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PJ34 (Synonyms: PJ-34;PJ 34)

Catalog No.GC10995

An inhibitor of poly (ADP-ribose) polymerases

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PJ34 Chemical Structure

Cas No.: 344458-19-1

Size Price Stock Qty
5mg
$35.00
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10mg
$46.00
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50mg
$125.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment [1]:

Cell lines

Mouse endothelial cells and human umbilical vein endothelial cells

Preparation method

The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

0.1 ~ 3 μM

Applications

In mouse endothelial cells, PJ34 significantly inhibited high glucose-induced PARP activation at the doses of 0.5 and 3 μM, as well as the development of endothelial dysfunction at the dose of 3 μM. Meanwhile, PARP inhibition caused by PJ34 (3 μM) did not alter the degree of NF-κB activation. In human umbilical vein endothelial cells, PJ34 at 1 μM exhibited marked inhibitory effect on high glucose-induced PARP activation.

Animal experiment [2]:

Animal models

MBP-immunized PLSJL mice

Dosage form

10 mg/kg; p.o.; b.i.d.

Applications

In MBP-immunized PLSJL mice, PJ34 inhibited the development of clinical signs of experimental allergic encephalomyelitis (EAE). PJ34 also suppressed the onset of EAE by reducing CNS inflammation and maintaining neurovascular integrity. In addition, PJ34 down-regulated the expression levels of TNF-α and ICAM-1 in the spinal cord tissues.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Garcia Soriano F, Virág L, Jagtap P, Szabó E, Mabley JG, Liaudet L, Marton A, Hoyt DG, Murthy KG, Salzman AL, Southan GJ, Szabó C. Diabetic endothelial dysfunction: the role of poly(ADP-ribose) polymerase activation. Nat Med. 2001 Jan;7(1):108-13.

[2]. Scott GS, Kean RB, Mikheeva T, Fabis MJ, Mabley JG, Szabó C, Hooper DC. 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.

Background

IC50 Value: 20 nM(EC50)[1] PJ34 (hydrochloride) is a novel potent specific inhibitor of PARP-l. PJ34 has been reported to enhance chemotherapeutic effects in certain types of tumors. in vitro: PJ34 inhibited peroxynitrite-induced cell necrosis with EC50 of 20 nM. PJ34 provides cardioprotection by decreasing myocardial infarct size and enhancing postischemic regional and global functional recovery [1]. Treatment with PJ34 increased NIS promoter activity without affecting PARP-1 binding to the promoter sequence, in addition to an increase of histone modification activation marks (H3K9K14ac, H3K4me3) [2]. in vivo: In a model of systemic endotoxemia, PJ34 pretreatment significantly reduced plasma levels of TNF-alpha, IL-1beta and nitrite/nitrate (breakdown products of nitric oxide) production. PJ34 treatment (oral gavage) induced a significant suppression of the inflammatory response in dextran sulfate colitis, multiple low dose streptozotocin diabetes [3]. The PJ34 showed significant reduction on infarct size (37.5%+/-4.5% and 50.5%+/-4.8% of the area at risk) for PJ34 and control pigs groups, respectively, (p < 0.05) [4]. Clinical trial: N/A

Chemical Properties

Cas No. 344458-19-1 SDF
Synonyms PJ-34;PJ 34
Chemical Name 2-(dimethylamino)-N-(6-oxo-5H-phenanthridin-2-yl)acetamide
Canonical SMILES CN(C)CC(=O)NC1=CC2=C(C=C1)NC(=O)C3=CC=CC=C32
Formula C17H17N3O2 M.Wt 295.34
Solubility Soluble in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 3.3859 mL 16.9296 mL 33.8593 mL
5 mM 0.6772 mL 3.3859 mL 6.7719 mL
10 mM 0.3386 mL 1.693 mL 3.3859 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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