For research use only. Not for therapeutic Use.
UPF 1069 is a PARP inhibitor, with IC50s of 8 and 0.3 μM for PARP-1 and PARP-2, respectively.
UPF 1069 (Compound 55) is a PARP inhibitor, with IC50s 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].
| Catalog Number | I000270 |
| CAS Number | 1048371-03-4 |
| Synonyms | 5-phenacyloxy-2H-isoquinolin-1-one |
| Molecular Formula | C17H13NO3 |
| Purity | ≥95% |
| 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 |
| SMILES | C1=CC=C(C=C1)C(=O)COC2=CC=CC3=C2C=CNC3=O |
| Reference | [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. |
