2-D08
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 270.2 |
Cas No. | 144707-18-6 |
Formula | C15H10O5 |
Solubility | ≥74.6 mg/mL in DMSO; ≥1.76 mg/mL in EtOH with gentle warming and ultrasonic; insoluble in H2O |
Chemical Name | 2-(2,3,4-trihydroxyphenyl)-4H-1-benzopyran-4-one |
SDF | Download SDF |
Canonical SMILES | O=C1C2=CC=CC=C2OC(C3=CC=C(O)C(O)=C3O)=C1 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
质量控制和MSDS
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