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MedKoo Biosciences/PJ-34 HCl/406128/200mg

作者: 时间:2024-11-10 点击量:

PJ-34 is a novel and potent PARP-1 inhibitor with potential anticancer activity. PJ34 has a high affinity for PARP-1 (IC(50) = 20 nM). PJ-34 inhibits PARP-1 expression and ERK phosphorylation in glioma-conditioned brain microvascular endothelial cells. PJ-34 reduces mesenteric vascular injury induced by experimental cardiopulmonary bypass with cardiac arrest. PJ-34 reduce cell inflammation and damage that follow PARP-1 overexpression. PJ-34 negatively modulate proinflammatory commitment of human glioblastoma cells.

MedKoo Cat#: 406128 Name: PJ-34 HCl CAS#: 344458-15-7 (HCl); 344458-19-1 (free base). Chemical Formula: C17H18ClN3O2 Exact Mass: Molecular Weight: 331.8 Elemental Analysis: C, 61.54; H, 5.47; Cl, 10.68; N, 12.66; O, 9.64

Synonym: PJ34; PJ-34; PJ 34; PJ-34 HCl; PJ-34 hydrochloride.

IUPAC/Chemical Name: 2-(dimethylamino)-N-(6-oxo-5,6-dihydrophenanthridin-2-yl)acetamide hydrochloride

SMILES Code: O=C(NC(C=C1C2=C3C=CC=C2)=CC=C1NC3=O)CN(C)C.[H]Cl

Technical Data

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: soluble in DMSO, soluble in dilute HCl, soluble in water.

Shelf Life: >5 years if stored properly

Drug Formulation: This drug may be formulated in DMSO or water

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code: 293490

Additional Information

        

References

1: Motta C, D\'Angeli F, Scalia M, Satriano C, Barbagallo D, Naletova I, Anfuso CD, Lupo G, Spina-Purrello V. PJ-34 inhibits PARP-1 expression and ERK phosphorylation in glioma-conditioned brain microvascular endothelial cells. Eur J Pharmacol. 2015 Aug 15;761:55-64. doi: 10.1016/j.ejphar.2015.04.026. Epub 2015 Apr 28. PubMed PMID: 25934569.

2: Scalia M, Satriano C, Greca R, Stella AM, Rizzarelli E, Spina-Purrello V. PARP-1 inhibitors DPQ and PJ-34 negatively modulate proinflammatory commitment of human glioblastoma cells. Neurochem Res. 2013 Jan;38(1):50-8. doi: 10.1007/s11064-012-0887-x. Epub 2012 Sep 26. PubMed PMID: 23011206.

3: Nasrabady SE, Kuzhandaivel A, Akrami A, Bianchetti E, Milanese M, Bonanno G, Nistri A. Unusual increase in lumbar network excitability of the rat spinal cord evoked by the PARP-1 inhibitor PJ-34 through inhibition of glutamate uptake. Neuropharmacology. 2012 Sep;63(3):415-26. doi: 10.1016/j.neuropharm.2012.04.014. Epub 2012 Apr 28. PubMed PMID: 22561282.

4: Nasrabady SE, Kuzhandaivel A, Nistri A. Studies of locomotor network neuroprotection by the selective poly(ADP-ribose) polymerase-1 inhibitor PJ-34 against excitotoxic injury to the rat spinal cord in vitro. Eur J Neurosci. 2011 Jun;33(12):2216-27. doi: 10.1111/j.1460-9568.2011.07714.x. Epub 2011 May 30. PubMed PMID: 21623955.

5: Mazzone GL, Nistri A. Effect of the PARP-1 inhibitor PJ 34 on excitotoxic damage evoked by kainate on rat spinal cord organotypic slices. Cell Mol Neurobiol. 2011 Apr;31(3):469-78. doi: 10.1007/s10571-010-9640-7. Epub 2010 Dec 29. PubMed PMID: 21190076.

6: Chevanne M, Zampieri M, Caldini R, Rizzo A, Ciccarone F, Catizone A, D\'Angelo C, Guastafierro T, Biroccio A, Reale A, Zupi G, Caiafa P. Inhibition of PARP activity by PJ-34 leads to growth impairment and cell death associated with aberrant mitotic pattern and nucleolar actin accumulation in M14 melanoma cell line. J Cell Physiol. 2010 Feb;222(2):401-10. doi: 10.1002/jcp.21964. PubMed PMID: 19890834.

7: Huang FC. Upregulation of Salmonella-induced IL-6 production in Caco-2 cells by PJ-34, PARP-1 inhibitor: involvement of PI3K, p38 MAPK, ERK, JNK, and NF-kappaB. Mediators Inflamm. 2009;2009:103890. doi: 10.1155/2009/103890. Epub 2010 Feb 24. PubMed PMID: 20204057; PubMed Central PMCID: PMC2828125.

8: Pyriochou A, Olah G, Deitch EA, Szabó C, Papapetropoulos A. Inhibition of angiogenesis by the poly(ADP-ribose) polymerase inhibitor PJ-34. Int J Mol Med. 2008 Jul;22(1):113-8. PubMed PMID: 18575783.

9: Szijártó A, Batmunkh E, Hahn O, Mihály Z, Kreiss A, Kiss A, Lotz G, Schaff Z, Váli L, Blázovics A, Geró D, Szabó C, Kupcsulik P. Effect of PJ-34 PARP-inhibitor on rat liver microcirculation and antioxidant status. J Surg Res. 2007 Sep;142(1):72-80. Epub 2007 Jul 5. PubMed PMID: 17612561.

10: Andrási TB, Blázovics A, Szabó G, Vahl CF, Hagl S. Poly(ADP-ribose) polymerase inhibitor PJ-34 reduces mesenteric vascular injury induced by experimental cardiopulmonary bypass with cardiac arrest. Am J Physiol Heart Circ Physiol. 2005 Jun;288(6):H2972-8. Epub 2005 Jan 28. PubMed PMID: 15681711.

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