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6(5H)-Phenanthridinone (Synonyms: NSC 11021, NSC 40943, NSC 61083)

Katalog-Nr.GC45772

An inhibitor of PARP1 and 2

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6(5H)-Phenanthridinone Chemische Struktur

Cas No.: 1015-89-0

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1mg
47,00 $
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5mg
168,00 $
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10mg
312,00 $
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25mg
720,00 $
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

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).1 It decreases radiation-induced PARP activity and proliferation of RDM4 murine lymphoma cells when used at a concentration of 50 μM.2 6(5H)-Phenanthridinone reduces NF-κB-induced transcription of the genes encoding TNF-α, IL-2, and IFN-γ in rat lymphocytes.3 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.4

|1. Perkins, E., Sun, D., Nguyen, A., et al. Novel inhibitors of poly(ADP-ribose) polymerase/PARP1 and PARP2 identified using a cell-based screen in yeast. Cancer Res. 61(10), 4175-4183 (2001).|2. Weltin, D., Holl, V., Hyun, J.W., et al. Effect of 6(5H)-phenanthridinone, a poly (ADP-ribose)polymerase inhibitor, and ionizing radiation on the growth of cultured lymphoma cells. Int. J. Radiat. Biol. 72(6), 685-692 (1997).|3. Chiarugi, A. Inhibitors of poly(ADP-ribose) polymerase-1 suppress transcriptional activation in lymphocytes and ameliorate autoimmune encephalomyelitis in rats. Br. J. Pharmacol. 137(6), 761-770 (2002).|4. Banasik, M., Stedeford, T., Strosznajder, R.P., et al. Inhibition of poly(ADP-ribose) polymerase-1 attenuates the toxicity of carbon tetrachloride. J. Enzyme Inhib. Med. Chem. 26(6), 883-889 (2011).

Chemical Properties

Cas No. 1015-89-0 SDF
Überlieferungen NSC 11021, NSC 40943, NSC 61083
Canonical SMILES O=C1C2=C(C=CC=C2)C3=CC=CC=C3N1
Formula C13H9NO M.Wt 195.2
Löslichkeit DMF: 1mg/mL,DMF:PBS (pH 7.2) (1:5): 0.16mg/mL Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 5.123 mL 25.6148 mL 51.2295 mL
5 mM 1.0246 mL 5.123 mL 10.2459 mL
10 mM 0.5123 mL 2.5615 mL 5.123 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 29 reference(s) in Google Scholar.)

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