6-Thioguanine | Anticancer agent / Downregulates DNMT1
NMR (Conforms)
Available Options
| Size : | Price | Quantity | |
|---|---|---|---|
| 100 mg | $30.00 | ||
| 1 gram | $110.00 |
6-Thioguanine (154-42-7) is a DNA methyltransferase inhibitor. After incorporation into DNA, it disrupts cytosine methylation by DNA methyltransferases in vitro and acts as a DNA demethylating agent in vivo.1 It reactivates epigenetically silenced genes in acute lymphoblastic leukemia cells by facilitating proteasome-mediated degradation of DNA methyltransferase (DNMT1).2 Incorporates into DNA and induces double strand breaks which destabilize DNA structure resulting in cytotoxicity.3 Selectively kills BRCA2-defective tumors and overcomes PARP inhibitor resistance in a xenograft model.4 Anticancer and immunosuppressive activity.
References/Citations:
1) Wang and Wang (2009), 6-thioguanine perturbs cytosine methylation at the CpG dinucleotide site by DNA methyltransferases in vitro and acts as a DNA demethylating agent in vivo; Biochemistry, 48 2290
2) Yuan et al. (2011), 6-thioguanine reactivates epigenetically silenced genes in acute lymphoblastic leukemia cells by facilitating proteasome-mediated degradation of DNMT1; Cancer Res., 71 1904
3) Bohon and de los Santos (2005), Effect of 6-thioguanine on the stability of duplex DNA; Nucleic Acid Res., 33 2880
4) Issaeva et al. (2010), 6-thioguanine selectively kills BRCA2-defective tumors and overcomes PARP inhibitor resistance; Cancer Res., 70 6268
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
6-Thioguanine (154-42-7) is a DNA methyltransferase inhibitor. After incorporation into DNA, it disrupts cytosine methylation by DNA methyltransferases in vitro and acts as a DNA demethylating agent in vivo.1 It reactivates epigenetically silenced genes in acute lymphoblastic leukemia cells by facilitating proteasome-mediated degradation of DNA methyltransferase (DNMT1).2 Incorporates into DNA and induces double strand breaks which destabilize DNA structure resulting in cytotoxicity.3 Selectively kills BRCA2-defective tumors and overcomes PARP inhibitor resistance in a xenograft model.4 Anticancer and immunosuppressive activity.
References/Citations:
1) Wang and Wang (2009), 6-thioguanine perturbs cytosine methylation at the CpG dinucleotide site by DNA methyltransferases in vitro and acts as a DNA demethylating agent in vivo; Biochemistry, 48 2290
2) Yuan et al. (2011), 6-thioguanine reactivates epigenetically silenced genes in acute lymphoblastic leukemia cells by facilitating proteasome-mediated degradation of DNMT1; Cancer Res., 71 1904
3) Bohon and de los Santos (2005), Effect of 6-thioguanine on the stability of duplex DNA; Nucleic Acid Res., 33 2880
4) Issaeva et al. (2010), 6-thioguanine selectively kills BRCA2-defective tumors and overcomes PARP inhibitor resistance; Cancer Res., 70 6268
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