Drug intelligence / Profile preview

pj34

Development stage
Unknown
Modality
Small Molecules
01

Overview

PJ34 is a small molecule inhibitor belonging to the phenanthridine class. It acts as a potent inhibitor of poly(ADP-ribose) polymerases PARP1 and PARP2 (IC50 values of 110 nM and 86 nM, respectively). By inhibiting these enzymes—key mediators in DNA repair—PJ34 exhibits antineoplastic (anti-cancer), cardioprotective, neuroprotective, anti-inflammatory, antiatherosclerotic, apoptosis-inducing and angiogenesis-inhibiting properties. Its primary mechanism involves blocking NAD(+)-dependent ADP-ribosylation catalyzed by PARPs. PJ34 has been studied for its potential in cancer therapy as well as for protection against ischemic injury and neurodegeneration[1][3][4].

Other names
N~2~,N~2~-dimethyl-N~1~-(6-oxo-5,6-dihydrophenanthridin-2-yl)glycinamide2-(dimethylamino)-N-(6-oxo-5H-phenanthridin-2-yl)acetamideN(2),N(2)-dimethyl-N-(6-oxo-5,6-dihydrophenanthridin-2-yl)glycinamideN-(5,6-Dihydro-6‑oxo‑2‑phenanthridinyl)-2-(dimethylamino)-acetamideN-(5,6-dihydro‑6‑oxophenanthridine‑2‑yl)-2-(dimethylamino)acetamide
02

Targets

PARP1 (Poly (adp-ribose) polymerase 1)PARP2 (Poly (adp-ribose) polymerase 2)PARP3 (Poly(adp-ribose) polymerase 3)TNKS (Poly(ADP-ribose) Polymerase 5a)

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