| Chemical Properties | Back Directory | [Boiling point ]
517.9±50.0 °C(Predicted) | [density ]
1.548±0.06 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
≥74.6 mg/mL in DMSO; ≥1.76 mg/mL in EtOH with gentle warming and ultrasonic; insoluble in H2O | [form ]
powder | [pka]
7.45±0.40(Predicted) | [color ]
white to beige |
| Hazard Information | Back Directory | [Uses]
2-D08 has been used as a small ubiquitin-like modifier (SUMO)ylation inhibitor. | [Biological Activity]
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. | [Biochem/physiol Actions]
2-D08 is a potent and cell-permeable inhibitor of sumoylation that block the transfer of SUMO (small ubiquitin-like modifier) from the E2 enzyme (Ubc9) thioester conjugate to the substrate. | [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]. | [IC 50]
Axl | [storage]
4°C, protect from light | [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. |
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