2-D08
Catalogue Number: C4445-APE
| Manufacturer: | Apexbio |
| Molecular Formula: | C15H10O5 |
| Physical state: | A crystalline solid |
| Type: | Other Inhibitors |
| Shipping Condition: | Blue Ice |
| Unit(s): | 10 mg, 25 mg, 5 mg |
Description
Description: 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.
Additional Text
Storage Note
Store at -20°C
Smile String
O=C1C2=CC=CC=C2OC(C3=CC=C(O)C(O)=C3O)=C1
Solubility
≥74.6 mg/mL in DMSO; ≥1.76 mg/mL in EtOH with gentle warming and ultrasonic; insoluble in H2O
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