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2-D08
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
2-D08图片
CAS NO:144707-18-6
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议

产品介绍

化学性质

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt270.2
Cas No.144707-18-6
FormulaC15H10O5
Solubility≥74.6 mg/mL in DMSO; ≥1.76 mg/mL in EtOH with gentle warming and ultrasonic; insoluble in H2O
Chemical Name2-(2,3,4-trihydroxyphenyl)-4H-1-benzopyran-4-one
Canonical SMILESO=C1C2=CC=CC=C2OC(C3=CC=C(O)C(O)=C3O)=C1
运输条件蓝冰运输或根据您的需求运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。

资料参考

2-D08 (2’,3’,4’-trihydroxyflavone) is a Sumoylation inhibitor.

Protein sumoylation is a dynamic posttranslational modification involved in various biological processes, such as cellular homeostasis and development. Sumoylation has been reported to play a key role in cancer, though so far there are few small molecule probes available.

In vitro: 2-D08 was identified as a cell permeable, mechanistically unique inhibitor of protein sumoylation. This compound was found to be able to block sumoylation of topoisomerase I in two different cancer cell lines when co-dosed with camptothecin. In addition, futher analyses indicated that 2-D08 inhibited sumoylation via preventing transfer of small ubiquitin-like modifier (SUMO) from the UBC9-SUMO thioester to the substrate without affecting SUMO-activating enzyme E1 (SAE-1/2) or E2 Ubc9-SUMO thioester formation, a mechanism of action that was unprecedented before [1]. Moreover, it was found that 2-D08 at 100 μM could effectively inhibit 10 μM Camptothecin induced Topoisomerase I SUMOylation in breast cancer without affecting overall cellular protein ubiquitinations [2].

In vivo: Up to now, there is no animal in vivo data reported for 2-D08.

Clinical trial: So far, no clinical study has been conducted.

References:
[1] Kim YS, Keyser SG, Schneekloth JS Jr.  Synthesis of 2',3',4'-trihydroxyflavone (2-D08), an inhibitor of protein sumoylation. Bioorg Med Chem Lett. 2014 Feb 15;24(4):1094-7.
[2] Kim YS, Nagy K, Keyser S, Schneekloth JS Jr.  An electrophoretic mobility shift assay identifies a mechanistically unique inhibitor of protein sumoylation. Chem Biol. 2013 Apr 18;20(4):604-13.