UPF 1069

Selective PARP2 inhibitor CAS# 1048371-03-4

UPF 1069

Catalog No. BCC2213----Order now to get a substantial discount!

Product Name & Size Price Stock
UPF 1069:10mg $90.00 In stock
UPF 1069:20mg $153.00 In stock
UPF 1069:50mg $360.00 In stock
UPF 1069:100mg $630.00 In stock
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Chemical structure

UPF 1069

3D structure

Chemical Properties of UPF 1069

Cas No. 1048371-03-4 SDF Download SDF
PubChem ID 25015515 Appearance Powder
Formula C17H13NO3 M.Wt 279.29
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : ≥ 100 mg/mL (358.05 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name 5-phenacyloxy-2H-isoquinolin-1-one
SMILES C1=CC=C(C=C1)C(=O)COC2=CC=CC3=C2C=CNC3=O
Standard InChIKey JJWMRRNGWSITSQ-UHFFFAOYSA-N
Standard 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)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of UPF 1069

DescriptionSelective poly(ADP-ribose) polymerase (PARP) 2 inhibitor (IC50 values are 0.3 and 8.0 μM for PARP-2 and PARP-1 respectively).

Protocol

Kinase Assay [2]
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[2].

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.

UPF 1069 Dilution Calculator

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UPF 1069 Molarity Calculator

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Preparing Stock Solutions of UPF 1069

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.5805 mL 17.9025 mL 35.8051 mL 71.6102 mL 89.5127 mL
5 mM 0.7161 mL 3.5805 mL 7.161 mL 14.322 mL 17.9025 mL
10 mM 0.3581 mL 1.7903 mL 3.5805 mL 7.161 mL 8.9513 mL
50 mM 0.0716 mL 0.3581 mL 0.7161 mL 1.4322 mL 1.7903 mL
100 mM 0.0358 mL 0.179 mL 0.3581 mL 0.7161 mL 0.8951 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on UPF 1069

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). Having been used to investigate the role of PARP-1 and PARP-2 in post-ischaemic brain damage, UPF 1069 enhances oxygen-glucose deprivation (OGD) injury in hippocampal slices.

Reference

Moroni F, Formentini L, Gerace E, Camaioni E, Pellegrini-Giampietro DE, Chiarugi A, Pellicciari R. 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(5):854-862

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References on UPF 1069

Selective PARP-2 inhibitors increase apoptosis in hippocampal slices but protect cortical cells in models of post-ischaemic brain damage.[Pubmed:19422384]

Br J Pharmacol. 2009 Jul;157(5):854-62.

BACKGROUND AND PURPOSE: Poly(ADP-ribose) polymerases (PARP)-1 and PARP-2 play complementary tasks in the maintenance of genomic integrity, but their role in cell death or survival processes is rather different. A recently described series of selective PARP-2 inhibitors (UPF-1035, UPF-1069) were used to study the role of PARP-1 and PARP-2 in post-ischaemic brain damage. EXPERIMENTAL APPROACH: We evaluated post-ischaemic brain damage in two different in vitro models: rat organotypic hippocampal slices exposed to oxygen-glucose deprivation (OGD) for 20-30 min, a model characterized by apoptosis-like cell death and mouse mixed cortical cell cultures exposed to 60 min OGD, a model in which cells die with mostly necrosis-like features. KEY RESULTS: In organotypic hippocampal slices, PARP-2 inhibition with UPF-1069 (0.01-1 micromolxL(-1)) caused a concentration-dependent exacerbation (up to 155%) of OGD-induced CA1 pyramidal cell death. Higher concentrations, acting on both PARP-1 and PARP-2, had no effect on OGD injury. In mouse mixed cortical cells exposed to OGD, on the contrary, UPF-1069 (1-10 micromolxL(-1)) significantly reduced post-ischaemic damage. CONCLUSION AND IMPLICATIONS: Selective PARP-2 inhibitors increased post-OGD cell death in a model characterized by loss of neurons through a caspase-dependent, apoptosis-like process (hippocampal slice cultures), but they reduced post-OGD damage and increased cell survival in a model characterized by a necrosis-like process (cortical neurons). UPF-1069 may be 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.

Mild activation of poly(ADP-ribose) polymerase (PARP) is neuroprotective in rat hippocampal slice models of ischemic tolerance.[Pubmed:22639866]

Eur J Neurosci. 2012 Jul;36(1):1993-2005.

Ischemic tolerance is a phenomenon in which exposure to a mild preconditioning stress results in resistance to a subsequent lethal ischemic insult. Here we investigated the role of poly(ADP-ribose) polymerase (PARP) in the development of ischemic tolerance by using organotypic rat hippocampal slices exposed to 30 min oxygen-glucose deprivation (OGD), which leads to selective injury of the CA1 subregion 24 h later. We developed models of pharmacological preconditioning by exposing slices to subtoxic concentrations of either N-methyl-D-aspartate (NMDA) or (S)-3,5-dihydroxyphenylglycine (DHPG) and then, 24 h later, to 30 min OGD. Under these conditions, we observed a significant reduction in OGD-induced CA1 damage. Exposure of slices to the PARP-1 and -2 inhibitors TIQ-A, PJ-34 and UPF 1069 during preconditioning prevented the development of OGD tolerance in a concentration-dependent manner. NMDA and DHPG preconditioning increased the activity of PARP, as detected by immunoblots using antibodies against the poly(ADP-ribose) polymer product, but was not associated with consumption of cellular NAD(+) or ATP. Neuroprotection induced by preconditioning was also prevented by the caspase inhibitor Z-VAD-FMK. The modest but significant increase in caspase-3/7 induced by preconditioning, however, was not associated with PARP-1 cleavage, as occurred with staurosporine. Finally, TIQ-A prevented the activation of ERK1/2 and Akt induced by NMDA preconditioning, suggesting that the protective mechanism evoked by PARP requires activation of these prosurvival mediators. Our results suggest that preconditioning with appropriate pharmacological stimuli may promote neuroprotective mechanisms triggered by the sublethal activation of two otherwise deleterious executioners such as PARP and caspase-3/7.

Description

UPF 1069 is a PARP inhibitor, with IC50s of 8 and 0.3 μM for PARP-1 and PARP-2, respectively.

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