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Product Infomation
Product Name2-D08
CAS No.144707-18-6
Molecular Weight

270.24

Formula

C₁₅H₁₀O₅

SMILES

O=C1C=C(C2=CC=C(O)C(O)=C2O)OC3=CC=CC=C13

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Product description

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.



IC50 & Target

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IC50: 0.49 nM (Axl)[2]


In Vitro

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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].





Powder-20°C3 years

4°C2 years
In solvent-80°C6 months

-20°C1 month







Peferences:

 [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.