PNMT-IN-1
PNMT-IN-1 (inhibtor 4) is a specific inhibitor of phenylethanolamine N-methyltransferas (PNMT) with a Ki value of 1.2 nM and a IC50 value of 81 nM. PNMT-IN-1 also inhibits the vitality of DNMT1 and DNMT3b, with the IC50 value of 61 μM and 17 μM, respectively, and has an antagonistic effect on epinephrine.PNMT-IN-1 (inhibtor 4 ) is a second generation inhibitor.
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- Formule: C27H36Cl2N8O5
- Masse moléculaire:623.53
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
Description
IC50 & Target
IC50:81 nM (Phenylethanolamine N-methyltransferase, PNMT )[1] IC50:61 nM (DNMT1)[1] IC50:17 nM (DNMT3b)[1]
In Vitro
PNMT-IN-1(inhibtor 4)(0.01 μM, 4h) inhibts the activity of hPNMT (IC50= 81 nM) but don’t affect protein methylation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:Overexpressed hPNMT in HEK293T cells using a lentiviral vector[1]
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Concentration:0-10 μM
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Incubation Time:24 h
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Result:Inhibted the activity of hPNMT (IC50=81nM)
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Cell Line:HT-29 cell[1]
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Concentration:10 μg
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Incubation Time:6 days
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Result:Changed total SDMA, ADMA, and Me3-lysine not significant.
Chemical Information
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Masse moléculaire 623.53
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Formule C27H36Cl2N8O5
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SMILES
ClC1=C(Cl)C=CC2=C1CNCC2CCCCN(C[C@@H]3[C@@H](O)[C@@H](O)[C@H](N4C=NC5=C4N=CN=C5N)O3)CC[C@H](N)C(O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)