Home DNA Damage/DNA Repair PARP inhibitor PJ34 HCl For research use only.

PJ34 HCl

PJ34 HCl is the hydrochloride salt of PJ34, which is a PARP inhibitor with EC50 of 20 nM and is equally potent to PARP1/2.

PJ34 HCl Chemical Structure

PJ34 HCl Chemical Structure

CAS No. 344458-15-7

Purity & Quality Control

PJ34 HCl Related Products

Signaling Pathway

PARP Signaling Pathways

PARP Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Escherichia coli BL21(DE3) cells Function assay 10 uM Inhibition of human coronavirus OC43 nucleocapsid protein expressed in Escherichia coli BL21(DE3) assessed as reduction of RNA-binding capacity by measuring resonance unit at 10 uM by surface plasmon resonance analysis relative to control 24564608
HeLa Function assay Inhibition of PARP1 in human HeLa cells by fluid scintillation counting using [adenylated-32P]NAD as substrate, IC50=0.02μM. 18713665
Escherichia coli Rosetta2 (DE3) Function assay Inhibition of human N-terminal 6xhis-tagged ARTD6 (873 to 1161) expressed in Escherichia coli Rosetta2 (DE3) cells using NAD+ as substrate by fluorescence assay, IC50=0.21878μM. 24900770
Escherichia coli Rosetta2 (DE3) Function assay Inhibition of human N-terminal 6xhis-tagged ARTD6 (873 to 1161) expressed in Escherichia coli Rosetta2 (DE3) cells using NAD+ as substrate by fluorescence assay, IC50=0.219μM. 24900770
Escherichia coli BL21 Star (DE3) Function assay Inhibition of 6xhis-tagged ARTD5 (unknown origin) expressed in Escherichia coli BL21 Star (DE3) cells, IC50=0.57μM. 24900770
Escherichia coli Rosetta2 (DE3) Function assay Inhibition of human 6xhis-tagged ARTD5 (1030 to 1317) expressed in Escherichia coli Rosetta2 (DE3) cells using NAD+ as substrate by fluorescence assay, IC50=1.3μM. 24900770
Escherichia coli Rosetta2 (DE3) Function assay Inhibition of human 6xhis-tagged ARTD5 (1030 to 1317) expressed in Escherichia coli Rosetta2 (DE3) cells using NAD+ as substrate by fluorescence assay, IC50=1.34896μM. 24900770
MEF Antiproliferative assay 72 hrs Antiproliferative activity against MEF cells harboring Brca1 deletion mutant at exon 11 assessed as cell viability after 72 hrs by MTT assay, IC50=13.2μM. 22365563
MEF Antiproliferative assay 72 hrs Antiproliferative activity against wild type MEF cells assessed as cell viability after 72 hrs by MTT assay, IC50=19.8μM. 22365563
Click to View More Cell Line Experimental Data

Biological Activity

Description PJ34 HCl is the hydrochloride salt of PJ34, which is a PARP inhibitor with EC50 of 20 nM and is equally potent to PARP1/2.
Features Water-soluble PARP1/2 inhibitor with >10,000-fold potentcy vs. 3-aminobenzamide (prototypical PARP inhibitor). Potential uses in cardiovascular diseases (stroke, cerebral ischemia, & myocardial ischemia).
Targets
PARP [1]
(Cell-free assay)
20 nM(EC50)
In vitro
In vitro

PJ34 is a potent, phenanthridinone PARS inhibitor, which is approximately 10,000 times more potent than the prototypical PARS inhibitor 3-aminobenzamide. 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]
Experimental Result Images Methods Biomarkers Images PMID
Western blot p53 / pS15-p53 / pChk1 / pChk2 21840268
Immunofluorescence p-p53 / p53 28095779
In Vivo
In vivo

PJ34 suppresses the development of clinical signs of EAE in MBP-immunized PLSJL mice. PJ34 exerted therapeutic effects at the onset of EAE that are associated with reduced CNS inflammation and the maintenance of neurovascular integrity. PJ34 partially inhibits the expression of TNF-α and ICAM-1 in the Spinal Cord Tissues of MBP-Immunized Mice.[2] PJ34 provides significant, dose-dependent, anti-inflammatory effects in a variety of local inflammation models. PJ34 dose-dependently suppresses neutrophil infiltration and nitric oxide (but not KC and IL-1β) production in peritonitis. In a model of systemic endotoxemia, PJ34 pretreatment significantly reduces plasma levels of TNF-α, IL-1β and nitrite/nitrate (breakdown products of nitric oxide) production. 
Animal Research Animal Models Female PLSJL mice
Dosages 10 mg/kg b.wt. twice daily
Administration orally

Chemical Information & Solubility

Molecular Weight 331.8 Formula

C17H17N3O2.HCl
CAS No. 344458-15-7 SDF --
Smiles CN(C)CC(=O)NC1=CC2=C(C=C1)NC(=O)C3=CC=CC=C32.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 66 mg/mL ( (198.91 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 66 mg/mL

Ethanol : Insoluble


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In vivo
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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.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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