[CAS NO. 1048371-03-4] UPF1069
PRODUCTS SPECIFICATIONS [1048371-03-4]
DESCRIPTION [1048371-03-4]
Overview
| MDL | MFCD14051631 |
|---|---|
| Molecular Weight | 279.29 |
| Molecular Formula | C17H13NO3 |
| SMILES | O=C1NC=CC2=C1C=CC=C2OCC(C3=CC=CC=C3)=O |
1 Publications Citing Use of MCE
Summary
UPF 1069 is a PARP inhibitor, with IC 50 s of 8 and 0.3 μM for PARP-1 and PARP-2, respectively.
IC50 & Target
|
PARP-2 0.3 μM (IC 50 ) |
PARP-1 8 μM (IC 50 ) |
In Vitro
UPF 1069 (Compound 55) is a PARP inhibitor, with IC 50 s of 8 and 0.3 μM for PARP-1 and PARP-2, respectively [1] . UPF 1069 (1 µM) reduces the residual PARP activity by approximately 80% of PARP-1-deficient fibroblasts, but only slightly inhibits the enzymic activity in wild-type fibroblasts. UPF 1069 (0.1-1 µM) markedly enhances CA1 hippocampal damage. UPF 1069 (10 µM) also exacerbates oxygen-glucose deprivation (OGD) damage in organotypic hippocampal slices. However, UPF 1069 alleviates the damage cuased by OGD in mixed cortical cell cultures, shows a potent neuroprotective activity both at a concentration (1 µM) selectively acting on PARP-2 and at a concentration (10 µM) inhibiting both PARP-1 and PARP-2 activities [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 100 mg/mL ( 358.05 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.5805 mL | 17.9025 mL | 35.8051 mL |
| 5 mM | 0.7161 mL | 3.5805 mL | 7.1610 mL |
| 10 mM | 0.3581 mL | 1.7903 mL | 3.5805 mL |
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Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (8.95 mM); Clear solution
References
- [1] Pellicciari R, et al. On the way to selective PARP-2 inhibitors. Design, synthesis, and preliminary evaluation of a series of isoquinolinone derivatives. ChemMedChem. 2008 Jun;3(6):914-23.
- [2] Moroni F, et al. Selective PARP-2 inhibitors increase apoptosis in hippocampal slices but protect cortical cells in models of post-ischaemic brain damage.