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2-D08

カタログ番号GC10408

2-D08 は、タンパク質の SUMO 化に対する細胞透過性の機構的にユニークな阻害剤です。 2-D08 は、0.49 nM の IC50 で Axl も阻害します。

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2-D08 化学構造

Cas No.: 144707-18-6

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5mg
$59.00
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10mg
$81.00
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25mg
$186.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

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.
[2]. Fujino N, et al. Phenotypic screening identifies Axl kinase as a negative regulator of an alveolar epithelial cell phenotype. Lab Invest. 2017 Sep;97(9):1047-1062.
[3]. Ghosh H, et al. Several posttranslational modifications act in concert to regulate gephyrin scaffolding and GABAergic transmission. Nat Commun. 2016 Nov 7;7:13365. doi: 10.1038/ncomms13365.

Background

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.

Chemical Properties

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
溶解度 ≤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.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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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
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Average Rating: 5 ★★★★★ (Based on Reviews and 27 reference(s) in Google Scholar.)

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