product name UPF 1069
Description: UPF 1069, a derivative of isoquinolinone, is a potent and selective inhibitor of poly-(ADP-ribose) polymerase 2 (PARP-2), with the value of 50% inhibition concentration IC50 of 0.3 μmol/L, that is capable of reducing PAR formation both in recombinant enzyme preparations and in nuclear extracts from PARP-1-/- fibroblasts. Although its inhibition towards PARP-2 is most selective among other PARP-2 inhibitors, UPF 1069 also inhibits PARP-1 with a lesser potency (the value of IC50 of 8 μmol/L).
References: Br J Pharmacol. 2009 Jul;157(5):854-62.
279.29
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 peoduct :
| In Vitro |
In vitro activity: UPF 1069 is a selective PARP2 inhibitor with IC50 of 0.3 μM while inhibiting PARP1 with IC50 of 8 μM. Kinase Assay: Cell Assay: |
|---|---|
| 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 | |
| Formulation & Dosage | |
| References | Br J Pharmacol. 2009 Jul;157(5):854-62. |
