2-D08

Catalog No.S8696 Synonyms: 2',3',4'-trihydroxy flavone

2-D08 Chemical Structure

Molecular Weight(MW): 270.24

2-D08 is a cell permeable, mechanistically unique inhibitor of protein sumoylation. It is also inhibits Axl, IRAK4, ROS1, MLK4, GSK3β, RET, KDR and PI3Kα with IC50 values of 0.49, 3.9, 5.3, 9.8, 11, 11, 17 and 35 nM respectively in biochemical assays.

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Biological Activity

Description 2-D08 is a cell permeable, mechanistically unique inhibitor of protein sumoylation. It is also inhibits Axl, IRAK4, ROS1, MLK4, GSK3β, RET, KDR and PI3Kα with IC50 values of 0.49, 3.9, 5.3, 9.8, 11, 11, 17 and 35 nM respectively in biochemical assays.
Targets
sumoylation [2]
()
Axl [1]
(Cell-free assay)
IRAK4 [1]
(Cell-free assay)
ROS1 [1]
(Cell-free assay)
MLK4 [1]
(Cell-free assay)
0.49 nM 3.9 nM 5.3 nM 9.8 nM
In vitro

2-D08 inhibits sumoylation by preventing transfer of SUMO from the UBC9-SUMO thioester to the substrate[2]. It decreases the ratio of p-Axl to t-Axl in a dose-dependent manner. Suppression of Axl kinase activity by 2D08 disrupts the cytoskeleton and actin filaments with re-organization at cellular junctions as shown by F-actin staining with phalloidin and increased expression of ZO-1 at cellular junctions. It also promotes translocation of β-catenin to cellular junctions and causes an upregulated E-cadherin. 2D08 significantly decreases the migration ability in lung multi-potent cell lines in a dose-dependent manner[1].

Protocol

Kinase Assay:

[1]

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In Vitro Biochemical Kinase Assay:

IC50 values of the Axl kinase inhibitor (2D08) are determined using kinase-mediated phosphorylation of poly-GAT by AlphaScreen luminescence detection technology. The inhibitor is tested at eight points of dilution in duplicate.
Cell Research:

[1]

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  • Cell lines: Human lung multi-potent cells at passage 5
  • Concentrations: 0.1, 1, 10 μM
  • Incubation Time: 3 h (+ 16 h)
  • Method:

    Human lung multi-potent cells at passage 5 are plated at a density of 250 000 cells per well in six-well plates with growth medium. After 24 h, multi-potent cells are incubated with DMEM+0.5% BSA+penicillin/streptomycin containing 0.1% DMSO (vehicle) or 2D08 (0.1, 1, 10 μM) for 3 h in a humidified 5% CO2 incubator at 37℃. These cells are trypsinized and seeded at 20 000 cells per well in three replicates on 12-well cell culture transwell inserts with 8 μm pore size with DMEM+0.5% BSA+penicillin/streptomycin. Lower transwell chambers contained DMEM+10% FBS+penicillin/streptomycin are used to allow cells to migrate. 0.1% DMSO or 2D08 is added to corresponding upper and lower transwell chambers. After 16 h, non-migrated cells are removed by cotton swabs. Migrated cells are fixed with 4% PFA, permeabilized with methanol and stained with crystal violet. The field-images per transwell are taken by an inverted light microscope.


    (Only for Reference)
Animal Research:

[3]

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  • Animal Models: α2−/− mice (Eight- to 10-week-old mice)
  • Formulation: saline
  • Dosages: 30 μM (10 μl)
  • Administration: injected on one hemisphere near the hippocampal area
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 54 mg/mL (199.82 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 270.24
Formula

C15H10O5

CAS No. 144707-18-6
Storage powder
in solvent
Synonyms 2',3',4'-trihydroxy flavone

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID