UPF 1069

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Technical Data

Molecular Weight 279.29 Storage powder
Formula

C17H13NO3

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CAS No. 1048371-03-4 Synonyms N/A
Solubility (25°C) * In vitro DMSO 56 mg/mL (200.5 mM)
Water Insoluble
Ethanol Insoluble
In vivo 2% DMSO+30% PEG 300+5% Tween 80+ddH2O 5mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 1(2H)-Isoquinolinone, 5-(2-oxo-2-phenylethoxy)-

Biological Activity

Description UPF 1069 is a selective PARP2 inhibitor with IC50 of 0.3 μM. It is ~27-fold selective against PARP1.
Targets
PARP2 [1] PARP1 [1]
0.3 μM 8.0 μM
In vitro UPF 1069 is a selective PARP2 inhibitor with IC50 of 0.3 μM while inhibiting PARP1 with IC50 of 8 μM. [1]
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. [1]
Features The most selective PARP2 inhibitor available to date. 

Protocol (Only for Reference)

Kinase Assay: [1]

PARP-1 and PARP-2 activity assays 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 mL of 50 mM Tris-HCl (pH 8.0) containing 5 mM MgCl2, 2 mM dithiothreitol, 10 mg sonicatedcalf thymus DNA, 0.2 mCi [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℃. 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. Nuclear extracts for PARP activity assay are prepared from PARP-1-/- and PARP-1+/+ mouse fibroblasts as previouslydescribed. Briefly, immortalized fibroblasts from PARP-1-/- and PARP-1+/+ mice are grown in DMEM supplemented with 2 mM glutamine, 10% bovine serum and antibiotics at 37℃. Nuclear extracts are prepared as follows: 10 cm confluent plates are scraped in 1 mL of homogenization buffer composed of 75 mM sucrose, 225 mM mannitol and 5 mM Tris, pH 7.4 plus 10 mL protease inhibitor cocktail. The cell suspension is homogenized with a Teflon pestle, and the mixture is centrifuged at 600 × g for 5 min at 4℃. The crude nuclear pellet is washed and resuspended in 1 mL of PARP assay buffer (5 mM MgCl2, 2 mM DTT, 50 mM Tris, pH 8) containing 100 mM N-methyl-N′-nitro-N-nitrosoguanidine (MNNG) to fully activate PARP activity. Samples containing 100 mL of the resuspended nuclear pellet are incubated for 60 min at 37℃ in the presence of 35.5 nM 3H-NAD. The reaction is stopped with 1 mL of 10% trichloroacetic acid (w/v), and the mixture is centrifuged at 12 000 × g for 10 min at 4℃. The reaction is terminated by the addition of 1 mL of 10% trichloroacetic acid (w/v), and radioactivity of the suspension is measured by liquid scintillation spectrometry.

Animal Study: [1]

Animal Models Rats deprived of hippocampi.
Formulation
Dosages 0.01-1 mM
Administration
 

References

PLEASE KEEP THE PRODUCT UNDER -20°C FOR LONG-TERM STORAGE.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.

Specific storage and handling information for each product is indicated on the product datasheet. Most Selleck products are stable under the recommended conditions. Products are sometimes shipped at a temperature that differs from the recommended storage temperature. Short-term storage of many products are stable in the short-term at temperatures that differ from that required for long-term storage.
We ensure that the product is shipped under conditions that will maintain the quality of the reagents. Upon receipt of the product, follow the storage recommendations on the product data sheet.

Chemical Structure

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