|2',3',4'-三羟基黄酮|CsnPharm

CAS No.: 144707-18-6

2-D08/2',3',4'-三羟基黄酮 Catalog No. CSN20235

Synonyms: 2';3';4'-trihydroxy flavone

2-D08 interacts with amyloid β, showing an anti-aggregatory and neuroprotective effect.

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技术信息

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描述The small ubiquitin-like modifier (SUMO) modification, also called sumoylation, is a posttranslational modification of protein substrates, which is essential in cellular stress response. 2',3',4'-Trihydroxyflavone (2-D08) is a synthetic oxygenated flavonoid that inhibits sumoylation with an IC50 of 6 μM. The treatment of 2-D08 for 90 min in vitro inhibited the conjugation of SUMO-1, SUMO-2, and SUMO-3 to IκBα dose-dependently from 1 - 30 μM. The incubation of 30 μM 2-D08 for 6 hours inhibited the sumoylation of topoisomerase-I in BT-474 breast cancer cell lines. A significant overall inhibition of fibril formation was observed in the presence of 100μM 2-D08 at 48 hours. The incubation of 0.1 – 2 μM Aβ_{1 - 42}Myc lymphoma cells 48 hour after the exposure, followed by rapid growth arrest and apoptotic cell death. When incubated with 75 μM 2-D08 for 24 hours, the fold change of the sub-G1 fraction in P493-6 lymphoma cells treated without tetracycline (Myc-off) were significantly lower than that in cells treated with tetracycline (Myc-on).
作用机制2',3',4'-Trihydroxyflavone inhibits protein sumoylation by preventing transfer of SUMO from the UBC9-SUMO thioester to the substrate.
参考文献

[1] Kim YS, Nagy K, et al. An electrophoretic mobility shift assay identifies a mechanistically unique inhibitor of protein sumoylation. Chem Biol. 2013;20(4):604-13.
[2] Marsh DT, Das S, et al. Structure-activity relationships for flavone interactions with amyloid β reveal a novel anti-aggregatory and neuroprotective effect of 2',3',4'-trihydroxyflavone (2-D08). Bioorg Med Chem. 2017;25(14):3827-3834.
[3] Hoellein A, Fallahi M, et al. Myc-induced SUMOylation is a therapeutic vulnerability for B-cell lymphoma. Blood. 2014;124(13):2081-90.
[4] Kim YS, Keyser SG, et al. Synthesis of 2',3',4'-trihydroxyflavone (2-D08), an inhibitor of protein sumoylation. Bioorg Med Chem Lett. 2014;24(4):1094-7.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.7004 mL
- 18.5021 mL
- 37.0041 mL
- 5 mM
- 0.7401 mL
- 3.7004 mL
- 7.4008 mL
- 10 mM
- 0.3700 mL
- 1.8502 mL
- 3.7004 mL

技术信息

CAS号

144707-18-6

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C15H10O5

运输

蓝冰

分子量

270.24

别名

2';3';4'-trihydroxy flavone;2',3',4'-Trihydroxyflavone

溶解度

DMSO	410.0 mg/mL (1517.2 mM)
Water	insoluble

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