Chemical Name: 9,10-Dihydro-4,5-dihydroxy-9,10-dioxo-2-anthracenecarboxylic acid
Biological ActivityRhein is a FTO (mRNA N6-methyladenine demethylase) inhibitor (IC50 = 1.2 - 21 μM; Ki = 1.8 μM). Competitively binds enzyme at active site preventing binding of N6-methyladenosine (m6A) substrate and resulting in accumulation of DNA damage in cells. Also inhibits ALKBH3 and ALKBH2 (IC50 values are 5.3 and 9.1 μM, respectively). Sensitizes glioblastoma cells to alkylating agents. Active in vivo.
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For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Fluorescent RNA Aptamers as a Tool to Study RNA-Modifying Enzymes.
Svensen and Jaffrey
Cell Chem.Biol., 2016;23:415
Development of cell-active N6-methyladenosine RNA demethylase FTO inhibitor.
Chen et al.
Rhein inhibits AlkB repair enzymes and sensitizes cells to methylated DNA damage.
Li et al.
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