PJ-34

Details

Stereochemistry	ACHIRAL
Molecular Formula	C17H17N3O2
Molecular Weight	295.3358
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CN(C)CC(=O)NC1=CC=C2NC(=O)C3=C(C=CC=C3)C2=C1

InChI

InChIKey=UYJZZVDLGDDTCL-UHFFFAOYSA-N

InChI=1S/C17H17N3O2/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)

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Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/11179503
Curator's Comment: description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/18695907 https://www.ncbi.nlm.nih.gov/pubmed/11845877

PJ34 is PARP inhibitor. It protects primary neuronal cells from oxygen-glucose deprivation in vitro and reduces infarct size following cerebral and cardiac ischemia in vivo. PJ34 exhibit suppresses cell growth and enhances the suppressive effects of cisplatin in liver cancer cells.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Poly [ADP-ribose] polymerase-2 2 Target ID: CHEMBL2794 Sources: https://www.ncbi.nlm.nih.gov/pubmed/15075382	Inhibitor 8297	86.0 nM [IC50]
Poly [ADP-ribose] polymerase-1 23 Target ID: CHEMBL3105 Sources: https://www.ncbi.nlm.nih.gov/pubmed/15075382	Inhibitor 8297	110.0 nM [IC50]
Poly [ADP-ribose] polymerase-1 23 Target ID: CHEMBL3105 Sources: https://www.ncbi.nlm.nih.gov/pubmed/16098744	Inhibitor 8297	110.0 nM [IC50]

Conditions

Condition	Modality	Highest Phase	Product
Hepatocellular carcinoma 83 Sources: https://www.ncbi.nlm.nih.gov/pubmed/18695907	Primary	Basic research	Unknown Approved Use Unknown
Myocardial infarction 121 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11845877	Preventing	Preclinical	Unknown Approved Use Unknown
Stroke 144 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11179503	Preventing	Preclinical	Unknown Approved Use Unknown

PubMed

Title	Date	PubMed
Protective effects of PJ34, a novel, potent inhibitor of poly(ADP-ribose) polymerase (PARP) in in vitro and in vivo models of stroke.	2001 Mar	11179503
Myocardial protection by PJ34, a novel potent poly (ADP-ribose) synthetase inhibitor.	2002 Feb	11845877

Patents

Sample Use Guides

In Vivo Use Guide

In mouse models of stroke PJ34 was administered intraperitoneally at 2.5 mg/kg 2 h before onset of ischemia and 6h later. In rat studies PJ34 was administered intravenously at 10 mg/kg i.v. bolus over 3 min.

Route of Administration: Other

In Vitro Use Guide

PJ34 was evaluated in vitro in the model of stroke. For oxygen-glucose deprivation (OGD) primary neuronal cultures of cerebral cortex were incubated in a balanced solution at pO2 < 2 mmHg. PJ34 was applied to cortical cell cultures 1 h before and during OGD. Neuronal injury was quantitatively assessed by the measurement of LDH at various time points in the medium. PJ34 at concentrations abobe 30 nM attenuates neuronal cell death in cortical cultures.

Name

Type

Language

PJ-34

Code

English

N,N-DIMETHYL-2-(6-OXO-5,6-DIHYDROPHENANTHRIDIN-2-YL)ACETAMIDE

Systematic Name

English

PJ34

Code

English

2-(DIMETHYLAMINO)-N-(6-OXO-5H-PHENANTHRIDIN-2-YL)ACETAMIDE

Systematic Name

English

ACETAMIDE, N-(5,6-DIHYDRO-6-OXO-2-PHENANTHRIDINYL)-2-(DIMETHYLAMINO)-

Systematic Name

English

N-(6-OXO-5,6-DIHYDROPHENANTHRIDIN-2-YL)-2-(N,N-DIMETHYLAMINO)ACETAMIDE

Systematic Name

English

Code System Code Type Description

CHEBI

167900