An inhibitor of poly (ADP-ribose) polymerases
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PJ-34

Item No. 14440

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(5,6-dihydro-6-oxo-2-phenanthridinyl)-2-(dimethylamino)-acetamide
CAS Number
344458-19-1
Molecular Formula
C17H17N3O2
Formula Weight
295.3
Purity
≥95%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 1 mg/mlPBS (pH 7.2): 10 mg/ml
λmax
240, 251, 258, 336 nm
SMILES
O=C(CN(C)C)NC(C=C1)=CC(C2=CC=CC=C23)=C1NC3=O
InChi Code
InChI=1S/C17H17N3O2/c1-20(2)10-16(21)18-11-7-8-15-14(9-11)12-5-3-4-6-13(12)17(22)19-15/h3-9H,10H2,1-2H3,(H,18,21)(H,19,22)
InChi Key
UYJZZVDLGDDTCL-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $41

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    5 mg

    $80

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    10 mg

    $119

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    25 mg

    $186

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    Product Description

    PJ-34 is an inhibitor of PARPs which can be used in cells or in animals.1,2,3 It binds and inhibits the PARP tankyrase1 (IC50 = 1 μM).4 PJ-34 also inhibits matrix metalloproteinase-2 when used at higher concentrations (IC50 = 56 μM).5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Soriano, F.G., Pacher, P., Mabley, J., et al. Rapid reversal of the diabetic endothelial dysfunction by pharmacological inhibition of poly(ADP-ribose) polymerase. Circ. Res. 89(8), 684-691 (2001).

    2. Fonfria, E., Marshall, I.C.B., Benham, C.D., et al. TRPM2 channel opening in response to oxidative stress is dependent on activation of poly(ADP-ribose) polymerase. Br. J. Pharmacol. 143, 186-192 (2004).

    3. Radnai, B., Antus, C., Racz, B., et al. Protective effect of the poly(ADP-ribose) polymerase inhibitor PJ34 on mitochondrial depolarization-mediated cell death in hepatocellular carcinoma cells involves attenuation of c-Jun N-terminal kinase-2 and protein kinase B/Akt activation. Mol. Cancer 11(34), (2012).

    4. Kirby, C.A., Cheung, A., Fazal, A., et al. Structure of human tankyrase 1 in complex with small-molecule inhibitors PJ34 and XAV939. Acta Crystallogr. Sect. F Struct. Biol. Cryst. Commun. 68 (Pt 2), 115-118 (2012).

    5. Nicolescu, A.C., Holt, A., Kandasamy, A.D., et al. Inhibition of matrix metalloproteinase-2 by PARP inhibitors. Biochem. Biophys. Res. Commun. 387(4), 646-650 (2009).