Isofistularin-3

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

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

Isofistularin-3 Chemical Structure

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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].

IC50 & Target

DNMT1

13.5 μM (IC50)

Traditional Cytotoxic Agents

 

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.

分子量

1114.01

Formula

C31H30Br6N4O11
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.
参考文献

  • [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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