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 ) |