PJ34 Hydrochloride

Product ID P3600

Cas No. 344458-15-7

Purity ≥95%

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Product Info
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Description
Product Info
Shipping and Storage
Downloads
References
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Description

PJ34 is a phenanthridinone derivative that acts as a competitive poly(ADP)-ribose polymerase (PARP) inhibitor. PJ34 exhibits cardioprotective, neuroprotective, anticancer, and anti-diabetic activities. In in vitro and in vivo models of oxygen glucose deprivation, PJ34 protects against stroke-related ischemic brain injury. This compound is also cardioprotective against myocardial infarction, decreasing infarct size and postsystolic shortening. In diabetic NOD mice, PJ34 decreased insulitis, beta-cell destruction, and diabetes incidence by decreasing islet IFN-γ expression and inducing apoptosis in islet-infiltrating leukocytes. In mouse models of allergic encephalitis, PJ34 exhibits protective benefit by shifting the immune response from a pro-inflammatory Th1-mediated response to an anti-inflammatory Th2-mediated response. Additionally, in a variety of cancer cell lines, PJ34 induces G2/M phase mitotic arrest and caspase-depedent apoptosis, potentially due to direct antagonism of Pim-1 kinase.

Product Info

Cas No.	344458-15-7
Purity	≥95%
Formula	C₁₇H₁₇N₃O₂ • HCl
Formula Wt.	331.80
IUPAC Name	2-(dimethylamino)-N-(6-oxo-5H-phenanthridin-2-yl)acetamide;hydrochloride
Solubility	DMSO 66 mg/mL (198.91 mM) Water 66 mg/mL (198.91 mM) Ethanol Insoluble
Appearance	Light grey to light brown

Shipping and Storage

Store Temp	-20°C
Ship Temp	Ambient

Downloads

MSDS	P3600 MSDS PDF
Info Sheet	P3600 Info Sheet PDF
Brochures	PARP Inhibitors Flyer

References

Antolín AA, Jalencas X, Yélamos J, et al. Identification of pim kinases as novel targets for PJ34 with confounding effects in PARP biology. ACS Chem Biol. 2012 Dec 21;7(12):1962-7. PMID: 23025350.

Gangopadhyay NN, Luketich JD, Opest A, et al. Inhibition of poly(ADP-ribose) polymerase (PARP) induces apoptosis in lung cancer cell lines. Cancer Invest. 2011 Nov;29(9):608-16. PMID: 22011283.

Madison DL, Stauffer D, Lundblad JR. The PARP inhibitor PJ34 causes a PARP1-independent, p21 dependent mitotic arrest. DNA Repair (Amst). 2011 Oct 10;10(10):1003-13. PMID: 21840268.

Scott GS, Kean RB, Mikheeva T, et al. The therapeutic effects of PJ34 [N-(6-oxo-5,6-dihydrophenanthridin-2-yl)-N,N-dimethylacetamide.HCl], a selective inhibitor of poly(ADP-ribose) polymerase, in experimental allergic encephalomyelitis are associated with immunomodulation. J Pharmacol Exp Ther. 2004 Sep;310(3):1053-61. PMID: 15159442.

Suarez-Pinzon WL, Mabley JG, Power R, et al. Poly (ADP-ribose) polymerase inhibition prevents spontaneous and recurrent autoimmune diabetes in NOD mice by inducing apoptosis of islet-infiltrating leukocytes. Diabetes. 2003 Jul;52(7):1683-8. PMID: 12829633.

Faro R, Toyoda Y, McCully JD, et al. Myocardial protection by PJ34, a novel potent poly (ADP-ribose) synthetase inhibitor. Ann Thorac Surg. 2002 Feb;73(2):575-81. PMID: 11845877.

Abdelkarim GE, Gertz K, Harms C, et al. Protective effects of PJ34, a novel, potent inhibitor of poly(ADP-ribose) polymerase (PARP) in in vitro and in vivo models of stroke. Int J Mol Med. 2001 Mar;7(3):255-60. PMID: 11179503.