2-D08 |
| Katalog-Nr.GC10408 |
2-D08 ist ein zellgÄngiger, mechanistisch einzigartiger Inhibitor der Protein-SUMOylierung. 2-D08 hemmt auch Axl mit einem IC50 von 0,49 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 144707-18-6
Sample solution is provided at 25 µL, 10mM.
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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.
Average Rating: 5 (Based on Reviews and 27 reference(s) in Google Scholar.)
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