6-Thioguanine

Product Description

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).

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

2 1 Recalculate

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	5.98 mL	29.91 mL	59.81 mL
5 mM	1.20 mL	5.98 mL	11.96 mL
10 mM	0.60 mL	2.99 mL	5.98 mL
50 mM	0.12 mL	0.60 mL	1.20 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Issaeva 6-Thioguanine selectively kills BRCA2-defective tumors and overcomes PARP inhibitor resistance. Cancer Res. 2010 PMID: 20631063
• Yuan 6-thioguanine reactivates epigenetically silenced genes in acute lymphoblastic leukemia cells by facilitating proteasome-mediated degradation of DNMT1. Cancer Res. 2011 PMID: 21239472
• Wang and Wang 6-Thioguanine perturbs cytosine methylation at CgP dinucleotide site by DNA methyltransferases in vitro and acts as a DNA demethylating agent in vivo. Biochemistry 2009 PMID: 19236003