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UPF 1069
- Soluble in DMSO
- MF: C17H13NO3
- MW: 279.29
Description
PARP-2 inhibitor with >26 fold selectivity over PARP1 (IC50 values 8.0 µM and 0.3 µM for PARP1 and PARP2, respectively) that exacerbates oxygen-glucose deprivation (OGD) injury in the hippocampus, but significantly attenuates OGD damage in mixed cortical cell cultures at concentrations high enough to inhibit both PARP1 and PARP2. UPF 1069 is a valuable tool to explore the function of PARP-2 in biological systems and to examine the different roles of PARP isoenzymes in the mechanisms of cell death and survival.
More Information
| Parent CAS No. | 1048371-03-4 |
|---|---|
| Chemical Name | 5-(2-oxo-2-phenylethoxy)isoquinolin-1(2H)-one |
| SMILES | C1C=C2C(=O)NC=CC2=C(OCC(=O)C2C=CC=CC=2)C=1 |
| MFCD | MFCD14051631 |
| InChi | InChI=1S/C17H13NO3/c19-15(12-5-2-1-3-6-12)11-21-16-8-4-7-14-13(16)9-10-18-17(14)20/h1-10H,11H2,(H,18,20) |
| InChiKey | JJWMRRNGWSITSQ-UHFFFAOYSA-N |
| CID | 25015515 |
| Short Description | PARP2 inhibitor |
References
- F. Moroni et al. Selective PARP-2 inhibitors increase apoptosis in hippocampal slices but protect cortical cells in models of post-ischaemic brain damage. Br. J. Pharmacol. 2009, 157, 854-862.
- R. Pellicciari et al. On the way to selective PARP-2 inhibitors. Design, synthesis, and preliminary evaluation of a series of isoquinolinone derivatives. ChemMedChem. 2008, 3, 914-923.
- T. Haikarainen et al. Evaluation and Structural Basis for the Inhibition of Tankyrases by PARP Inhibitors. ACS Med. Chem. Lett. 2013, 5, 18-22.
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