- 貨號 Cat. No.
- S8038
- 規格 Size
- 5~200mg
- 品牌 Brand
- Selleckchem
Description
UPF 1069
Catalog No.S8038
UPF 1069 is a selective PARP2 inhibitor with IC50 of 0.3 μM. It is ~27-fold selective against PARP1.
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10mM/1mLIn DMSO |
USD 239 |
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10mg |
USD 185 |
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50mg |
USD 592 |
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
Description |
UPF 1069 is a selective PARP2 inhibitor with IC50 of 0.3 μM. It is ~27-fold selective against PARP1. |
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Targets |
PARP2 |
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IC50 |
0.3 μM [1] |
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In vitro |
UPF 1069 is a selective PARP2 inhibitor with IC50 of 0.3 μM while inhibiting PARP1 with IC50 of 8 μM. [1] |
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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. [1] |
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Features |
The most selective PARP2 inhibitor available to date. |
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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. |
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Animal Study: [1]
Animal Models |
Rats deprived of hippocampi. |
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Dosages |
0.01-1 mM |
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Administration |
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1
References
Download UPF 1069 SDF
Molecular Weight (MW) |
279.29 |
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Formula |
C17H13NO3
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CAS No. |
1048371-03-4 |
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Storage |
3 years -20℃Powder |
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6 months-80℃in DMSO |
Syonnyms |
N/A |
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Solubility (25°C) * |
In vitro |
DMSO |
56 mg/mL (200 mM) |
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Water |
<1 mg/mL (<1 mM) |
Ethanol |
<1 mg/mL (<1 mM) |
* <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)- |
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Stock Solution (1ml DMSO) |
1mM |
10mM |
20mM |
30mM |
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Mass(mg) |
0.27929 |
2.7929 |
5.5858 |
8.3787 |
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