WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H406128
CAS#: 344458-15-7 (HCl)
Description: 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.
Hodoodo Cat#: H406128
Name: PJ-34 HCl
CAS#: 344458-15-7 (HCl)
Chemical Formula: C17H18ClN3O2
Exact Mass: 0.00
Molecular Weight: 331.800
Elemental Analysis: C, 61.54; H, 5.47; Cl, 10.68; N, 12.66; O, 9.64
Related CAS #: 344458-15-7 (HCl) 344458-19-1 (free base),
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
InChi Key: RURAZZMDMNRXMI-UHFFFAOYSA-N
InChi Code: InChI=1S/C17H17N3O2.ClH/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);1H
SMILES Code: O=C(NC(C=C1C2=C3C=CC=C2)=CC=C1NC3=O)CN(C)C.[H]Cl
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).
HS Tariff Code: 2934.99.9001
More Info:
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 331.80 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
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.