6(5H)-Phenanthridinone (Synonyms: NSC 11021, NSC 40943, NSC 61083) |
| カタログ番号GC45772 |
PARP1および2の阻害剤
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1015-89-0
Sample solution is provided at 25 µL, 10mM.
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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).
| Cas No. | 1015-89-0 | SDF | |
| 同義語 | NSC 11021, NSC 40943, NSC 61083 | ||
| Canonical SMILES | O=C1C2=C(C=CC=C2)C3=CC=CC=C3N1 | ||
| Formula | C13H9NO | M.Wt | 195.2 |
| 溶解度 | 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| 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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 29 reference(s) in Google Scholar.)
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