MC3817 free base
MC3817 free base is a selective DNMT1 inhibitor. MC3817 free base inhibits DNMT1 and DNMT3A/3L with IC50s of 0.044 μM and > 10μM, respectively. MC3817 free base inhibits P53-dependent cancer cell proliferation, induces apoptosis and DNA damage. MC3817 free base elevates cleaved Caspase 3, P53, and γH2AX. MC3817 free base can be used in non-small cell lung cancer, colon cancer, cervical cancer, triple-negative breast cancer and histiocytic lymphoma research.
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- Formule: C33H37N9O
- Masse moléculaire:575.71
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
Description
IC50 & Target
[1]|
DNMT1 0.044 μM (IC50) |
In Vitro
MC3817 (compound 14) (0.05-100 μM, 48 h) free base exhibits antiproliferative activity against A549 and H460 (non-small cell and lung cancer), HCT-116 (colon cancer), HeLa (cervical cancer), MDA-MB-231 (triple-negative breast cancer), and U937 (histiocytic lymphoma) cells[1].
MC3817 (2 μM, 24-48 h) free base induces S/G2M phase arrest and triggers apoptotic cell death in HCT-116 cells[1].
MC3817 (0.5-5 μM, 16-48 h) free base triggers DNA damage and activates the p53/γH2AX pathway, leading to cell-cycle arrest and apoptosis in HCT 116 cells[1].
MC3817 (2.5 μM, 48 h) free base induces a much higher level of apoptosis in HCT-116 P53 WT cells compared with HCT-116 P53-/- cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549 , H460, HCT-116, HeLa , MDA-MB 231, and U937
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Concentration:0.05-100 μM
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Incubation Time:48 h
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Result:Had IC50 values of 5.5 μM, 6.8 μM, 0.4 μM, 4.2 μM, 1.9 μM and 5.5 μM for A549 cells, H460 cells, HCT-116 cells, HeLa cells, MDA-MB 231 cells, and U937 cells.
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Cell Line:HCT-116 cells
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Concentration:2 μM
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Incubation Time:48 h
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Result:Caused a block in the S/G2M phase associated with apoptotic cell death, affecting over 50% of the cells after 48 h.
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Cell Line:HCT-116 colon cancer cells
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Concentration:0.5, 1, 2.5, 5 μM
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Incubation Time:48 h
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Result:Induced the accumulation of γH2AX and elevated p53 levels, indicating p53 stabilization and activation in response to DNA damage.
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Cell Line:HCT-116 P53-/- cells and HCT-116 P53 WT cells.
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Concentration:2.5 μM
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Incubation Time:48 h
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Result:Induced apoptotic cell death, as evidenced by significant PI/Annexin V fluorescence and extensive membrane blebbing in both cell lines.
Chemical Information
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Masse moléculaire 575.71
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Formule C33H37N9O
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SMILES
O=C(NC1=CC(CN(C)C)=CC(NC2=NC(N)=NC(C)=C2)=C1)C3=CC(CN(C)C)=CC(NC4=C5C=CC=CC5=NC=C4)=C3
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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.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MC3817 free base Related Classifications
HY-179409A Related Classifications
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