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Description: FTO (mRNA N6-methyladenine demethylase) inhibitor; also inhibits ALKBH2 and ALKBH3
Chemical Name: 9,10-Dihydro-4,5-dihydroxy-9,10-dioxo-2-anthracenecarboxylic acid
Purity: ≥98% (HPLC)

Biological Activity for Rhein

Rhein 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.

Technical Data for Rhein

M. Wt 284.22
Formula C15H8O6
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 478-43-3
PubChem ID 10168
Smiles OC(=O)C1=CC2=C(C(O)=C1)C(=O)C1=C(O)C=CC=C1C2=O

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.

Solubility Data for Rhein

Solvent Max Conc. mg/mL Max Conc. mM
1.1eq. NaOH 28.42 100

Preparing Stock Solutions for Rhein

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.

Select a batch to recalculate based on the batch molecular weight:
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

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References for Rhein

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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