6(5H)-Phenanthridinone

6(5H)-Phenanthridinone is an inhibitor of poly(ADP-ribose) polymerase 1 (PARP1) and PARP2 (EC50s = 10.2 and 36.3 ?M, respectively, in yeast cells expressing the human enzymes).{53044} It decreases radiation-induced PARP activity and proliferation of RDM4 murine lymphoma cells when used at a concentration of 50 ?M.{53045} 6(5H)-Phenanthridinone reduces NF-kB-induced transcription of the genes encoding TNF-a, IL-2, and IFN-y in rat lymphocytes.{53046} In vivo, 6(5H)-phenanthridinone (60 mg/kg) reduces spinal cord expression of inducible nitric oxide synthase (iNOS), IL-1B, TNF-a, IL-2, and IFN-y and reduces disease score in a rat model of experimental autoimmune encephalomyelitis (EAE). It also decreases serum levels of lactate dehydrogenase as well as hepatic lipid peroxidation, oxidative DNA damage, and PARP levels in a mouse model of carbon tetrachloride-induced hepatotoxicity when administered at a dose of 10 mg/kg.{53047}