| 2-D08Sumoylation inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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- Purity = 98.00%
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- MSDS (Material Safety Data Sheet)
Chemical structure
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| Cas No. | 144707-18-6 | SDF | Download SDF |
| Chemical Name | 2-(2,3,4-trihydroxyphenyl)-4H-1-benzopyran-4-one | ||
| Canonical SMILES | O=C1C2=CC=CC=C2OC(C3=CC=C(O)C(O)=C3O)=C1 | ||
| Formula | C15H10O5 | M.Wt | 270.2 |
| Solubility | ≤1mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide | Storage | Store at 4°C |
| Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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.
