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Isofistularin-3
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。
Isofistularin-3 Chemical Structure
| 规格 |
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是否有货 |
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| 100 mg |
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询价 |
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| 250 mg |
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询价 |
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| 500 mg |
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询价 |
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* Please select Quantity before adding items.
| 生物活性 |
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].
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| IC50 & Target |
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DNMT1
13.5 μM (IC50)
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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].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
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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| 分子量 |
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| Formula |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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| 参考文献 |
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[1]. Florean C, et al. Discovery and characterization of Isofistularin-3, a marine brominated alkaloid, as a new DNA demethylating agent inducing cell cycle arrest and sensitization to TRAIL in cancer cells. Oncotarget. 2016 Apr 26;7(17):24027-49.
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