Isofistularin-3 ((+)-11-epi-Fistularin 3) 是一种直接的 DNA 竞争性DNMT1抑制剂，IC50为 13.5 μM。Isofistularin-3 作为 DNA 去甲基化剂，可诱导肿瘤细胞周期阻滞和 TRAIL 致敏。Isofistularin-3 可作用做抗体偶联药物 (ADC) 的毒素部分。
| 生物活性 | Isofistularin-3 is a direct, DNA-competitiveDNMT1inhibitor, with anIC50of 13.5 μM. Isofistularin-3, as a DNA demethylating agent, induces cell cycle arrest and sensitization to TRAIL incancercells. Isofistularin-3 can be used as anADC cytotoxin[1]. |
| IC50& Target | DNMT1 13.5 μM (IC50) | Traditional Cytotoxic Agents |
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体外研究
(In Vitro) | 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: | RAJI and U-937 lymphoma cells | | Concentration: | 1, 5, 15, 25, 50 μM | | Incubation Time: | 24 and 72 hours | | Result: | A marked reduction of cell proliferation. |
Cell Cycle Analysis[1] | Cell Line: | RAJI and U-937 cells | | Concentration: | 5, 50 μM | | Incubation Time: | 24 hours | | Result: | An arrest in the G0/G1 phase of the cell cycle for both cell lines. |
RT-PCR[1] | Cell Line: | RAJI cells | | Concentration: | 25 μM | | Incubation Time: | 72 h | | Result: | AHR mRNA expression level was 5.1 times higher. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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