2-D08 |
| Catalog No.GC10408 |
2-D08은 단백질 SUMOylation의 세포 투과성, 기계적 독특한 억제제입니다. 2-D08은 또한 0.49nM의 IC50으로 Axl을 억제합니다.
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.
Cell experiment: | Human lung multi-potent cells at passage 5 are incubated with DMEM+0.5% BSA+penicillin/streptomycin containing either 0.1% DMSO (vehicle) or 2D08 (10 μM) on Permanox culture slides for 6 days. Cells are fixed with 4% PFA for 30 min and then blocked and permeabilized with 10% goat serum and 0.3% Triton-X 100 in PBS for 30 min[2]. |
Animal experiment: | Mice[3]Eight- to 10-week-old mice (both male and female) are used for the study. A 5 cm-long glass pipette is buffered with Mineral Oil and then attached to the injection apparatus to take up 10 μL of 2-D08 (30 μM) or NaCl[3]. |
References: [1]. Kim YS, et al. Synthesis of 2',3',4'-trihydroxyflavone (2-D08), an inhibitor of protein sumoylation. Bioorg Med Chem Lett. 2014 Feb 15;24(4):1094-7. | |
| Cas No. | 144707-18-6 | SDF | |
| Chemical Name | 2-(2,3,4-trihydroxyphenyl)-4H-1-benzopyran-4-one | ||
| Canonical SMILES | O=C1C2=CC=CC=C2OC(C3=CC=C(O)C(O)=C3O)=C1 | ||
| Formula | C15H10O5 | M.Wt | 270.2 |
| Solubility | ≤1mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide | Storage | 4°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.701 mL | 18.5048 mL | 37.0096 mL |
| 5 mM | 0.7402 mL | 3.701 mL | 7.4019 mL |
| 10 mM | 0.3701 mL | 1.8505 mL | 3.701 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 27 reference(s) in Google Scholar.)
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