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2-D08

Names

[ CAS No. ]:
144707-18-6

[ Name ]:
2-D08

[Synonym ]:
4H-1-Benzopyran-4-one, 2-(2,3,4-trihydroxyphenyl)-
2-(2,3,4-Trihydroxyphenyl)-4H-chromen-4-one
MFCD27995567

Biological Activity

[Description]:

2-D08 is a cell permeable, mechanistically unique inhibitor of protein SUMOylation. 2-D08 also inhibits Axl with an IC50 of 0.49 nM.

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> E1/E2/E3 Enzyme
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> TAM Receptor
Research Areas >> Cancer

[Target]

IC50: 0.49 nM (Axl)[2]


[In Vitro]

2-D08 inhibits sumoylation by preventing transfer of SUMO from the UBC9-SUMO thioester to the substrate[1]. 2-D08 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[2].

[Cell Assay]

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 admin]

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.


[Related Small Molecules]

Bemcentinib (R428) | Gilteritinib | Ginkgolic acid C15:1 | PYR-41 | BMS-777607 | NSC232003 | CC122 | SZL P1-41 | TP-0903 | TAK-243(MLN7243) | LDC1267 | CEP-40783 | 2-Chloro-N-(3,4-dimethoxybenzyl)acetamide | SGI-7079 | UNC2250

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Boiling Point ]:
517.9±50.0 °C at 760 mmHg

[ Molecular Formula ]:
C15H10O5

[ Molecular Weight ]:
270.237

[ Flash Point ]:
201.7±23.6 °C

[ Exact Mass ]:
270.052826

[ LogP ]:
2.77

[ Vapour Pressure ]:
0.0±1.4 mmHg at 25°C

[ Index of Refraction ]:
1.732

[ Storage condition ]:
-20℃

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H302

[ RIDADR ]:
NONH for all modes of transport

Related Compounds