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| 10mg |
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| 25mg |
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UPF 1069 (UPF-1069), an isoquinolinone derivative, is a novel, potent and selective inhibitor of poly-(ADP-ribose) polymerase 2 (PARP-2) with potential neurprotective and anti-ischemic effects in vivo. It inhibits PARP-2, with IC50 values for PARP-1 and PARP-2 of 8 and 0.3 μM, respectively. It can decrease PAR formation and cause apoptosis in nuclear extracts from PARP-1-/-fibroblasts as well as in recombinant enzyme preparations. With an IC50 of 8 μmol/L, UPF 1069 exhibits greater selectivity for PARP-2 compared to PARP-1. It has been applied to study the function of PARP-1 and PARP-2 in brain damage following an ischemia.
| Targets |
PARP-2 ( IC50 = 0.3 μM ); PARP-1 ( IC50 = 8 μM )
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| ln Vivo |
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| Enzyme Assay |
Recombinant mouse PARP-2 and bovine PARP-1, which are readily available for purchase, are used to measure PARP activity. The enzymatic reaction is conducted in 100 µL of 50 mM Tris-HCl (pH 8.0) supplemented with 5 mM MgCl22, 2 mM dithiothreitol, 10 µg of 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). That is, in brief. The mixture is mixed and incubated at 37°C for one hour at varying concentrations of the potential inhibitors. After adding 1 mL of 10% trichloroacetic acid (w/v) to stop the reaction, the mixture is centrifuged. Following two washings in 1 mL of H2O, the pellets are resuspended in 1 mL of 0.1 M NaOH. Liquid scintillation spectrometry is used to measure the radioactivity incorporated from [adenine-2,8-3H]NAD into proteins[2].
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| References |
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| Molecular Formula |
C17H13NO3
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| Molecular Weight |
279.29
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| Exact Mass |
279.09
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| Elemental Analysis |
C, 73.11; H, 4.69; N, 5.02; O, 17.19
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| CAS # |
1048371-03-4
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| Related CAS # |
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| Appearance |
White to off-white solid powder
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| SMILES |
C1=CC=C(C=C1)C(=O)COC2=CC=CC3=C2C=CNC3=O
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| InChi Key |
JJWMRRNGWSITSQ-UHFFFAOYSA-N
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| 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)
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| Chemical Name |
5-phenacyloxy-2H-isoquinolin-1-one
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| Synonyms |
UPF 1069; UPF1069; UPF-1069
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.95 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.95 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 2% DMSO+30% PEG 300+5% Tween 80+ddH2O: 5mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5805 mL | 17.9025 mL | 35.8051 mL | |
| 5 mM | 0.7161 mL | 3.5805 mL | 7.1610 mL | |
| 10 mM | 0.3581 mL | 1.7903 mL | 3.5805 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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