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Biological Activity for 6-Thioguanine
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 (PLpro; IC50 = 5 μM for PLpro deubiquitination activity).
Technical Data for 6-Thioguanine
|Storage||Store at RT|
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 6-Thioguanine
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for 6-Thioguanine
The following data is based on the product molecular weight 167.19. 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.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||5.98 mL||29.91 mL||59.81 mL|
|5 mM||1.2 mL||5.98 mL||11.96 mL|
|10 mM||0.6 mL||2.99 mL||5.98 mL|
|50 mM||0.12 mL||0.6 mL||1.2 mL|
References for 6-Thioguanine
References are publications that support the biological activity of the product.
Wang and Wang (2009) 6-Thioguanine perturbs cytosine methylation at CgP dinucleotide site by DNA methyltransferases in vitro and acts as a DNA demethylating agent in vivo. Biochemistry 48 2290 PMID: 19236003
Issaeva et al (2010) 6-Thioguanine selectively kills BRCA2-defective tumors and overcomes PARP inhibitor resistance. Cancer Res. 70 6268 PMID: 20631063
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 PMID: 21239472
If you know of a relevant reference for 6-Thioguanine, please let us know.
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Citations for 6-Thioguanine
Citations are publications that use Tocris products.
Currently there are no citations for 6-Thioguanine. Do you know of a great paper that uses 6-Thioguanine from Tocris? Please let us know.
Reviews for 6-Thioguanine
Average Rating: 5 (Based on 1 Review.)
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