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Isofistularin-3, a direct DNA-competitive DNMT1 inhibitor with an IC50 of 13.5 μM, functions as a DNA demethylating agent, leading to cell cycle arrest and increased sensitivity to TRAIL in cancer cells. Additionally, it can be employed as an ADC cytotoxin.
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500 mg | Inquiry | Backorder |
Description | Isofistularin-3, a direct DNA-competitive DNMT1 inhibitor with an IC50 of 13.5 μM, functions as a DNA demethylating agent, leading to cell cycle arrest and increased sensitivity to TRAIL in cancer cells. Additionally, it can be employed as an ADC cytotoxin. |
Targets&IC50 | DNMT1:13.5 μM |
In vitro | 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.Isofistularin-3 (1-50 μM; 24-72 hours) shows a marked reduction of cell proliferation. Isofistularin-3 (5-50 μM; 24 hours) increases arrests cancer cells in G0/G1 cell cycle phase. Isofistularin-3 (25 μM; 72 hours) increases AHR expression. Isofistularin-3 induces AHR promoter demethylation. |
Molecular Weight | 1114.01 |
Formula | C31H30Br6N4O11 |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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