Other grades of this product :
| Product Name: | 2-D08 | | Synonyms: | 2-D08;4H-1-Benzopyran-4-one, 2-(2,3,4-trihydroxyphenyl)-;2-D08 >=98% (HPLC) | | CAS: | 144707-18-6 | | MF: | C15H10O5 | | MW: | 270.24 | | EINECS: | | Product Categories: | API | | Mol File: | 144707-18-6.mol |
| 2-D08 Chemical Properties |
| 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 |
| WGK Germany | 3 | | HS Code | 2932990090 |
| 2-D08 Usage And Synthesis |
| 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]. | | 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. |
| 2-D08 Preparation Products And Raw materials |
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