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Product Details

6-Thioguanine | Anticancer agent / Downregulates DNMT1

6-Thioguanine (154-42-7) is a 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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Focus Biomolecules supplier, chemical structure of 6-Thioguanine | Anticancer agent | Downregulates DNMT1 | CAS 154-42-7

Catalog#  10-1282-0100

$30.00
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CAS:
154-42-7
Catalog Number:
10-1282
Activity:
Anticancer agent / Downregulates DNMT1
Chemical Name:
2-Amino-6-mercaptopurine
Alternate Names:
6-TG; NSC 752, NSC 76504
Molecular Weight:
167.19
Molecular Formula:
C5H5N5S
Solubility:
Soluble in DMF (up to 1.5 mg/ml with warming)
Physical Properties:
Pale yellow solid
Purity:
96% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMF may be stored at -20°C for up to 1 month.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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