitor of PARP2 with an IC50 of 0.3 μm, whereas inhibition of PARP1 has an IC50 of 8 μm. |
| In vivo study | Treatment of organotypic hippocampal slices on UPF-1069 (0.01-1 mM) inhibited the dramatic increase (up to 155%) in CA1 pyramidal cell death induced by oxygen-glucose deprivation (OGD) by PARP-2. Higher concentrations were effective at PARP-1 and PARP-2 with no effect on OGD damage. UPF-1069 (1-10 mM) treatment of mixed cortical cells of OGD mice significantly reduced ischemic damage. |
| Hazard Symbols | Xn - Harmful![]() |
| Risk Codes | 22 - Harmful if swallowed |
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 3.581 ml | 17.903 ml | 35.805 ml |
| 5 mM | 0.716 ml | 3.581 ml | 7.161 ml |
| 10 mM | 0.358 ml | 1.79 ml | 3.581 ml |
| 5 mM | 0.072 ml | 0.358 ml | 0.716 ml |
| biological activity | UPF 1069 is a selective PARP2 inhibitor with IC50 of 0.3 μM, which is about 27 times higher than the selectivity for PARP1. |
| in vitro study | UPF 1069 is a selective PARP2 inhibitor with IC50 of 0.3 μM, while when PARP1 is inhibited, IC50 is 8 μM. |
| in vivo study | UPF-1069 (0.01-1 mM) treated organotypic hippocampal brain slices, inhibiting PARP-2 and oxygen-glucose deprivation (OGD)-induced CA1 pyramidal cell death (up to 155%). Higher concentrations can effectively act on PARP-1 and PARP-2, but have no effect on OGD damage. UPF-1069 (1-10 mM) treated the cortical cells of OGD mice, which significantly reduced ischemic damage. |
| features | UPF-1069 are the most selective PARP2 inhibitors. |
| target | PARP-2 0.3 μ m (IC 50 ) PARP-1 8 μ m (IC 50 ) |