An inhibitor of PARP1 and 2 (EC50s = 10.2 and 36.3 μM

6(5H)-Phenanthridinone – 10 mg

Brand:
Cayman
CAS:
1015-89-0
Storage:
-20
UN-No:
Non-Hazardous - /

6(5H)-Phenanthridinone is an inhibitor of poly(ADP-ribose) polymerase 1 (PARP1) and PARP2 (EC50s = 10.2 and 36.3 μM, 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 μM.{53045} 6(5H)-Phenanthridinone reduces NF-κB-induced transcription of the genes encoding TNF-α, IL-2, and IFN-γ in rat lymphocytes.{53046} In vivo, 6(5H)-phenanthridinone (60 mg/kg) reduces spinal cord expression of inducible nitric oxide synthase (iNOS), IL-1β, TNF-α, IL-2, and IFN-γ 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}  

 

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SKU: 28730 - 10 mg Category:

Description

An inhibitor of PARP1 and 2 (EC50s = 10.2 and 36.3 μM, respectively, in yeast cells expressing the human enzymes); decreases radiation-induced PARP activity and proliferation of RDM4 murine lymphoma cells at 50 μM; reduces NF-κB-induced transcription of the genes encoding TNF-α, IL-2, and IFN-γ in rat lymphocytes; reduces spinal cord expression of iNOS, IL-1β, TNF-α, IL-2, and IFN-γ and reduces disease score in a rat model of EAE at 60 mg/kg; 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 at 10 mg/kg

Formal name:

Synonyms:  NSC 11021|NSC 40943|NSC 61083

Molecular weight: 195.2

CAS: 1015-89-0

Purity: ≥98%

Formulation: A solid

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