A selective PARP2 inhibitors
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UPF-1069

Item No. 17760

Technical Information
Formal Name
5-(2-oxo-2-phenylethoxy)-1(2H)-isoquinolinone
CAS Number
1048371-03-4
Synonyms
  • GKT237841
Molecular Formula
C17H13NO3
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 0.5 mg/mLDMSO: 0.5 mg/mLEthanol: 0.3 mg/mL
λmax
240, 280, 291, 330, 345 nm
SMILES
O=C1NC=CC2=C(OCC(C3=CC=CC=C3)=O)C=CC=C21
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)
InChi Key
JJWMRRNGWSITSQ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    Product Description

    UPF-1069 is a PARP inhibitor that demonstrates a modest preference for PARP2 over PARP1 (IC50s = 0.3 and 8 µM, respectively).1 In rat models of post-ischemic brain damage, it has been shown to increase cell death in hippocampal slice cultures in a model characterized by loss of neurons through a caspase-dependent, apoptosis-like process but to be protective of cortical neurons in a model characterized by a necrosis-like process.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Pellicciari, R., Camaioni, E., Costantino, G., et alOn the way to selective PARP-2 inhibitors. Design, synthesis, and preliminary evaluation of a series of isoquinolinone derivatives. Chem. Med. Chem. 3(6), 914-923 (2008).

    2. Moroni, F., Formentini, L., Gerace, E., et alSelective PARP-2 inhibitors increase apoptosis in hippocampal slices but protect cortical cells in models of post-ischaemic brain damage. Brit. J. Pharmacol. 157(5), 854-862 (2009).