87099-50-1
基本信息
1-Oxa-2-azaspiro[4.5]deca-2,6,8-triene-3-carboxamide, 7,9-dibromo-N-[(2R)-3-[2,6-dibromo-4-[2-[[[(5S,10R)-7,9-dibromo-10-hydroxy-8-methoxy-1-oxa-2-azaspiro[4.5]deca-2,6,8-trien-3-yl]carbonyl]amino]-1-hydroxyethyl]phenoxy]-2-hydroxypropyl]-10-hydroxy-8-methoxy-, (5S,10R)-
物理化学性质
| 密度 | 2.19±0.1 g/cm3(Predicted) |
| 酸度系数(pKa) | 10.66±0.70(Predicted) |
| 形态 | 白色至类白色无定形固体 |
安全数据
| 危险性符号(GHS) |  GHS07 |
| 警示词 | 警告 |
| 危险性描述 | H315-H319-H335 |
| 防范说明 | P271-P261 |
常见问题列表
|
DNMT1 13.5 μM (IC 50 ) |
Traditional Cytotoxic Agents
|
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. Isofistularin-3 (72 hours) inhibits a broader panel of cancer cell lines proliferation, with the GI
50
s 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.
Cell Proliferation Assay
| 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
| 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
| Cell Line: | RAJI cells |
| Concentration: | 25 μM |
| Incubation Time: | 72 h |
| Result: | AHR mRNA expression level was 5.1 times higher. |