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
SMILES
CN(C)CC(=O)NC1=CC2=C(NC(=O)C3=C2C=CC=C3)C=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)
| Molecular Formula | C17H17N3O2 |
| Molecular Weight | 295.3358 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/11179503Curator'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
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
Sources: https://www.ncbi.nlm.nih.gov/pubmed/11179503
Curator's Comment: Known to be CNS active (reduces infarction size) in mice and rats. Human data not available.
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL2794 Sources: https://www.ncbi.nlm.nih.gov/pubmed/15075382 |
86.0 nM [IC50] | ||
Target ID: CHEMBL3105 Sources: https://www.ncbi.nlm.nih.gov/pubmed/15075382 |
110.0 nM [IC50] | ||
Target ID: CHEMBL3105 Sources: https://www.ncbi.nlm.nih.gov/pubmed/16098744 |
110.0 nM [IC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | Unknown Approved UseUnknown |
|||
| Preventing | Unknown Approved UseUnknown |
|||
| Preventing | Unknown Approved UseUnknown |
PubMed
| Title | Date | PubMed |
|---|---|---|
| PJ34, an inhibitor of PARP-1, suppresses cell growth and enhances the suppressive effects of cisplatin in liver cancer cells. | 2008-09 |
|
| 4-Phenyl-1,2,3,6-tetrahydropyridine, an excellent fragment to improve the potency of PARP-1 inhibitors. | 2005-10-01 |
|
| Myocardial protection by PJ34, a novel potent poly (ADP-ribose) synthetase inhibitor. | 2002-02 |
|
| Protective effects of PJ34, a novel, potent inhibitor of poly(ADP-ribose) polymerase (PARP) in in vitro and in vivo models of stroke. | 2001-03 |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/11179503
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
Sources: https://www.ncbi.nlm.nih.gov/pubmed/16098744
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.
| Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 22:50:02 GMT 2025
by
admin
on
Mon Mar 31 22:50:02 GMT 2025
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| Record UNII |
NA92ZAR7N2
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| Record Status |
Validated (UNII)
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| Record Version |
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344458-19-1
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NA92ZAR7N2
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356042-41-6
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SUPERSEDED |
| Related Record | Type | Details | ||
|---|---|---|---|---|
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SALT/SOLVATE -> PARENT |
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| Related Record | Type | Details | ||
|---|---|---|---|---|
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ACTIVE MOIETY |