CAS NO: | 1048371-03-4 |
规格: | ≥98% |
包装 | 价格(元) |
5mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
Molecular Weight (MW) | 279.29 |
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Formula | C17H13NO3 |
CAS No. | 1048371-03-4 |
Storage | -20℃ for 3 years in powder form |
-80℃ for 2 years in solvent | |
Solubility (In vitro) | DMSO: 56 mg/mL (200.5 mM) |
Water: <1 mg/mL | |
Ethanol: <1 mg/mL | |
Solubility (In vivo) | 2% DMSO+30% PEG 300+5% Tween 80+ddH2O: 5mg/mL |
Synonyms & Other info | Synonym: UPF-1069, UPF 1069, UPF1069 Chemical Name: 5-(2-oxo-2-phenylethoxy)isoquinolin-1(2H)-one InChi Key: JJWMRRNGWSITSQ-UHFFFAOYSA-N InChi Code: 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) SMILES Code: O=C1NC=CC2=C1C=CC=C2OCC(C3=CC=CC=C3)=O |
In Vitro | In vitro activity: PF 1069 (Compound 55) is a PARP inhibitor, with IC50s of 8 and 0.3 μM for PARP-1 and PARP-2, respectively. 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. Kinase Assay: PARP activity is evaluated by utilizing commercially available recombinant bovine PARP-1 and mouse PARP-2. Briefly, the enzymatic reaction is carried out in 100 μL of 50 mM Tris-HCl (pH 8.0) containing 5 mM MgCl2, 2 mM dithiothreitol, 10 μg sonicated calf thymus DNA, 0.2 μCi [adenine-2,8-3H]NAD and recombinant enzyme PARP-1 or PARP-2 (0.03 U per sample). Different concentrations of the putative inhibitors are added, and the mixture is incubated for 1 h at 37°C. The reaction is terminated by adding 1 mL of 10% trichloroacetic acid (w/v) and centrifuged. Pellets are then washed twice with 1 mL of H2O and resuspended in 1 mL of 0.1 M NaOH. The radioactivity incorporated from [adenine-2,8-3H]NAD into proteins is evaluated by liquid scintillation spectrometry. |
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In Vivo | In organotypic hippocampal slices, PARP-2 inhibition with UPF-1069 (0.01-1 mM) causes a concentration-dependent exacerbation (up to 155%) of oxygen-glucose deprivation (OGD)-induced CA1 pyramidal cell death. Higher concentrations, acting on both PARP-1 and PARP-2, have no effect on OGD injury. In mouse mixed cortical cells exposed to OGD, UPF-1069 (1-10 mM) significantly reduces post-ischaemic damage. |
Animal model | Mouse |
Formulation & Dosage | 0.01-1 mM |
References | Br J Pharmacol. 2009 Jul;157(5):854-62. |