Isofistularin-3
Isofistularin-3 is a direct, DNA-competitive DNMT1 inhibitor, with an IC50 of 13.5 μM. Isofistularin-3, as a DNA demethylating agent, induces cell cycle arrest and sensitization to TRAIL in cancer cells. Isofistularin-3 can be used as an ADC cytotoxin.
For research use only. We do not sell to patients.
- Formula: C31H30Br6N4O11
- Molecular Weight:1114.01
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
All DNA Methyltransferase Isoforms
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Biological Activity
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DNMT1 13.5 μM (IC50) |
Traditional Cytotoxic Agents |
Isofistularin-3 (1-50 μM; 24-72 hours) shows a marked reduction of cell proliferation[1].
Isofistularin-3 (5-50 μM; 24 hours) increases arrests cancer cells in G0/G1 cell cycle phase[1].
Isofistularin-3 (25 μM; 72 hours) increases AHR expression[1].
Isofistularin-3 induces AHR promoter demethylation. Isofistularin-3 (72 hours) inhibits a broader panel of cancer cell lines proliferation, with the GI50s ranging from 7.3-14.8 μM. Isofistularin-3 induces morphological changes and autophagy in RAJI cells. Isofistularin-3 induces caspase-dependent and -independent cell death. Isofistularin-3 sensitizes lymphoma cells to TRAIL-induced apoptosis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RAJI and U-937 lymphoma cells
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Concentration:1, 5, 15, 25, 50 μM
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Incubation Time:24 and 72 hours
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Result:A marked reduction of cell proliferation.
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Cell Line:RAJI and U-937 cells
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Concentration:5, 50 μM
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Incubation Time:24 hours
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Result:An arrest in the G0/G1 phase of the cell cycle for both cell lines.
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Cell Line:RAJI cells
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Concentration:25 μM
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Incubation Time:72 h
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Result:AHR mRNA expression level was 5.1 times higher.
Chemical Information
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Molecular Weight 1114.01
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Formula C31H30Br6N4O11
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SMILES
COC1=C(Br)[C@H](O)[C@@]2(ON=C(C(NC[C@H](O)COC3=C(Br)C=C([C@H](O)CNC(C4=NO[C@]5(C4)C=C(Br)C(OC)=C(Br)[C@H]5O)=O)C=C3Br)=O)C2)C=C1Br
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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