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2-D08

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Chemical Structure| 144707-18-6 同义名 : -
CAS号 : 144707-18-6
货号 : A725415
分子式 : C15H10O5
纯度 : 99%+
分子量 : 270.237
MDL号 : MFCD27995567
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 145 mg/mL(536.57 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
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 Aβ1 - 42Myc 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.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.70mL

0.74mL

0.37mL

18.50mL

3.70mL

1.85mL

37.00mL

7.40mL

3.70mL
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.