Bioactivity | 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[1]. |
Invitro | 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]. Cell Proliferation Assay[1] Cell Line: |
Name | Isofistularin-3 |
Formula | C31H30Br6N4O11 |
Molar Mass | 1114.01 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |