DPQA highly potent, selective PARP inhibitor

DPQ (CAS 129075-73-6)

DPQ | CAS 129075-73-6 is rated 5.0 out of 5 by 1.
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Synonym: 3,4-Dihydro-5[4-(1-piperindinyl)but; PARP Inhibitor III, oxy]-1(2H)-isoquinoline
Application: A highly potent, selective PARP inhibitor
CAS Number: 129075-73-6
Purity: ≥98%
Molecular Weight: 302.41
Molecular Formula: C18H26N2O2
* Refer to Certificate of Analysis for lot specific data (including water content).
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PARP inhibitor III (DPQ) is a highly potent and selective inhibitor of PARP (Poly ADP-ribose polymerase) (IC50 = 40 nM). The PARP family is comprised of 17 nuclear enzymes involved in a myriad of cellular functions such as apoptosis, DNA repair, telometric maintenance and post-translational modification. DNA damage from oxidative and nitrosative stress can activate PARP, which catalyzes teh attachment of ADP ribose units from NAD to nuclear proteins. PARP also plays an important role in activating inflammatory genes, which can serve as a useful research topic for various cardiovascular and inflammatory diseases. Research shows that rapid activation of the enzyme depletes intracellular concentrations of NAD, thus slowing the rate of glycolysis, electron transport and subsequently ATP formation, resulting in cellular dysfunction and death. PARP Inhibitor III, DPQ is an inhibitor of PARP-1 and PARP-2.


References

1. Suto, M.J., et al. 1991. Anticancer Drug Des. 6: 107-117. PMID: 1903948
2. Eliasson, M.J., et al. 1997. Nat. Med. 3: 1089-1095. PMID: 9334719
3. Szabó, C., et al. 1998. Trends Pharmacol. Sci. 19: 287-298. PMID: 9703762
4. Moroni, F., et al. 2001. Cell Death Differ. 8: 921-932. PMID: 11526447
5. Giovannelli, L., et al. 2002. J. Cereb. Blood Flow Metab. 22: 697-704. PMID: 12045668
6. Graziani, G. and Szabó, C. 2005. Pharmacol. Res. 52: 109-118. PMID: 15911339
7. Espinoza, L.A., et al. 2007. Free Radic. Biol. Med. 42: 1430-1440. PMID: 17395016

Physical State :
solid
Solubility :
Soluble in DMSO (5 mg/ml), and ethanol (slightly). Insoluble in water.
Storage :
Store at -20° C
Melting Point :
196.74° C (Predicted)
Boiling Point :
528.80° C at 760 mmHg (Predicted)
Density :
1.10 g/cm3 (Predicted)
Refractive Index :
n20D 1.54 (Predicted)
IC50 :
ADP-ribosyltransferase: IC50 = 40 nM (Mus musculus); Poly [ADP-ribose] polymerase-1: IC50 = 40 nM (Mus musculus); Poly [ADP-ribose] polymerase-2: IC50 = 40 nM (Mus musculus)
pK Values :
pKb: 9.63
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
9948349
Merck Index :
14: 3442
MDL Number :
MFCD01866274
SMILES :
C1CCN(CC1)CCCCOC2=CC=CC3=C2CCNC3=O

Download SDS (MSDS)

Certificate of Analysis

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DPQ  Product Citations

See how others have used DPQ. Click on the entry to view the PubMed entry .

Citations 1 to 10 of 12 total

PMID: # 27757983  Wei, SJ. et al. 2017. Clin. Exp. Pharmacol. Physiol. 44: 114-122.

PMID: # 29107864  Aminzadeh, M. et al. 2017. International immunopharmacology. 54: 78-85.

PMID: # 27731349  Tseng, HH. et al. 2016. Sci Rep. 6: 35016.

PMID: # 26443841  Xu, H. et al. 2016. Toxicol. Sci. 149: 31-41.

PMID: # 26331430  Zhang, GH. et al. 2015. Clin. Exp. Pharmacol. Physiol. 42: 1266-74.

PMID: # 25329809  Lechaftois, M. et al. 2014. PloS one. 9: e110776.

PMID: # 24278171  Wang, G. et al. 2013. PloS one. 8: e79757.

PMID: # 23974709  Lee, Y. et al. 2013. Nature neuroscience. 16: 1392-400.

PMID: # 23038248  King, BS. et al. 2012. The Journal of biological chemistry. 287: 39824-33.

PMID: # 21458523  Liu, FQ. et al. 2011. Mol. Cell. Endocrinol. 339: 25-33.

Citations 1 to 10 of 12 total
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Rated 5 out of 5 by from Wang et al Wang et al. (PubMed ID 25412407) found that DPQ, a PARP-1 inhibitor, improved heart function in rats by reducing myocardial infarction-induced apoptosis and inflammation. -SCBT Publication Review
Date published: 2015-02-03
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