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UPF 1069Selective PARP2 inhibitor

UPF 1069

Catalog No. A4163
Size Price Stock Qty
10mM (in 1mL DMSO) $99.00 In stock
10mg $90.00 In stock
50mg $290.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Quality Control & MSDS

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Chemical structure

UPF 1069

Biological Activity

UPF 1069 is a selective inhibitor of PARP2 with IC50 of 0.3 μM. It is ~27-fold selective against PARP1.
Targets PARP2          
IC50 0.3 μM          

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Chemical Properties

Cas No. 1048371-03-4 SDF Download SDF
Synonyms UPF-1069,UPF1069
Chemical Name 5-phenacyloxy-2H-isoquinolin-1-one
Canonical SMILES C1=CC=C(C=C1)C(=O)COC2=CC=CC3=C2C=CNC3=O
Formula C17H13NO3 M.Wt 279.29
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
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.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

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