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Submit ReviewRhein 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.
分子量 | 284.22 |
公式 | C15H8O6 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 478-43-3 |
PubChem ID | 10168 |
InChI Key | FCDLCPWAQCPTKC-UHFFFAOYSA-N |
Smiles | OC(=O)C1=CC2=C(C(O)=C1)C(=O)C1=C(O)C=CC=C1C2=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
参考文献是支持产品生物活性的出版物。
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
关键词: Rhein, Rhein supplier, mRNA, N6-methyladenine, demethylase, FTO, ALKBH9, 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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