6-Thioguanine

Biological Activity

6-Thioguanine is an anticancer and immunosuppressive agent often used to treat immune disorders and leukemia. Displays cytotoxic and antineoplastic properties; disrupts cytosine methylation by DNA methyltransferases after incorporation into DNA. Selectively kills BRCA2-defective tumors in a xenograft model. Also facilitates proteasome-mediated degradation of DNA (cytosine-5)-methyltransferase 1 (DNMT1). Also inhibits SARS-CoV papain-like protease (PL^pro; IC₅₀ = 5 μM for PL^pro deubiquitination activity).

Technical Data

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.

Background References

1. 6-thioguanine reactivates epigenetically silenced genes in acute lymphoblastic leukemia cells by facilitating proteasome-mediated degradation of DNMT1.
   Yuan et al.
   Cancer Res., 2011;71:1904
2. 6-Thioguanine perturbs cytosine methylation at CgP dinucleotide site by DNA methyltransferases in vitro and acts as a DNA demethylating agent in vivo.
   Wang and Wang
   Biochemistry, 2009;48:2290
3. 6-Thioguanine selectively kills BRCA2-defective tumors and overcomes PARP inhibitor resistance.
   Issaeva et al.
   Cancer Res., 2010;70:6268

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