An inhibitor of poly(ADP-ribose) polymerases
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DPQ

Item No. 14450

Technical Information
Formal Name
3,4-dihydro-5-[4-(1-piperidinyl)butoxy]-1(2H)-isoquinolinone
CAS Number
129075-73-6
Synonyms
  • PARP Inhibitor III
Molecular Formula
C18H26N2O2
Formula Weight
Purity
≥99%
Formulation
A solid
SMILES
O=C1NCCC2=C(OCCCCN3CCCCC3)C=CC=C21
InChi Code
InChI=1S/C18H26N2O2/c21-18-16-7-6-8-17(15(16)9-10-19-18)22-14-5-4-13-20-11-2-1-3-12-20/h6-8H,1-5,9-14H2,(H,19,21)
InChi Key
RVOUDNBEIXGHJY-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    The poly(ADP-ribose) polymerases (PARPs) form a family of enzymes with roles in DNA repair and apoptosis, particularly in response to reactive oxygen and nitrogen species.1,2 DPQ is a potent inhibitor of PARPs, inhibiting PARP1 with an IC50 value of 40 nM.3 It is approximately 10-fold less potent against PARP2.4 DPQ can be used in either cells or in animals.5,6

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Davar, D., Beumer, J.H., Hamieh, L., et alRole of PARP inhibitors in cancer biology and therapy. Curr. Med. Chem. 19(23), 3907-3921 (2012).

    2. Mathews, M.T., and Berk, B.C. PARP-1 inhibition prevents oxidative and nitrosative stress-induced endothelial cell death via transactivation of the VEGF receptor 2. Arterioscler. Thromb. Vasc. Biol. 28, 711-717 (2008).

    3. Costantino, G., Macchiarulo, A., Camaioni, E., et alModeling of poly(ADP-ribose)polymerase (PARP) inhibitors. Docking of ligands and quantitative structure-activity relationships analysis. J. Med. Chem. 44, 3786-3794 (2001).

    4. Eltze, T., Boer, R., Wagner, T., et alImidazoquinolinone, imidazopyridine, and isoquinolindione derivatives as novel and potent inhibitors of the poly(ADP-ribose) polymerase (PARP): A comparison with standard PARP inhibitors. Mol. Pharmacol. 74(6), 1587-1598 (2008).

    5. Fonfria, E., Marshall, I.C.B., Benham, C.D., et alTRPM2 channel opening in response to oxidative stress is dependent on activation of poly(ADP-ribose) polymerase. Br. J. Pharmacol. 143, 186-192 (2004).

    6. Giovannelli, L., Cozzi, A., Guarnieri, I., et alComet assay as a novel approach for studying DNA damage in focal cerebral ischemia: Differential effects of NMDA receptor antagonists and poly(ADP-ribose) polymerase inhibitors. J. Cereb. Blood Flow Metab. 22(6), 697-704 (2002).