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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.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 284.22. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||3.52 mL||17.59 mL||35.18 mL|
|5 mM||0.7 mL||3.52 mL||7.04 mL|
|10 mM||0.35 mL||1.76 mL||3.52 mL|
|50 mM||0.07 mL||0.35 mL||0.7 mL|
References are publications that support the biological activity of the product.
Chen et al (2012) Development of cell-active N6-methyladenosine RNA demethylase FTO inhibitor. J.Am.Chem.Soc. 134 17963 PMID: 23045983
Svensen and Jaffrey et al (2016) Fluorescent RNA aptamers as a tool to study RNA-modifying enzymes. Cell.Chem.Biol. 23 415 PMID: 26877022
Li et al (2016) Rhein inhibits AlkB repair enzymes and sensitizes cells to methylated DNA damage. J.Biol.Chem. 291 11083 PMID: 27015802
If you know of a relevant reference for Rhein, please let us know.
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Keywords: Rhein, Rhein supplier, mRNA, N6-methyladenine, demethylase, FTO, ALKBH5, Fat, mass, and, obesity-associated, protein, α, alpha-ketoglutarate-dependent, dioxygenase, inhibitors, inhibits, competitive, anti-inflammatory, anticancer, chemosensitizers, chemosensitizing, ALKBH2, ALKBH3, DNA, damage, r, Other, Oxygenases/Oxidases, 6867, Tocris Bioscience
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